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Topotecan HCl Topoisomerase Remmer

Name: Topotecan HCl
Brand: Selleck Chemicals
SKU: S1231
Rating: 5 (58 reviews)

Cat.Nr.: S1231

Topotecan HCl is een topoisomerase I-remmer voor MCF-7 Luc-cellen en DU-145 Luc-cellen met een IC50 van respectievelijk 13 nM en 2 nM in celvrije assays. Deze verbinding induceert autophagy en apoptosis.

Topotecan HCl Topoisomerase Remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 457.91

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.98%

99.98

Gerelateerde doelwitten	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis PPAR Sirtuin Casein Kinase eIF
Overige Topoisomerase Inhibitoren	Camptothecin (CPT) Betulinic acid (S)-10-Hydroxycamptothecin Beta-Lapachone Ellagic acid Amonafide Voreloxin (SNS-595) hydrochloride Hydroxy Camptothecine Cu(II)-Elesclomol 7-Ethylcamptothecin

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

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
human MDA-MB-435 cells	Cytotoxic assay		72 h	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, ic50=1 nM	20371183
human Bel7402 cells	Cytotoxic assay		96 h	Cytotoxicity against human Bel7402 cells after 96 hrs by MTT assay, IC50=1.2 nM	15165144
human HCT8 cells	Cytotoxic assay		96 h	Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay, IC50=1.5 nM	15165144
human MCF7 cells	Cytotoxic assay		96 h	Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay, IC50=1.8 nM	15165144
human A549 cells	Cytotoxic assay		96 h	Cytotoxicity against human A549 cells after 96 hrs by MTT assay, IC50=3.2 nM	15165144
human colon carcinoma SW620 cell	Cytotoxic assay			Cytotoxic potentiation of Topotecan (TP) by the compound in human colon carcinoma SW620 cell line, IC50=3.2 nM	12408707
human MESSA cells	Cytotoxic assay		72 h	Cytotoxicity against human MESSA cells after 72 hrs by alamar blue assay, IC50=4 nM	21341674
human BGC823 cells	Cytotoxic assay		96 h	Cytotoxicity against human BGC823 cells after 96 hrs by MTT assay, IC50=4.3 nM	15165144
human Ketr3 cells	Cytotoxic assay		96 h	Cytotoxicity against human Ketr3 cells after 96 hrs by MTT assay, IC50=4.9 nM	15165144
LOX cells	Cytotoxic assay			Cytotoxicity was determined in vitro in LOX cells (melanoma) of human tumor cell lines by using MTT assay, IC50=5 nM	7853331
human A549 cells	Function assay		4 h	Antitumor activity against human A549 cells after 4 hrs by MTT assay, IC50=5 nM	18207748
human H69 cells	Cytotoxic assay		72 h	Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay, IC50=6 nM	21341674
human A2780 cells	Cytotoxic assay		72 h	Cytotoxicity against human A2780 cells overexpressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay, IC50=6 nM	22959246
human LNCAP cells	Cytotoxic assay		72 h	Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay, IC50=9 nM	21341674
human HOP62 cells	Growth inhibition assay			Growth inhibition of human HOP62 cells by five-dose growth inhibition assay, IC50=10 nM	25909279
human MCF7 cells	Growth inhibition assay			Growth inhibition of human MCF7 cells by five-dose growth inhibition assay, IC50=10 nM	25909279
human UACC62 cells	Growth inhibition assay			Growth inhibition of human UACC62 cells by five-dose growth inhibition assay, IC50=10 nM	25909279
human DU145 cells	Growth inhibition assay			Growth inhibition of human DU145 cells by five-dose growth inhibition assay, IC50=10 nM	25909279
LoVo cell line	Cytotoxic assay			Cytotoxic potentiation of Topotecan (TP) by the compound in (human colorectal cancer LoVo cell line, IC50=11.6 nM	12408707
human lymphoblast tumor cell line RPM18402	Cytotoxic assay			Cytotoxicity against human lymphoblast tumor cell line RPM18402, IC50=12 nM	12392745
human HL60 cells	Function assay			Antitumor activity against human HL60 cells by SRB method, IC50=12 nM	19541483
