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PD-0332991 (Palbociclib) Hydrochloride inhibiteur de CDK4/6
N° Cat.S1116
Structure chimique
Poids moléculaire: 483.99
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Contrôle qualité
Lot :
Pureté :
99.99%
99.99
Produits Souvent Utilisés Avec PD-0332991 (Palbociclib) Hydrochloride
Culture cellulaire, traitement et concentration de travail
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | PMID |
|---|---|---|---|---|---|---|
| MOLM13 | Kinase Assay | 24 h | Inhibition of CDK4 assessed as inhibition of Rb phosphorylation with IC50 of 0.002 μM | 24641103 | ||
| COLO205 | Growth Inhibition Assay | 72 h | Antiproliferative activity assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.036 μM | 24641103 | ||
| U937 | Growth Inhibition Assay | 72 h | Antiproliferative activity assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.14 μM | 24641103 | ||
| MOLM13 | Growth Inhibition Assay | 72 h | Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.096 μM | 24641103 | ||
| MOLM13 | Growth Inhibition Assay | 72 h | Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.096 μM | 24641103 | ||
| MDA-MB-435 | Growth Inhibition Assay | 24 h | IC50=0.16 μM | 15801831 | ||
| K562 | Cytotoxic Assay | 96 h | DMSO | IC50=2 μM | 24417566 | |
| DU145 | Cytotoxic Assay | 96 h | DMSO | IC50=7.5 μM | 24417566 | |
| MDA-MB-231 | Growth Inhibition Assay | 1 μM | 24 h | DMSO | Cell cycle arrest assessed as accumulation at G1 phase | 24417566 |
| MCF7 | Growth Inhibition Assay | 1 μM | 24 h | DMSO | Cell cycle arrest assessed as accumulation at G1 phase | 24417566 |
| MCF7 | Kinase Assay | 5 μM | 24 h | DMSO | Inhibition of recombinant CDK4/cyclinD1 assessed as inhibition of retinoblastoma phosphorylation at Ser780 | 24417566 |
| MDA-MB-231 | Kinase Assay | 5 μM | 24 h | DMSO | Inhibition of recombinant CDK4/cyclinD1 assessed as inhibition of retinoblastoma phosphorylation at Ser780 | 24417566 |
| MDA-MB-231 | Function Assay | 1-10 μM | 24 h | DMSO | does not induce apoptosis assessed as PARP cleavage | 24417566 |
| MCF7 | Function Assay | 1-10 μM | 24 h | DMSO | does not induce apoptosis assessed as PARP cleavage | 24417566 |
| MDA-MB-231 | Function Assay | 0.5-1 μM | 48 h | DMSO | has no Cell cycle arrest assessed as accumulation at sub-G1 phase | 24417566 |
| MCF7 | Function Assay | 0.5-1 μM | 48 h | DMSO | has no Cell cycle arrest assessed as accumulation at sub-G1 phase | 24417566 |
| MOLM13 | CDK4 inhibition assay | 24 h | IC50 = 0.011 μM | 24641103 | ||
| A2780 | Growth inhibition assay | 72 h | GI50 = 0.032 μM | 28156111 | ||
| COLO205 | Antiproliferative activity assay | 72 h | IC50 = 0.036 μM | 24641103 | ||
| MV4-11 | Growth inhibition assay | 72 h | GI50 = 0.05 μM | 28156111 | ||
| MOLM13 | Growth inhibition assay | 72 h | GI50 = 0.062 μM | 28156111 | ||
| NB4 | Growth inhibition assay | 72 h | GI50 = 0.066 μM | 28156111 | ||
| PC3 | Growth inhibition assay | 72 h | GI50 = 0.071 μM | 28156111 | ||
| MOLM13 | Antiproliferative activity assay | 72 h | IC50 = 0.096 μM | 24641103 | ||
| MOLM13 | Antiproliferative activity assay | 72 h | IC50 = 0.096 μM | 24641103 | ||
| MDA-MB-453 | Cytotoxicity assay | 48 h | IC50 = 0.137 μM | 27448913 | ||
| U937 | Antiproliferative activity assay | 72 h | IC50 = 0.14 μM | 24641103 | ||
| MDA-MB-435 | Antiproliferative activity assay | 24 h | IC50 = 0.16 μM | 26115571 | ||
| MCF7 | Cytotoxicity assay | 48 h | IC50 = 0.24 μM | 27448913 | ||
| MDA-MB-453 | Growth inhibition assay | 72 h | GI50 = 0.326 μM | 28156111 | ||
| MCF7 | Growth inhibition assay | 72 h | GI50 = 0.557 μM | 28156111 | ||
| MDA-MB-231 | Cytotoxicity assay | 48 h | IC50 = 0.58 μM | 27448913 | ||
| M229 | Growth inhibition assay | 72 h | GI50 = 1.22 μM | 28156111 | ||
| M238 | Growth inhibition assay | 72 h | GI50 = 1.97 μM | 28156111 | ||
| M249 | Growth inhibition assay | 72 h | GI50 = 1.99 μM | 28156111 | ||
| K562 | Cytotoxicity assay | 96 h | IC50 = 2 μM | 24417566 | ||
| M249R | Growth inhibition assay | 72 h | GI50 = 2.96 μM | 28156111 | ||
| MOLM13 | FLT3 inhibition assay | 24 h | IC50 = 3 μM | 24641103 | ||
| MDA-MB-468 | Antiproliferative activity assay | 24 h | IC50 = 3 μM | 26115571 | ||
| C4-2B | Growth inhibition assay | 72 h | GI50 = 4.15 μM | 28156111 | ||
| DU145 | Growth inhibition assay | 72 h | GI50 = 5.792 μM | 28156111 | ||
| MDA-MB-468 | Growth inhibition assay | 72 h | GI50 = 5.96 μM | 28156111 | ||
| BPH1 | Growth inhibition assay | 72 h | GI50 = 7.442 μM | 28156111 | ||
| DU145 | Cytotoxicity assay | 96 h | IC50 = 7.5 μM | 24417566 | ||
