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Belinostat (PXD101) HDAC Remmer

Name: Belinostat (PXD101)
Brand: Selleck Chemicals
SKU: S1085
Rating: 5 (106 reviews)

Cat.Nr.: S1085

Belinostat is een nieuwe HDAC-remmer met een IC50 van 27 nM in een celvrije test, met activiteit aangetoond in cisplatin-resistente tumoren. Belinostat (PXD101) induceert autophagy.

Belinostat (PXD101) HDAC Remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 318.35

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.74%

99.74

Gerelateerde doelwitten	JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Sirtuin
Overige HDAC Inhibitoren	ITF-2357 (Givinostat) Hydrochloride Monohydrate Fimepinostat (CUDC-907) Trichostatin A (TSA) Entinostat (MS-275) RGFP966 Quisinostat (JNJ-26481585) Dihydrochloride Tubastatin A Hydrochloride Tubastatin A Mocetinostat (MGCD0103) Ricolinostat (ACY-1215)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	PMID
HCT116	Function Assay	0.9 μM	24 h		down-regulats TS protein levels after 6 h incubation	17124594
HCT116	Growth Inhibition Assay		48 h		EC50=0.28 μM	17124594
Granta-519	Growth Inhibition Assay		24 h		IC50=56.3 μM	20068080
Jeko-1	Growth Inhibition Assay		24 h		IC50=0.2 μM	20068080
HBL-2	Growth Inhibition Assay		24 h		IC50=0.4 μM	20068080
Panc-1	Apoptosis Assay	100/500/1000 nM	48 h		induces dose dependent apoptosis	22681698
AsPC-1	Apoptosis Assay	100/500/1000 nM	48 h		induces dose dependent apoptosis	22681698
T3M4	Apoptosis Assay	100/500/1000 nM	48 h		induces dose dependent apoptosis	22681698
Panc-1	Growth Inhibition Assay	0-800 nM	48 h		inhibits cell proliferation in a dose dependent manner	22681698
AsPC-1	Growth Inhibition Assay	0-800 nM	48 h		inhibits cell proliferation in a dose dependent manner	22681698
T3M4	Growth Inhibition Assay	0-800 nM	48 h		inhibits cell proliferation in a dose dependent manner	22681698
MiaPaCa2	Function Assay	1/10 μM	24 h		induces growth arrested in G2/M	23475695
AsPc1	Function Assay	1/10 μM	24 h		induces growth arrested in G2/M	23475695
Panc0403	Apoptosis Assay	1 μM	24 h		induces apoptosis	23475695
Panc1005	Apoptosis Assay	1 μM	24 h		induces apoptosis	23475695
Panc0327	Apoptosis Assay	1 μM	24 h		induces apoptosis	23475695
Panc0203	Growth Inhibition Assay		48 h		EC50=22.2 μM	23475695
PL45	Growth Inhibition Assay		48 h		EC50=20.8 μM	23475695
Panc1005	Growth Inhibition Assay		48 h		EC50=1.1 μM	23475695
Panc0403	Growth Inhibition Assay		48 h		EC50=1.1 μM	23475695
BxPc3	Growth Inhibition Assay		48 h		EC50=1.0 μM	23475695
MiaPaCa2	Growth Inhibition Assay		48 h		EC50=0.7 μM	23475695
Panc0327	Growth Inhibition Assay		48 h		EC50=0.5 μM	23475695
AsPc1	Growth Inhibition Assay		48 h		EC50=0.3 μM	23475695
PC9	Function Assay	0.5/1/2 μM	4 h	DMSO	inhibits the levels of Akt (p-Akt) and EGFR	23515752
H1650	Function Assay	0.5/1/2 μM	4 h	DMSO	inhibits the levels of Akt (p-Akt) and EGFR	23515752
H460	Function Assay	0.5/1/2 μM	4 h	DMSO	inhibits the levels of Akt (p-Akt) and EGFR	23515752
PC9	Function Assay	500 nM	24 h	DMSO	decreases EGFR expression	23515752
H1650	Function Assay	500 nM	24 h	DMSO	decreases EGFR expression	23515752
H460	Function Assay	500 nM	24 h	DMSO	decreases EGFR expression	23515752
HCC4006	Growth Inhibition Assay		72 h	DMSO	IC50=0.46 μM	23515752
HCC2935	Growth Inhibition Assay		72 h	DMSO	IC50=0.97 μM	23515752
HCC827	Growth Inhibition Assay		72 h	DMSO	IC50=0.29 μM	23515752
HCC2279	Growth Inhibition Assay		72 h	DMSO	IC50=0.4 μM	23515752
PC9	Growth Inhibition Assay		72 h	DMSO	IC50=0.29 μM	23515752
H820	Growth Inhibition Assay		72 h	DMSO	IC50=0.4 μM	23515752