human A375 cells	Cytotoxic assay		72 h	Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay, IC50=13 nM	21341674
COR-L23/P cell	Cytotoxic assay			Cytotoxicity measured using the COR-L23 parental (COR-L23/P) human non small cell lung carcinoma cell line, IC50=13.2 nM	11806724
human NCI-H460 cells	Proliferation assay		72 h	Antiproliferative activity against human NCI-H460 cells after 72 hrs by coulter counter analysis, IC50=16 nM	21783369
human MOLT4 cells	Cytotoxic assay		72 h	Cytotoxicity against human MOLT4 cells after 72 hrs by MTT assay, IC50=19 nM	24900725
human LoVo cells	Cytotoxic assay		72 h	Cytotoxicity against human LoVo cells after 72 hrs by MTT assay, IC50=20 nM	20371183
RPM18402 tumor cell line	Proliferation assay			Concentration required to inhibit cell proliferation in RPM18402 tumor cell line, IC50=20 nM	15482929
human SN12C cells	Growth inhibition assay			Growth inhibition of human SN12C cells by five-dose growth inhibition assay, GI50=20 nM	25909279
human RPMI8226 cells	Cytotoxic assay			Cytotoxicity against human RPMI8226 cells by MTT method, IC50=21 nM	19012996
HT-29 cells	Cytotoxic assay			Cytotoxicity was determined in vitro in HT-29 cells(colon) of human tumor cell lines by using MTT assay, IC50=25 nM	7853331
SK-BR-3 cells	Cytotoxic assay			In Vitro cytotoxicity against human breast cancer cell line (SK-BR-3), IC50=26 nM	11334569
HeLa cells	Growth inhibition assay			Growth inhibition of HeLa cells after 4 days, GI50=30 nM	17418582
UACC 62 cells	Cytotoxic assay			Tested in vitro for cytotoxicity against human tumor cell line UACC 62 (melanoma), GI50=30 nM	10714502
human HCT116 cells	Growth inhibition assay			Growth inhibition of human HCT116 cells by five-dose growth inhibition assay, GI50=30 nM	25909279
human lung cancer cell line (H128)	Cytotoxic assay			In Vitro cytotoxicity against human lung cancer cell line (H128), IC50=31 nM	11334569
human MES-SA/Dx5 cells	Cytotoxic assay			Cytotoxicity against human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs by alamar blue assay, IC50=33 nM	21341674
human A2780 cells	Cytotoxic assay		72 h	Cytotoxicity against human A2780 cells after 72 hrs by MTT assay, IC50=33 nM	24900725
human MDA-MB-435 cells	Cytotoxic assay		72 h	Cytotoxicity against human MDA-MB-435 cells incubated for 72 hrs by MTT assay, GI50=34 nM	22867019
human stomach cancer cell line (MKN45)	Cytotoxic assay			In Vitro cytotoxicity against human stomach cancer cell line (MKN45), IC50=38 nM	11334569
human KB3-1 cells	Cytotoxic assay			Cytotoxicity against human KB3-1 cells after MTT assay, IC50=40 nM	18829334
mouse P388 cells	Cytotoxic assay			Cytotoxicity against mouse P388 cells after MTT assay, IC50=45 nM	18829334
A427 human lung carcinoma	Proliferation assay			Antiproliferative activity measured against A427 human lung carcinoma, IC50=49 nM	9876111
human U251 cells	Function assay		6-24 h	Inhibition of topoisomerase-1 in human U251 cells assessed as inhibition of hypoxia-induced HIF-1alpha accumulation in nuclear extract after 6 to 24 hrs by immunoblot analysis, EC50=54 nM	22305612
human colon cancer cell line (WiDr)	Cytotoxic assay			In Vitro cytotoxicity against human colon cancer cell line (WiDr), IC50=56 nM	11334569
human HepG2 cells	Cytotoxic assay		4 days	Cytotoxicity against human HepG2 cells after 4 days by MTT assay, IC50=60 nM	18554906
human KB cells	Cytotoxic assay		72 h	Cytotoxicity against human KB cells after 72 hrs sulforhodamine B colorimetric assay, IC50=62.5 nM	25008456
human HCT8 cells	Cytotoxic assay		3 days	Cytotoxicity against human HCT8 cells after 3 days by MTT assay, IC50=70 nM	20392545
human GBM2 cells	Proliferation assay		72 h	Antiproliferative activity against human GBM2 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=0.13 μM	26355532
SK-MEL-2 cells	Cytotoxic assay		72 h	Cytotoxicity against human SK-MEL-2 cells after 72 hrs by alamar blue assay, IC50=0.14 μM	21341674