| MRC5 | Growth inhibition assay | 72 h | GI50 = 10 μM | 28156111 | ||
| 697 | Growth Inhibition Assay | IC50=148.38 nM | SANGER | |||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=96.04 nM | SANGER | |||
| NB69 | Growth Inhibition Assay | IC50=161.8 nM | SANGER | |||
| EoL-1 | Growth Inhibition Assay | IC50=187.26 nM | SANGER | |||
| BHT-101 | Growth Inhibition Assay | IC50=198.25 nM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=220.02 nM | SANGER | |||
| MHH-NB-11 | Growth Inhibition Assay | IC50=220.19 nM | SANGER | |||
| AsPC-1 | Growth Inhibition Assay | IC50=252.53 nM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=256.25 nM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=258.19 nM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=258.49 nM | SANGER | |||
| ES7 | Growth Inhibition Assay | IC50=273.09 nM | SANGER | |||
| KY821 | Growth Inhibition Assay | IC50=314.1 nM | SANGER | |||
| RT-112 | Growth Inhibition Assay | IC50=321.05 nM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=340.66 nM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=345.13 nM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=376.16 nM | SANGER | |||
| SK-N-AS | Growth Inhibition Assay | IC50=387.83 nM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=405.02 nM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=411.89 nM | SANGER | |||
| HTC-C3 | Growth Inhibition Assay | IC50=432.95 nM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=444.27 nM | SANGER | |||
| KOSC-2 | Growth Inhibition Assay | IC50=466.9 nM | SANGER | |||
| NB14 | Growth Inhibition Assay | IC50=483.58 nM | SANGER | |||
| CAL-27 | Growth Inhibition Assay | IC50=494.59 nM | SANGER | |||
| H9 | Growth Inhibition Assay | IC50=495.43 nM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=504.73 nM | SANGER | |||
| PA-1 | Growth Inhibition Assay | IC50=509.86 nM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=513.85 nM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=521.62 nM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=526.86 nM | SANGER | |||
| HGC-27 | Growth Inhibition Assay | IC50=564.99 nM | SANGER | |||
| CHP-212 | Growth Inhibition Assay | IC50=593.59 nM | SANGER | |||
| NB10 | Growth Inhibition Assay | IC50=599.18 nM | SANGER | |||
| HH | Growth Inhibition Assay | IC50=599.43 nM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=603.52 nM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=605.21 nM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=605.67 nM | SANGER | |||
| A204 | Growth Inhibition Assay | IC50=633.91 nM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=636.99 nM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=650.64 nM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=652.48 nM | SANGER | |||
| ONS-76 | Growth Inhibition Assay | IC50=677.82 nM | SANGER | |||
| KM-H2 | Growth Inhibition Assay | IC50=695.54 nM | SANGER | |||
| D-263MG | Growth Inhibition Assay | IC50=717.12 nM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=728.93 nM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=732.27 nM | SANGER | |||
| NBsusSR | Growth Inhibition Assay | IC50=742.99 nM | SANGER | |||
| NCI-H520 | Growth Inhibition Assay | IC50=746.52 nM | SANGER | |||
| ES5 | Growth Inhibition Assay | IC50=752.8 nM | SANGER | |||
| T-24 | Growth Inhibition Assay | IC50=778.71 nM | SANGER | |||
| SW962 | Growth Inhibition Assay | IC50=808.63 nM | SANGER | |||
| EW-3 | Growth Inhibition Assay | IC50=808.76 nM | SANGER | |||
| RXF393 | Growth Inhibition Assay | IC50=812.79 nM | SANGER | |||
| U251 | Growth Inhibition Assay | IC50=813.88 nM | SANGER | |||
| CAMA-1 | Growth Inhibition Assay | IC50=833.94 nM | SANGER | |||
| JVM-3 | Growth Inhibition Assay | IC50=851.78 nM | SANGER | |||
| COLO-800 | Growth Inhibition Assay | IC50=897.78 nM | SANGER | |||
| OVCAR-5 | Growth Inhibition Assay | IC50=900.1 nM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=927.56 nM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=929.41 nM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=936.06 nM | SANGER | |||
| Mewo | Growth Inhibition Assay | IC50=936.6 nM | SANGER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=940.55 nM | SANGER | |||
| HO-1-N-1 | Growth Inhibition Assay | IC50=962.81 nM | SANGER | |||
| HSC-3 | Growth Inhibition Assay | IC50=966.48 nM | SANGER | |||
| TYK-nu | Growth Inhibition Assay | IC50=998.25 nM | SANGER | |||
| KYSE-150 | Growth Inhibition Assay | IC50=1.00076 μM | SANGER | |||
| SN12C | Growth Inhibition Assay | IC50=1.00875 μM | SANGER | |||