H1650	Growth Inhibition Assay		72 h	DMSO	IC50=0.88 μM	23515752
H1975	Growth Inhibition Assay		72 h	DMSO	IC50=0.68 μM	23515752
H520	Growth Inhibition Assay		72 h	DMSO	IC50=0.75 μM	23515752
H1299	Growth Inhibition Assay		72 h	DMSO	IC50=1.2 μM	23515752
H460	Growth Inhibition Assay		72 h	DMSO	IC50=0.86 μM	23515752
H1666	Growth Inhibition Assay		72 h	DMSO	IC50>10 μM	23515752
PANC-1	Function Assay	10 μM	2/4 h	DMSO	increases intracellular ROS level	23743198
PANC-1	Cell Viability Assay	1/10 μM	48 h	DMSO	decreases cell viability in a dose dependent manner	23743198
PANC-1	Function Assay	10 μM	2/4/6 h	DMSO	induces AMPK activation	23743198
HL-60	Function Assay	0.2 μM	24/48/72 h		enhances RA-induced granulocytic differentiation	25864732
NB4	Function Assay	0.2 μM	24/48/72 h		enhances RA-induced granulocytic differentiation	25864732
HL-60	Function Assay	2 μM	24/48 h		blocks cell cycle in S phase	25864732
NB4	Function Assay	2 μM	24/48 h		blocks cell cycle in S phase	25864732
HL-60	Cell Viability Assay	0.2/2 μM	24/48/72 h		decreases cell viability in both time and dose dependent manner	25864732
NB4	Cell Viability Assay	0.2/2 μM	24/48/72 h		decreases cell viability in both time and dose dependent manner	25864732
RAW264.7	Anti-inflammatory assay		1 hr		Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of IL6 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method, IC50 = 0.000059 μM.	25113875
HEK293	Function assay				Inhibition of HDAC6 in HEK293 cells, IC50 = 0.015 μM.	18308563
HEK293	Function assay				Inhibition of HDAC1 in HEK293 cells, IC50 = 0.018 μM.	18308563
HeLa	Function assay		30 mins		Inhibition of HDAC in human HeLa cells nuclear extracts incubated for 30 mins by fluorescent assay, IC50 = 0.0264 μM.	25113875
HeLa	Function assay				Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay, IC50 = 0.027 μM.	23639537
HeLa	Function assay				Inhibition of HDAC from human HeLa cells, IC50 = 0.028 μM.	18247554
HEK293	Function assay				Inhibition of HDAC3 in HEK293 cells, IC50 = 0.046 μM.	18308563
MDA-MB-231	Antiproliferative assay		72 hrs		Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by resazurin dye based fluorescence assay, IC50 = 0.062 μM.	29456804
Jurkat	Antiproliferative assay		48 hrs		Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay, IC50 = 0.07 μM.	29533873
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells after 72 hrs by resazurin dye based fluorescence assay, IC50 = 0.077 μM.	29456804
HeLa	Antiproliferative assay		72 hrs		Antiproliferative activity against human HeLa cells after 72 hrs by resazurin dye based fluorescence assay, IC50 = 0.087 μM.	29456804
MCF7	Antiproliferative assay		72 hrs		Antiproliferative activity against human MCF7 cells after 72 hrs by resazurin dye based fluorescence assay, IC50 = 0.096 μM.	29456804
HEL	Antiproliferative assay		48 hrs		Antiproliferative activity against human HEL cells after 48 hrs by MTT assay, IC50 = 0.1 μM.	29533873
Huh7	Antiviral assay		3 days		Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay, EC50 = 0.12 μM.	25490700
HCT116	Antiproliferative assay		48 hrs		Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay, GI50 = 0.13 μM.	27344487
MOLT4	Antiproliferative assay		48 hrs		Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay, IC50 = 0.14 μM.	29533873
HCT116	Antiproliferative assay				Antiproliferative activity against human HCT116 cells assessed as growth inhibition, IC50 = 0.16 μM.	21650221
HCT116	Antiproliferative assay				Antiproliferative activity against human HCT116 cells, IC50 = 0.16 μM.	21742496