human IGROV1 cells	Cytotoxic assay		72 h	Cytotoxicity against human IGROV1 cells after 72 hrs by alamar blue assay, IC50=0.16 μM	21341674
human U87 cells	Proliferation assay		48 h	Antiproliferative activity against human U87 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=0.16 μM	24826818
human HT1080 cells	Proliferation assay		48 h	Antiproliferative activity against human HT1080 cells assessed as growth inhibition incubated for 48 hrs by sulforhodamine B assay, IC50=0.18 μM	26408815
human Hep3B cells	Proliferation assay		72 h	Antiproliferative activity against human Hep3B cells after 72 hrs by XTT assay, GI50=0.22 μM	19796956
human GBM3 cells	Proliferation assay		72 h	Antiproliferative activity against human GBM3 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=0.38 μM	26355532
human KBVIN cells	Cytotoxic assay		72 h	Cytotoxicity against human KBVIN cells after 72 hrs by SRB assay, IC50=0.4 μM	25438769
human GBM1 cells	Proliferation assay		72 h	Antiproliferative activity against human GBM1 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=0.46 μM	26355532
human U937 cells	Cytotoxic assay		48 h	Cytotoxicity against human U937 cells expressing p53 mutant after 48 hrs by SRB assay ， IC50=1.1 μM	19715319
Caco2	Cytotoxicity assay		24 hrs	Cytotoxicity against human Caco2 cells after 24 hrs by MTT assay, IC50=0.119μM.	24980118
Jurkat	Cytotoxicity assay		24 hrs	Cytotoxicity against human Jurkat cells after 24 hrs by MTT assay, IC50=0.127μM.	24980118
A375	Cytotoxicity assay		24 hrs	Cytotoxicity against human A375 cells after 24 hrs by MTT assay, IC50=0.162μM.	24980118
HeLa	Cytotoxicity assay		24 hrs	Cytotoxicity against human HeLa cells after 24 hrs by MTT assay, IC50=0.38μM.	24980118
MDA-MB-231	Cytotoxicity assay		24 hrs	Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=0.473μM.	24980118
NCI-H460	Antiproliferative assay		1 hr	Antiproliferative activity against human NCI-H460 cells after short term exposure for 1 hr measured after 72 hrs in drug-free medium, IC50=0.61μM.	19530720
HCT8	Antiproliferative assay		48 hrs	Antiproliferative activity against human HCT8 cells after 48 hrs by CCK8 assay, IC50=1.875μM.	25481395
KB	Antiproliferative assay		48 hrs	Antiproliferative activity against human KB cells after 48 hrs by CCK8 assay, IC50=2.282μM.	25481395
SGC7901	Antiproliferative assay		48 hrs	Antiproliferative activity against human SGC7901 cells after 48 hrs by CCK8 assay, IC50=2.292μM.	25481395
HepG2	Antiproliferative assay		48 hrs	Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay, IC50=4.208μM.	25481395
MDA-MB-231	Apoptosis assay			Induction of apoptosis in human MDA-MB-231 cells assessed as p53 phosphorylation at Ser15 by Western blotting analysis	24980118
HeLa	Apoptosis assay	0.8 to 1.6 uM	24 hrs	Induction of apoptosis in human HeLa cells assessed as inhibition of DNA synthesis at 0.8 to 1.6 uM after 24 hrs by BrdU staining-based ELISA	24980118
MDA-MB-231	Apoptosis assay	0.8 to 1.6 uM	24 hrs	Induction of apoptosis in human MDA-MB-231 cells assessed as inhibition of DNA synthesis at 0.8 to 1.6 uM after 24 hrs by BrdU staining-based ELISA	24980118
A375	Apoptosis assay	0.8 to 1.6 uM	24 hrs	Induction of apoptosis in human A375 cells assessed as inhibition of DNA synthesis at 0.8 to 1.6 uM after 24 hrs by BrdU staining-based ELISA	24980118
Caco2	Apoptosis assay	0.8 to 1.6 uM	24 hrs	Induction of apoptosis in human Caco2 cells assessed as inhibition of DNA synthesis at 0.8 to 1.6 uM after 24 hrs by BrdU staining-based ELISA	24980118
A375	Apoptosis assay			Induction of apoptosis in human A375 cells assessed as p53 phosphorylation at Ser15 by Western blotting analysis	24980118
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells	29435139
Daoy	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells	29435139
Klik om meer experimentele gegevens over de cellijn te bekijken