| MOLT-13 | Growth Inhibition Assay | IC50=1.01421 μM | SANGER | |||
| TE-11 | Growth Inhibition Assay | IC50=1.04812 μM | SANGER | |||
| DB | Growth Inhibition Assay | IC50=1.07273 μM | SANGER | |||
| CAL-39 | Growth Inhibition Assay | IC50=1.07522 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=1.08408 μM | SANGER | |||
| CHP-134 | Growth Inhibition Assay | IC50=1.11807 μM | SANGER | |||
| TGW | Growth Inhibition Assay | IC50=1.12395 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=1.13134 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=1.16354 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=1.17186 μM | SANGER | |||
| MHH-ES-1 | Growth Inhibition Assay | IC50=1.17986 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=1.1862 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=1.20734 μM | SANGER | |||
| COR-L23 | Growth Inhibition Assay | IC50=1.22933 μM | SANGER | |||
| BFTC-905 | Growth Inhibition Assay | IC50=1.24267 μM | SANGER | |||
| Hs-578-T | Growth Inhibition Assay | IC50=1.25817 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=1.26686 μM | SANGER | |||
| HEL | Growth Inhibition Assay | IC50=1.29338 μM | SANGER | |||
| A549 | Growth Inhibition Assay | IC50=1.29399 μM | SANGER | |||
| COLO-741 | Growth Inhibition Assay | IC50=1.32089 μM | SANGER | |||
| PC-3 | Growth Inhibition Assay | IC50=1.35221 μM | SANGER | |||
| HOS | Growth Inhibition Assay | IC50=1.35296 μM | SANGER | |||
| HT-1080 | Growth Inhibition Assay | IC50=1.37519 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=1.41774 μM | SANGER | |||
| BHY | Growth Inhibition Assay | IC50=1.46923 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=1.50528 μM | SANGER | |||
| HN | Growth Inhibition Assay | IC50=1.54071 μM | SANGER | |||
| NCI-H441 | Growth Inhibition Assay | IC50=1.54907 μM | SANGER | |||
| RPMI-8866 | Growth Inhibition Assay | IC50=1.58507 μM | SANGER | |||
| CAL-62 | Growth Inhibition Assay | IC50=1.60862 μM | SANGER | |||
| MG-63 | Growth Inhibition Assay | IC50=1.61813 μM | SANGER | |||
| SK-LU-1 | Growth Inhibition Assay | IC50=1.62152 μM | SANGER | |||
| BCPAP | Growth Inhibition Assay | IC50=1.66457 μM | SANGER | |||
| 22RV1 | Growth Inhibition Assay | IC50=1.67843 μM | SANGER | |||
| T47D | Growth Inhibition Assay | IC50=1.68061 μM | SANGER | |||
| MSTO-211H | Growth Inhibition Assay | IC50=1.69603 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=1.70273 μM | SANGER | |||
| H4 | Growth Inhibition Assay | IC50=1.73212 μM | SANGER | |||
| CAL-51 | Growth Inhibition Assay | IC50=1.74855 μM | SANGER | |||
| ABC-1 | Growth Inhibition Assay | IC50=1.78582 μM | SANGER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=1.79542 μM | SANGER | |||
| YKG-1 | Growth Inhibition Assay | IC50=1.81061 μM | SANGER | |||
| KM12 | Growth Inhibition Assay | IC50=1.81602 μM | SANGER | |||
| L-363 | Growth Inhibition Assay | IC50=1.87412 μM | SANGER | |||
| KU812 | Growth Inhibition Assay | IC50=1.89282 μM | SANGER | |||
| LOXIMVI | Growth Inhibition Assay | IC50=1.91228 μM | SANGER | |||
| G-401 | Growth Inhibition Assay | IC50=1.92428 μM | SANGER | |||
| SW780 | Growth Inhibition Assay | IC50=1.96246 μM | SANGER | |||
| SW872 | Growth Inhibition Assay | IC50=1.9833 μM | SANGER | |||
| NB7 | Growth Inhibition Assay | IC50=1.99323 μM | SANGER | |||
| T98G | Growth Inhibition Assay | IC50=2.00666 μM | SANGER | |||
| SW1710 | Growth Inhibition Assay | IC50=2.06945 μM | SANGER | |||
| NCI-H1573 | Growth Inhibition Assay | IC50=2.07298 μM | SANGER | |||
| KE-37 | Growth Inhibition Assay | IC50=2.08951 μM | SANGER | |||
| 786-0 | Growth Inhibition Assay | IC50=2.15439 μM | SANGER | |||
| SAS | Growth Inhibition Assay | IC50=2.20374 μM | SANGER | |||
| CAL-54 | Growth Inhibition Assay | IC50=2.20413 μM | SANGER | |||
| SF268 | Growth Inhibition Assay | IC50=2.23122 μM | SANGER | |||
| SW620 | Growth Inhibition Assay | IC50=2.26169 μM | SANGER | |||
| MN-60 | Growth Inhibition Assay | IC50=2.3106 μM | SANGER | |||
| EFO-27 | Growth Inhibition Assay | IC50=2.32058 μM | SANGER | |||
| NCI-H747 | Growth Inhibition Assay | IC50=2.32199 μM | SANGER | |||
| HCC2218 | Growth Inhibition Assay | IC50=2.35374 μM | SANGER | |||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=2.36437 μM | SANGER | |||
| SJSA-1 | Growth Inhibition Assay | IC50=2.37796 μM | SANGER | |||
| RKO | Growth Inhibition Assay | IC50=2.38496 μM | SANGER | |||
| NB6 | Growth Inhibition Assay | IC50=2.40374 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=2.45422 μM | SANGER | |||