SK-N-BE(2)	Antiproliferative assay		48 hrs		Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay, IC50 = 0.31 μM.	29533873
PC3	Antiproliferative assay		48 hrs		Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay, GI50 = 0.39 μM.	27344487
PC3	Antiproliferative assay		96 hrs		Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay, IC50 = 0.45 μM.	21634430
H1299	Antiproliferative assay				Antiproliferative activity against human H1299 cells, IC50 = 0.46 μM.	21650221
HeLa	Antiproliferative assay		48 hrs		Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.51 μM.	29533873
HCT116	Antiproliferative assay		96 hrs		Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay, IC50 = 0.6 μM.	21634430
A2780	Antiproliferative assay		96 hrs		Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay, IC50 = 0.67 μM.	21634430
HuH7	Cytotoxicity assay		3 days		Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay, CC50 = 0.68 μM.	25490700
COLO205	Antiproliferative assay		96 hrs		Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay, IC50 = 0.7 μM.	21634430
A549	Antiproliferative assay		48 hrs		Antiproliferative activity against human A549 cells after 48 hrs by SRB assay, GI50 = 0.78 μM.	27344487
HL60	Antiproliferative assay		48 hrs		Antiproliferative activity against human HL60 cells after 48 hrs by SRB assay, GI50 = 1.09 μM.	27344487
K562	Antiproliferative assay		48 hrs		Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 1.1 μM.	29533873
PC3	Antiproliferative assay		48 hrs		Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 1.3 μM.	29533873
NFF	Cytotoxicity assay		72 hrs		Cytotoxicity against human NFF cells after 72 hrs by SRB assay, IC50 = 1.4 μM.	28241112
HEK293	Cytotoxicity assay		48 hrs		Cytotoxicity against HEK293 cells after 48 hrs by resazurin assay, IC50 = 1.4 μM.	28241112
NFF	Cytotoxicity assay		72 hrs		Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay, IC50 = 1.42 μM.	30245402
HEK293	Cytotoxicity assay		48 hrs		Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay, IC50 = 1.42 μM.	30245402
RAW264.7	Anti-inflammatory assay		1 hr		Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of nitric oxide production pre-incubated for 1 hr before LPS stimulation for 24 hrs by Griess reagent based assay, IC50 = 2.2 μM.	25113875
RAW264.7	Anti-inflammatory assay		1 hr		Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of TNFalpha production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method, IC50 = 4.7 μM.	25113875
RAW264.7	Anti-inflammatory assay		1 hr		Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of PGE2 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by enzyme immunoassay method, IC50 = 8.28 μM.	25113875
Huh-luc/neo7	Function assay	1 uM	1 to 3 hrs		Inhibition of HDAC class 1 in human Huh-luc/neo7 cells assessed as histone H3 acetylation at 1 uM after 1 to 3 hrs by Western blotting analysis	25937017
PC3	Function assay	0.3 uM	48 hrs		Inhibition of HDAC in human PC3 cells assessed as increase in amount of acetylated histone H3 at 0.3 uM after 48 hrs by Western blot analysis	27344487
HCT116	Function assay	0.3 uM	48 hrs		Inhibition of HDAC in human HCT116 cells assessed as increase in amount of acetylated histone H3 at 0.3 uM after 48 hrs by Western blot analysis	27344487
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht	318.35	Formule	C₁₅H₁₄N₂O₄S	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	866323-14-0	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	PXD101,NSC726630, PX-105684			Smiles	C1=CC=C(C=C1)NS(=O)(=O)C2=CC=CC(=C2)C=CC(=O)NO