| EGI-1 | Growth Inhibition Assay | IC50=2.46883 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=2.52773 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=2.55951 μM | SANGER | |||
| GT3TKB | Growth Inhibition Assay | IC50=2.59199 μM | SANGER | |||
| SK-HEP-1 | Growth Inhibition Assay | IC50=2.59266 μM | SANGER | |||
| GAMG | Growth Inhibition Assay | IC50=2.59394 μM | SANGER | |||
| SK-MES-1 | Growth Inhibition Assay | IC50=2.61803 μM | SANGER | |||
| RO82-W-1 | Growth Inhibition Assay | IC50=2.62057 μM | SANGER | |||
| ECC10 | Growth Inhibition Assay | IC50=2.70206 μM | SANGER | |||
| MCF7 | Growth Inhibition Assay | IC50=2.71464 μM | SANGER | |||
| D-283MED | Growth Inhibition Assay | IC50=2.7243 μM | SANGER | |||
| RPMI-7951 | Growth Inhibition Assay | IC50=2.75694 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=2.77099 μM | SANGER | |||
| KGN | Growth Inhibition Assay | IC50=2.81884 μM | SANGER | |||
| NUGC-3 | Growth Inhibition Assay | IC50=2.82505 μM | SANGER | |||
| NCI-H292 | Growth Inhibition Assay | IC50=2.85053 μM | SANGER | |||
| Becker | Growth Inhibition Assay | IC50=2.95832 μM | SANGER | |||
| NCI-H1299 | Growth Inhibition Assay | IC50=3.05263 μM | SANGER | |||
| ETK-1 | Growth Inhibition Assay | IC50=3.0543 μM | SANGER | |||
| TK10 | Growth Inhibition Assay | IC50=3.20165 μM | SANGER | |||
| VMRC-RCZ | Growth Inhibition Assay | IC50=3.36488 μM | SANGER | |||
| YH-13 | Growth Inhibition Assay | IC50=3.44079 μM | SANGER | |||
| DU-145 | Growth Inhibition Assay | IC50=3.46269 μM | SANGER | |||
| SW1088 | Growth Inhibition Assay | IC50=3.4747 μM | SANGER | |||
| HOP-92 | Growth Inhibition Assay | IC50=3.50342 μM | SANGER | |||
| KP-N-YS | Growth Inhibition Assay | IC50=3.62139 μM | SANGER | |||
| NCI-H460 | Growth Inhibition Assay | IC50=3.6673 μM | SANGER | |||
| U-2-OS | Growth Inhibition Assay | IC50=3.72535 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=3.76936 μM | SANGER | |||
| MDA-MB-231 | Growth Inhibition Assay | IC50=3.81951 μM | SANGER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=3.832 μM | SANGER | |||
| COR-L105 | Growth Inhibition Assay | IC50=4.018 μM | SANGER | |||
| NCI-H1437 | Growth Inhibition Assay | IC50=4.02302 μM | SANGER | |||
| CAL-85-1 | Growth Inhibition Assay | IC50=4.02461 μM | SANGER | |||
| MZ1-PC | Growth Inhibition Assay | IC50=4.18556 μM | SANGER | |||
| VM-CUB-1 | Growth Inhibition Assay | IC50=4.31284 μM | SANGER | |||
| CHL-1 | Growth Inhibition Assay | IC50=4.32169 μM | SANGER | |||
| MDA-MB-361 | Growth Inhibition Assay | IC50=4.33153 μM | SANGER | |||
| NCI-H661 | Growth Inhibition Assay | IC50=4.50092 μM | SANGER | |||
| EW-11 | Growth Inhibition Assay | IC50=4.52231 μM | SANGER | |||
| BEN | Growth Inhibition Assay | IC50=4.52815 μM | SANGER | |||
| BFTC-909 | Growth Inhibition Assay | IC50=4.56275 μM | SANGER | |||
| NCI-H2087 | Growth Inhibition Assay | IC50=4.58164 μM | SANGER | |||
| RVH-421 | Growth Inhibition Assay | IC50=4.6669 μM | SANGER | |||
| P30-OHK | Growth Inhibition Assay | IC50=4.68008 μM | SANGER | |||
| NCI-H28 | Growth Inhibition Assay | IC50=4.81661 μM | SANGER | |||
| ES6 | Growth Inhibition Assay | IC50=4.83016 μM | SANGER | |||
| 769-P | Growth Inhibition Assay | IC50=4.85926 μM | SANGER | |||
| OE33 | Growth Inhibition Assay | IC50=4.88161 μM | SANGER | |||
| SW982 | Growth Inhibition Assay | IC50=4.95061 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=5.02983 μM | SANGER | |||
| TI-73 | Growth Inhibition Assay | IC50=5.06194 μM | SANGER | |||
| HCT-116 | Growth Inhibition Assay | IC50=5.09889 μM | SANGER | |||
| HuP-T3 | Growth Inhibition Assay | IC50=5.18709 μM | SANGER | |||
| G-402 | Growth Inhibition Assay | IC50=5.19416 μM | SANGER | |||
| NCI-H1792 | Growth Inhibition Assay | IC50=5.24622 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=5.25942 μM | SANGER | |||
| NCI-H1650 | Growth Inhibition Assay | IC50=5.30634 μM | SANGER | |||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=5.31808 μM | SANGER | |||
| S-117 | Growth Inhibition Assay | IC50=5.36976 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=5.39681 μM | SANGER | |||
| NCI-H2122 | Growth Inhibition Assay | IC50=5.49397 μM | SANGER | |||
| NCI-H1793 | Growth Inhibition Assay | IC50=5.67593 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=5.70088 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=5.80556 μM | SANGER | |||
| LCLC-103H | Growth Inhibition Assay | IC50=5.917 μM | SANGER | |||
| A673 | Growth Inhibition Assay | IC50=5.91932 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=5.9836 μM | SANGER | |||
| SF295 | Growth Inhibition Assay | IC50=6.00422 μM | SANGER | |||
| KU-19-19 | Growth Inhibition Assay | IC50=6.01731 μM | SANGER | |||
| CFPAC-1 | Growth Inhibition Assay | IC50=6.04443 μM | SANGER | |||
| LoVo | Growth Inhibition Assay | IC50=6.05063 μM | SANGER | |||
| 8505C | Growth Inhibition Assay | IC50=6.07573 μM | SANGER | |||
| GMS-10 | Growth Inhibition Assay | IC50=6.15002 μM | SANGER | |||
| Ca9-22 | Growth Inhibition Assay | IC50=6.1671 μM | SANGER | |||
| DOK | Growth Inhibition Assay | IC50=6.22072 μM | SANGER | |||
| FADU | Growth Inhibition Assay | IC50=6.26039 μM | SANGER | |||
| BxPC-3 | Growth Inhibition Assay | IC50=6.2732 μM | SANGER | |||
| CAL-33 | Growth Inhibition Assay | IC50=6.29201 μM | SANGER | |||
| SHP-77 | Growth Inhibition Assay | IC50=6.31512 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=6.33455 μM | SANGER | |||
| GB-1 | Growth Inhibition Assay | IC50=6.382 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=6.38447 μM | SANGER | |||
| D-502MG | Growth Inhibition Assay | IC50=6.42376 μM | SANGER | |||
| LAN-6 | Growth Inhibition Assay | IC50=6.51023 μM | SANGER | |||
| H-EMC-SS | Growth Inhibition Assay | IC50=6.56147 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=6.60076 μM | SANGER | |||
| NCI-H1693 | Growth Inhibition Assay | IC50=6.62215 μM | SANGER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=6.75044 μM | SANGER | |||
| D-423MG | Growth Inhibition Assay | IC50=6.76117 μM | SANGER | |||
| KNS-42 | Growth Inhibition Assay | IC50=6.78197 μM | SANGER | |||
| GCT | Growth Inhibition Assay | IC50=6.938 μM | SANGER | |||
| DSH1 | Growth Inhibition Assay | IC50=7.0633 μM | SANGER | |||
| D-247MG | Growth Inhibition Assay | IC50=7.07881 μM | SANGER | |||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=7.18371 μM | SANGER | |||
| TE-6 | Growth Inhibition Assay | IC50=7.20601 μM | SANGER | |||
| NOMO-1 | Growth Inhibition Assay | IC50=7.22127 μM | SANGER | |||
| NB17 | Growth Inhibition Assay | IC50=7.30309 μM | SANGER | |||
| EW-22 | Growth Inhibition Assay | IC50=7.34348 μM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=7.35162 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=7.4402 μM | SANGER | |||
| TGBC1TKB | Growth Inhibition Assay | IC50=7.49899 μM | SANGER | |||
| GR-ST | Growth Inhibition Assay | IC50=7.52594 μM | SANGER | |||
| KYSE-520 | Growth Inhibition Assay | IC50=7.55515 μM | SANGER | |||
| CAPAN-1 | Growth Inhibition Assay | IC50=7.5951 μM | SANGER | |||
| HCE-4 | Growth Inhibition Assay | IC50=7.62279 μM | SANGER | |||
| MLMA | Growth Inhibition Assay | IC50=7.62957 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=7.65368 μM | SANGER | |||
| KYSE-180 | Growth Inhibition Assay | IC50=7.71169 μM | SANGER | |||
| TE-5 | Growth Inhibition Assay | IC50=7.95971 μM | SANGER | |||
| IGROV-1 | Growth Inhibition Assay | IC50=7.98551 μM | SANGER | |||
| NCI-H1581 | Growth Inhibition Assay | IC50=8.012 μM | SANGER | |||
| SW1990 | Growth Inhibition Assay | IC50=8.04659 μM | SANGER | |||
| EFM-19 | Growth Inhibition Assay | IC50=8.08545 μM | SANGER | |||
| OGR-1 | Growth Inhibition Assay | IC50=8.43023 μM | SANGER | |||
| U-118-MG | Growth Inhibition Assay | IC50=8.43463 μM | SANGER | |||
| SK-OV-3 | Growth Inhibition Assay | IC50=8.46765 μM | SANGER | |||
| KNS-62 | Growth Inhibition Assay | IC50=8.51761 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=8.57635 μM | SANGER | |||
| 8305C | Growth Inhibition Assay | IC50=8.70484 μM | SANGER | |||
| RPMI-2650 | Growth Inhibition Assay | IC50=8.71955 μM | SANGER | |||
| NEC8 | Growth Inhibition Assay | IC50=8.74307 μM | SANGER | |||
| KYSE-450 | Growth Inhibition Assay | IC50=8.86548 μM | SANGER | |||
| RMG-I | Growth Inhibition Assay | IC50=9.14058 μM | SANGER | |||
| CAKI-1 | Growth Inhibition Assay | IC50=9.31979 μM | SANGER | |||
| KYSE-510 | Growth Inhibition Assay | IC50=9.35778 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=9.36701 μM | SANGER | |||
| AN3-CA | Growth Inhibition Assay | IC50=9.45444 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=9.72849 μM | SANGER | |||
| HSC-2 | Growth Inhibition Assay | IC50=9.76629 μM | SANGER | |||
| EW-1 | Growth Inhibition Assay | IC50=9.79369 μM | SANGER | |||
| D-566MG | Growth Inhibition Assay | IC50=9.83664 μM | SANGER | |||
| COLO-792 | Growth Inhibition Assay | IC50=9.98746 μM | SANGER | |||
| TE-10 | Growth Inhibition Assay | IC50=10.0396 μM | SANGER | |||
| NCI-H650 | Growth Inhibition Assay | IC50=10.4286 μM | SANGER | |||
| U-266 | Growth Inhibition Assay | IC50=10.455 μM | SANGER | |||
| Detroit562 | Growth Inhibition Assay | IC50=11.0515 μM | SANGER | |||