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 64 mg/mL (201.03 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	4.000mg/ml (12.56mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.000mg/ml (3.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Kenmerken	Lead compound of Topotarget.
Targets/IC₅₀/Ki	HDAC (Cell-free assay) 27 nM
In vitro	Belinostat inhibits the growth of tumor cells (A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852) with IC50 from 0.2-0.66 μM. PD101 shows low activity in A2780/cp70 and 2780AD cells, which are cisplatin and doxorubicin-resistant derivatives of A2780 cells. This compound could induce apoptosis through PARP cleavage and acetylation of histones H3/H4. It inhibits bladder cancer cell growth, especially in 5637 cells, which shows accumulation of G0-G1 phase, decrease in S phase and increase in G2-M phase. The growth inhibitory activity of this chemical on cell lines is not strongly influenced by the multidrug-resistant phenotype, whereas the activity of docetaxel is clearly affected. It could enhance the growth inhibitory activity of docetaxel or carboplatin in OVCAR-3 and A2780 cells. This compound also shows enhanced tubulin acetylation in ovarian cancer cell lines. A recent study shows that it activates protein kinase A in a TGF-β signaling-dependent mechanism and decreases survivin mRNA.
Kinase Assay	Histonedeacetylase-activiteit
Kinase Assay	Subconfluente culturen worden geoogst en tweemaal gewassen in ijskoud PBS en gepelleteerd door centrifugatie bij 200 × g gedurende 5 min. De celpellet wordt geresuspendeerd in twee volumes lysisbuffer [60 mM Tris-buffer (pH 7,4) met 30% glycerol en 450 mM NaCl] en gelyseerd door drie vries (droogijs) dooi (30 °C waterbad) cycli. Celafval wordt verwijderd door centrifugatie bij 1,2 × 10⁴ g gedurende 5 min, en het supernatant wordt bewaard bij −80 °C. Histon H4-peptide (sequentie SGRGKGGKGLGKGGAKRHRK overeenkomend met de 20 NH2-terminale residuen) wordt geacetyleerd door een recombinant eiwit dat het hypoxanthine-aminopterine-thymidine-domein van p300 bevat, met behulp van [³H]acetyl CoA als bron van acetaat. H4-peptide (100 μg) wordt gemengd met hypoxanthine-aminopterine-thymidine-buffer (50 mM Tris HCl pH 8,0, 5% glycerol, 50 mM KCl en 0,1 mM EDTA), 1 mM DTT, 1 mM 4-(2-aminoethyl) benzeensulfonylfluoride, 1 × complete protease-remmers, 50 μL gezuiverd p300 en 1,85 m [³H]acetyl CoA (4,50Ci/mmol) in een eindvolume van 300 μL en geïncubeerd bij 30 °C gedurende 45 min. Het p300-eiwit wordt verwijderd door incubatie met 20 μL 50% Ni-agaroseparels gedurende 1 uur bij 4 °C en centrifugatie. Het supernatant wordt aangebracht op een 2 mL Sephadex G15-kolom en de doorstroom wordt opgevangen. Een milliliter gedestilleerd H₂O wordt voorzichtig aangebracht en drie druppelfracties worden opgevangen; dit wordt herhaald totdat 4–5 mL gedestilleerd H₂O is toegevoegd, en ~40 fracties worden opgevangen. Drie microliter van elke fractie wordt verdund in 2 mL scintillatievloeistof en geteld in een scintillatieteller om de fracties te identificeren die het gelabelde peptide bevatten. Deze fracties worden gepoold, en 1 μL van het gecombineerde monster wordt gemeten om de radioactiviteit in elke peptidebatch (3-7×10³ cpm/μL) te beoordelen. Voor activiteitsassays wordt de reactie uitgevoerd in een totaal volume van 150 μL buffer [60 mM Tris (pH 7,4) met 30% glycerol] met 2 μL celextract en, indien gebruikt, 2 μL van deze verbinding. De reactie wordt gestart door de toevoeging van 2 μL [³H]-gelabeld substraat (geacetyleerd histon H4-peptide overeenkomend met de 20 NH₂-terminale residuen). Monsters worden geïncubeerd bij 37 °C gedurende 45 min, en de reactie wordt gestopt door de toevoeging van HCl en azijnzuur (respectievelijk 0,72 en 0,12 M eindconcentraties). Vrijgekomen [³H]acetaat wordt geëxtraheerd in 750 μL ethylacetaat, en monsters worden gecentrifugeerd bij 1,2× 10⁴ g gedurende 5 min. De bovenste fase (600 μL) wordt overgebracht naar 3 mL scintillatievloeistof en geteld.
In vivo	Belinostat indicates significant tumor growth delay in A2780 and A2780/cp70 xenograft at a dose of 10mg/kg with no effects on the body weight. This compound also induces p21WAF1, HDAC core and cell communication genes in mouse bladder tumors. Its monotherapy induces dose-proportional antitumor effects with TGI of 47% at a dose of 100mg/kg in A2780 xenograft. The combination of this chemical (100 mg/kg) with carboplatin (40 mg/kg) could delay tumor growth from 18.6 days to 22.5 days. Combining with bortezomib, it results in great tumor inhibition and gastrointestinal toxicity in mice with bortezomib-resistant UMSCC-11A xenograft.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/12939461/ [2] https://pubmed.ncbi.nlm.nih.gov/17935615/ [3] https://pubmed.ncbi.nlm.nih.gov/16928830/ [4] https://pubmed.ncbi.nlm.nih.gov/21757750/ [5] https://pubmed.ncbi.nlm.nih.gov/17237265/