| NH-12 | Growth Inhibition Assay | IC50=11.1446 μM | SANGER | |||
| CO-314 | Growth Inhibition Assay | IC50=11.2842 μM | SANGER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=11.5323 μM | SANGER | |||
| KNS-81-FD | Growth Inhibition Assay | IC50=11.5527 μM | SANGER | |||
| SW1463 | Growth Inhibition Assay | IC50=11.5989 μM | SANGER | |||
| NCI-H23 | Growth Inhibition Assay | IC50=11.6552 μM | SANGER | |||
| SK-MEL-2 | Growth Inhibition Assay | IC50=11.7197 μM | SANGER | |||
| NB13 | Growth Inhibition Assay | IC50=12.1495 μM | SANGER | |||
| Daoy | Growth Inhibition Assay | IC50=12.2856 μM | SANGER | |||
| NCI-H1623 | Growth Inhibition Assay | IC50=12.3801 μM | SANGER | |||
| NMC-G1 | Growth Inhibition Assay | IC50=12.717 μM | SANGER | |||
| DK-MG | Growth Inhibition Assay | IC50=12.9482 μM | SANGER | |||
| TCCSUP | Growth Inhibition Assay | IC50=13.1284 μM | SANGER | |||
| SCC-15 | Growth Inhibition Assay | IC50=13.2651 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=13.2893 μM | SANGER | |||
| RH-1 | Growth Inhibition Assay | IC50=13.3037 μM | SANGER | |||
| SK-MEL-3 | Growth Inhibition Assay | IC50=13.3728 μM | SANGER | |||
| NB5 | Growth Inhibition Assay | IC50=13.4067 μM | SANGER | |||
| SNU-387 | Growth Inhibition Assay | IC50=13.5072 μM | SANGER | |||
| CAL-120 | Growth Inhibition Assay | IC50=13.6718 μM | SANGER | |||
| Mo-T | Growth Inhibition Assay | IC50=13.707 μM | SANGER | |||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=13.7992 μM | SANGER | |||
| CAN | Growth Inhibition Assay | IC50=14.0288 μM | SANGER | |||
| SK-MEL-30 | Growth Inhibition Assay | IC50=14.063 μM | SANGER | |||
| COLO-678 | Growth Inhibition Assay | IC50=14.0822 μM | SANGER | |||
| SCC-9 | Growth Inhibition Assay | IC50=14.1021 μM | SANGER | |||
| KINGS-1 | Growth Inhibition Assay | IC50=14.1402 μM | SANGER | |||
| SL-513 | Growth Inhibition Assay | IC50=14.187 μM | SANGER | |||
| HLE | Growth Inhibition Assay | IC50=14.3852 μM | SANGER | |||
| SW1573 | Growth Inhibition Assay | IC50=14.4435 μM | SANGER | |||
| KYSE-140 | Growth Inhibition Assay | IC50=14.6327 μM | SANGER | |||
| SK-PN-DW | Growth Inhibition Assay | IC50=14.8001 μM | SANGER | |||
| A253 | Growth Inhibition Assay | IC50=15.0625 μM | SANGER | |||
| CAL-12T | Growth Inhibition Assay | IC50=15.4662 μM | SANGER | |||
| COLO-679 | Growth Inhibition Assay | IC50=15.7683 μM | SANGER | |||
| UACC-257 | Growth Inhibition Assay | IC50=16.1201 μM | SANGER | |||
| U-87-MG | Growth Inhibition Assay | IC50=16.3523 μM | SANGER | |||
| HCC1806 | Growth Inhibition Assay | IC50=16.7071 μM | SANGER | |||
| NCI-H2170 | Growth Inhibition Assay | IC50=17.2448 μM | SANGER | |||
| AGS | Growth Inhibition Assay | IC50=17.3808 μM | SANGER | |||
| MEL-HO | Growth Inhibition Assay | IC50=17.7503 μM | SANGER | |||
| SW48 | Growth Inhibition Assay | IC50=17.7716 μM | SANGER | |||
| HuP-T4 | Growth Inhibition Assay | IC50=18.0206 μM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=18.1402 μM | SANGER | |||
| RCC10RGB | Growth Inhibition Assay | IC50=18.1697 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=18.2254 μM | SANGER | |||
| A427 | Growth Inhibition Assay | IC50=18.5094 μM | SANGER | |||
| HCC2998 | Growth Inhibition Assay | IC50=18.6051 μM | SANGER | |||
| EPLC-272H | Growth Inhibition Assay | IC50=19.0434 μM | SANGER | |||
| C32 | Growth Inhibition Assay | IC50=19.045 μM | SANGER | |||
| UMC-11 | Growth Inhibition Assay | IC50=19.2123 μM | SANGER | |||
| CaR-1 | Growth Inhibition Assay | IC50=19.6804 μM | SANGER | |||
| KYSE-410 | Growth Inhibition Assay | IC50=19.9139 μM | SANGER | |||
| HuCCT1 | Growth Inhibition Assay | IC50=20.6294 μM | SANGER | |||
| LB996-RCC | Growth Inhibition Assay | IC50=20.7168 μM | SANGER | |||
| KYSE-70 | Growth Inhibition Assay | IC50=20.8059 μM | SANGER | |||
| CAL-72 | Growth Inhibition Assay | IC50=20.915 μM | SANGER | |||
| Capan-2 | Growth Inhibition Assay | IC50=21.0413 μM | SANGER | |||
| PANC-08-13 | Growth Inhibition Assay | IC50=21.2515 μM | SANGER | |||
| SBC-1 | Growth Inhibition Assay | IC50=21.3081 μM | SANGER | |||
| MFM-223 | Growth Inhibition Assay | IC50=21.3342 μM | SANGER | |||
| BB49-HNC | Growth Inhibition Assay | IC50=21.5716 μM | SANGER | |||
| SH-4 | Growth Inhibition Assay | IC50=21.6618 μM | SANGER | |||
| HuO9 | Growth Inhibition Assay | IC50=21.9825 μM | SANGER | |||
| AM-38 | Growth Inhibition Assay | IC50=22.0485 μM | SANGER | |||
| A431 | Growth Inhibition Assay | IC50=23.2119 μM | SANGER | |||
| YAPC | Growth Inhibition Assay | IC50=23.2651 μM | SANGER | |||