Toepassingen (Applications)

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	p-H2AX(Ser139) / KU70 / KU80 / RAD51 / RAD52 / ERCC1 Acetyl Histone H3 / Acetyl Histone H4 / Acetyl tubulin p21 / p27 SOS1 / SOS2 PARP / p-ERK / p-p38 / p38 / p-BRAF / p-MEK / MEK		24155971
Growth inhibition assay	Cell viability IC50		24155971

Informatie klinische proef (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT06406465	Not yet recruiting	Carcinoma Neuroendocrine\|Tumor Neuroendocrine\|Tumors Neuroendocrine\|Neuroendocrine; Carcinoma\|Small Cell; Receptors	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	May 15 2024	Phase 2
NCT04315233	Recruiting	Metastatic Breast Cancer\|Recurrent Ovarian Carcinoma	University of Utah\|Novartis\|Acrotech Biopharma	May 3 2021	Phase 1
NCT04703920	Recruiting	Metastatic Breast Cancer\|Metastatic Castration-resistant Prostate Cancer\|Metastatic Ovarian Carcinoma	University of Michigan Rogel Cancer Center\|Pfizer\|Acrotech Biopharma Inc.	March 4 2021	Phase 1
NCT03772925	Active not recruiting	Recurrent Acute Myeloid Leukemia\|Recurrent Myelodysplastic Syndrome\|Refractory Acute Myeloid Leukemia\|Refractory Myelodysplastic Syndrome	National Cancer Institute (NCI)	June 20 2019	Phase 1

Veelgestelde vragen (Frequently Asked Questions)

Vraag 1:
Could you please give some suggestions for the use of it in vivo (i.p. injection)?

Antwoord:
For I.P. injection, it can be dissolved in 2% DMSO+30% PEG 300+ddH2O at 10 mg/ml clearly. When preparing the solution, please dissolve this compound in DMSO clearly first. Then add PEG, after they mixed well, then dilute with water. Hope this information is useful to you.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):