| LU-139 | Growth Inhibition Assay | IC50=23.4809 μM | SANGER | |||
| HEC-1 | Growth Inhibition Assay | IC50=23.4937 μM | SANGER | |||
| SCC-25 | Growth Inhibition Assay | IC50=24.3006 μM | SANGER | |||
| HT-29 | Growth Inhibition Assay | IC50=24.3823 μM | SANGER | |||
| PC-14 | Growth Inhibition Assay | IC50=24.6571 μM | SANGER | |||
| Calu-6 | Growth Inhibition Assay | IC50=25.5071 μM | SANGER | |||
| SJRH30 | Growth Inhibition Assay | IC50=25.6496 μM | SANGER | |||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=26.1629 μM | SANGER | |||
| IA-LM | Growth Inhibition Assay | IC50=26.3645 μM | SANGER | |||
| GP5d | Growth Inhibition Assay | IC50=26.4491 μM | SANGER | |||
| NCI-H2291 | Growth Inhibition Assay | IC50=26.6541 μM | SANGER | |||
| BALL-1 | Growth Inhibition Assay | IC50=26.9397 μM | SANGER | |||
| HCC1954 | Growth Inhibition Assay | IC50=26.9808 μM | SANGER | |||
| NCI-H2452 | Growth Inhibition Assay | IC50=27.4163 μM | SANGER | |||
| LU-99A | Growth Inhibition Assay | IC50=27.5582 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=27.7299 μM | SANGER | |||
| PANC-10-05 | Growth Inhibition Assay | IC50=27.7775 μM | SANGER | |||
| NCI-H2405 | Growth Inhibition Assay | IC50=27.9387 μM | SANGER | |||
| MDA-MB-415 | Growth Inhibition Assay | IC50=28.4137 μM | SANGER | |||
| NCI-H2342 | Growth Inhibition Assay | IC50=28.5281 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=28.7117 μM | SANGER | |||
| LU-134-A | Growth Inhibition Assay | IC50=28.9261 μM | SANGER | |||
| SCC-4 | Growth Inhibition Assay | IC50=31.0494 μM | SANGER | |||
| Saos-2 | Growth Inhibition Assay | IC50=31.9306 μM | SANGER | |||
| RERF-LC-MS | Growth Inhibition Assay | IC50=32.8231 μM | SANGER | |||
| M14 | Growth Inhibition Assay | IC50=32.9764 μM | SANGER | |||
| HPAF-II | Growth Inhibition Assay | IC50=33.5011 μM | SANGER | |||
| NCI-H1755 | Growth Inhibition Assay | IC50=34.3305 μM | SANGER | |||
| D-392MG | Growth Inhibition Assay | IC50=35.8674 μM | SANGER | |||
| A704 | Growth Inhibition Assay | IC50=36.0427 μM | SANGER | |||
| CP50-MEL-B | Growth Inhibition Assay | IC50=36.1911 μM | SANGER | |||
| EW-18 | Growth Inhibition Assay | IC50=36.452 μM | SANGER | |||
| WM-115 | Growth Inhibition Assay | IC50=36.8099 μM | SANGER | |||
| LU-65 | Growth Inhibition Assay | IC50=37.1417 μM | SANGER | |||
| NCI-H1563 | Growth Inhibition Assay | IC50=37.2484 μM | SANGER | |||
| DBTRG-05MG | Growth Inhibition Assay | IC50=38.0691 μM | SANGER | |||
| NCI-H630 | Growth Inhibition Assay | IC50=38.4714 μM | SANGER | |||
| NCI-H1155 | Growth Inhibition Assay | IC50=39.242 μM | SANGER | |||
| OVACR-3 | Growth Inhibition Assay | IC50=39.9195 μM | SANGER | |||
| OAW-42 | Growth Inhibition Assay | IC50=40.4258 μM | SANGER | |||
| JVM-2 | Growth Inhibition Assay | IC50=41.2415 μM | SANGER | |||
| C3A | Growth Inhibition Assay | IC50=41.3447 μM | SANGER | |||
| HT55 | Growth Inhibition Assay | IC50=42.2841 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=42.2974 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=42.4616 μM | SANGER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=43.9892 μM | SANGER | |||
| JEG-3 | Growth Inhibition Assay | IC50=44.947 μM | SANGER | |||
| BPH-1 | Growth Inhibition Assay | IC50=46.3998 μM | SANGER | |||
| MPP-89 | Growth Inhibition Assay | IC50=47.2898 μM | SANGER | |||
| ALL-PO | Growth Inhibition Assay | IC50=47.4188 μM | SANGER | |||
| HT | Growth Inhibition Assay | IC50=47.492 μM | SANGER | |||
| NCI-H2347 | Growth Inhibition Assay | IC50=48.0715 μM | SANGER | |||
| A2780 | Growth Inhibition Assay | IC50=49.4228 μM | SANGER | |||
| KARPAS-299 | Growth Inhibition Assay | IC50=49.5119 μM | SANGER | |||
| NCI-H1651 | Growth Inhibition Assay | IC50=49.8821 μM | SANGER | |||
| Cliquez pour voir plus de données expérimentales sur les lignées cellulaires | ||||||
Informations chimiques, stockage et stabilité
| Poids moléculaire | 483.99 | Formule | C24H29N7O2.HCl |
Stockage (À partir de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 827022-32-2 | Télécharger le SDF | Stockage des solutions mères |
|
|
| Synonymes | N/A | Smiles | CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl | ||
Solubilité
|
In vitro |
Water : 50 mg/mL
DMSO
: 13 mg/mL
(26.86 mM)
Ethanol : Insoluble |
Calculateur de molarité
Calculateur de dilution
Calculateur de poids moléculaire
|
In vivo |
|||||
Calculateur de formulation in vivo (Solution claire)
Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
mg/kg
g
μL
Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.
Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.
Mécanisme daction
| Fonctionnalités |
Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).
|
|---|---|
| Targets/IC50/Ki |
CDK4/CyclinD3
(Cell-free assay) 9 nM
CDK4/CyclinD1
(Cell-free assay) 11 nM
CDK6/CyclinD2
(Cell-free assay) 15 nM
|
| In vitro |
Le PD 0332991 a peu d'effet sur d'autres protéines kinases, y compris EGFR, FGFR, PGFR, IR. Le PD 0332991 est un inhibiteur non compétitif de l'ATP de Cdk4. Le PD 0332991 inhibe les cellules de carcinome mammaire MDA-MB-435 avec un IC50 de 66 nM, ce qui est dû à une phosphorylation réduite de Rb au niveau de la Ser780. Le PD 0332991 inhibe l'incorporation de thymidine dans l'ADN des carcinomes mammaires, coliques et pulmonaires humains Rb-positifs ainsi que des leucémies humaines, avec des valeurs d'IC50 allant de 0,04 à 0,17 μM. Le PD 0332991 ne montre aucune activité dans les cellules Rb-négatives. Le PD 0332991 provoque une accumulation de cellules en G1 dans les cellules mammaires MDA-MB-453 et les cellules de carcinome Colo-205. Le PD 0332991 montre également une activité dans les cellules de myélome 5T33MM (modèle immunocompétent) et sensibilise les cellules à la mort par le bortézomib. Le PD 0332991 inhibe les lignées cellulaires de cancer du sein luminales ER-positives ainsi que HER2-amplifiées, y compris MDA-MB-175, ZR-75-30, CAMA-1, MDA-MB-134, HCC-202 et UACC-893. Le PD 0332991 améliore l'activité du tamoxifène et du trastuzumab dans ces lignées cellulaires. Le PD 0332991 améliore la sensibilité du tamoxifène dans les cellules MCF7 résistantes au tamoxifène. Une étude récente montre que le PD 0332991 pourrait supprimer les lignées cellulaires de tumeurs rhabdoïdes malignes (MRT), y compris MP-MRT-AN, KP-MRT-RY, G401, KP-MRT-NS et que la sensibilité des lignées cellulaires MRT au PD 0332991 est inversement corrélée à l'expression de p16.
|
| Kinase Assay |
Essais Cdk
|
|
Une solution mère de PD0332991 est préparée dans du DMSO. Les essais CDK sont réalisés dans des plaques filtrantes à 96 puits. Tous les complexes kinase CDK-cycline sont exprimés dans des cellules d'insectes par infection par baculovirus et purifiés. Le substrat des essais est un fragment (acides aminés 792–928) de pRb fusionné à la GST (GST·RB-Cterm). Le volume total dans chaque puits est de 0,1 mL contenant une concentration finale de 20 mM Tris-HCl, pH 7,4, 50 mM NaCl, 1 mM dithiothréitol, 10 mM MgCl2, 25 μM ATP (pour CDK4-cycline D1, CDK6-cycline D2 et CDK6-cycline D3) ou 12 μM ATP (pour CDK2-cycline E, CDK2-cycline A et CDC2-cycline B) contenant 0,25 μCi de [γ-32P]ATP, 20 ng d'enzyme, 1 μg de GST·RB-Cterm et de PD 0332991 (0,001-0,1 μM). Tous les composants, à l'exception du [γ-32P]ATP, sont ajoutés aux puits, et la plaque est placée sur un mélangeur de plaques pendant 2 min. La réaction est initiée par l'ajout du [γ-32P]ATP et la plaque est incubée à 25 °C pendant 15 min. La réaction est terminée par l'ajout de 0,1 mL d'acide trichloroacétique à 20 % et la plaque est maintenue à 4 °C pendant au moins 1 heure pour permettre la précipitation du substrat. Les puits sont ensuite lavés 5 fois avec 0,2 mL d'acide trichloroacétique à 10 % et l'incorporation radioactive est déterminée avec un compteur de plaques β.
|
|
| In vivo |
Le PD 0332991 indique une stase tumorale complète dans une xénogreffe MDA-MB-435 à 150 mg/kg. Le PD 0332991 montre également une activité antitumorale à large spectre dans plusieurs xénogreffes de tumeurs humaines en éliminant la phospho-Rb et le marqueur prolifératif Ki-67 du tissu tumoral et en régulant à la baisse les gènes sous le contrôle transcriptionnel d'E2F.
|
Références |
|
Applications
| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Western blot | RB1 (pT821) / RB1 (pS780) / RB1 / CDK6 / CCND2 / RUNX1 / ETO pRb(S807, 811) / CDK4 / CDK6 / PARP LC3-I / LC3-II pAMPKα(T172) / pULK1(S317) SMAD2 (pS255) |
|
30300583 |
| Growth inhibition assay | Cell viability |
|
29670090 |
| Immunofluorescence | SAHF/ATRX LC3B |
|
26988987 |
| ELISA | PGE2 |
|
26540629 |
Informations sur lessai clinique
(données de https://clinicaltrials.gov, mis à jour le 2024-05-22)
| Numéro NCT | Recrutement | Conditions | Sponsor/Collaborateurs | Date de début | Phases |
|---|---|---|---|---|---|
| NCT05665361 | Recruiting | Advanced Clear Cell Renal Carcinoma (Ccrcc)|Papillary Renal Cell Carcinoma (Prcc) |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
April 24 2024 | Phase 1|Phase 2 |
| NCT06307457 | Completed | Breast Cancer |
Pfizer |
March 11 2024 | -- |
| NCT05912933 | Not yet recruiting | Breast Cancer |
Pfizer |
March 1 2024 | -- |
| NCT05709158 | Not yet recruiting | Breast Cancer |
Pfizer |
March 1 2024 | -- |
Support technique
Tel: +1-832-582-8158 Ext:3
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