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

Moleculair gewicht	457.91	Formule	C₂₃H₂₃N₃O₅.HCl	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	119413-54-6	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	Nogitecan HCl, SKFS 104864A, NSC 609699			Smiles	CCC1(C2=C(COC1=O)C(=O)N3CC4=CC5=C(C=CC(=C5CN(C)C)O)N=C4C3=C2)O.Cl

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 91 mg/mL (198.72 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : 91 mg/mL

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.
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	Saline Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	30.000mg/ml (65.52mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

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	Topotecan is a water-soluble derivative of camptothecin.
Targets/IC₅₀/Ki	Topo I (DU-145 Luc cells) (Cell-free assay) 2 nM Topo I (MCF-7 Luc cells) (Cell-free assay) 13 nM
In vitro	Een sterkere medicijnactiviteit van Topotecan HCl wordt waargenomen voor DU-145 Luc- en MCF-7 Luc-cellen. Deze verbinding veroorzaakt cytotoxiciteit tijdens de DNA-replicatie door het covalente complex tussen topoisomerase I en DNA te stabiliseren en de herligatie van enzymgebonden enkelstrengs DNA-breuk te voorkomen. Het stabiliseert topoisomerase I/DNA-splijtbare complexen in stralingsresistente menselijke B-lijn acute lymfoblastische leukemie (ALL) cellen, veroorzaakt snelle apoptotische celdood ondanks een hoge expressie van bcl-2-eiwit, en remt de clonogene groei van ALL-cellen op een dosisafhankelijke manier.
In vivo	Dieren die s.c. zijn geïnoculeerd met DU-145 Luc-cellen en vervolgens zijn behandeld met Topotecan HCl vertonen significante tumorgroei en -regressie, gemeten met schuifmaten en luminescentiebeelden. De correlatiecoëfficiënt is 0,75 voor de onbehandelde controlegroep en 0,93 voor de met deze verbinding behandelde groep. Op vergelijkbare wijze zijn tumorprogressie en -regressie meetbaar met behulp van luminescentiebeelden voor onbehandelde en met deze chemische stof behandelde muizen die i.p. zijn geïnoculeerd met MCF-7 Luc-cellen. Deze verbinding vertoonde een krachtige antileukemische activiteit in SCID-muismodellen (severe combined immune-deficiency) van menselijke ALL met een slechte prognose. Het verbeterde de event-vrije overleving van SCID-muizen, die waren blootgesteld aan anders fatale doses van menselijke leukemiecellen op systemische medicijnexpositieniveaus, aanzienlijk. Gliomen brengen bij voorkeur TRAIL R2 tot expressie en behandeling met deze chemische stof reguleert de expressie ervan significant op.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/12960742/ [2] https://pubmed.ncbi.nlm.nih.gov/7742543/ [3] https://pubmed.ncbi.nlm.nih.gov/15719269/ [4] https://pubmed.ncbi.nlm.nih.gov/22689924/ [5] https://pubmed.ncbi.nlm.nih.gov/9523734/

Toepassingen (Applications)

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	LC3 / p62 p53 / sesn2 / p-AMPK		23024792
Growth inhibition assay	Cell viability		28544814

Informatie klinische proef (Clinical Trial Information)

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

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT04455139	Terminated	Eye Cancer Retinoblastoma	Prof. Beck Popovic Maja\|University of Lausanne Hospitals	November 15 2021	Phase 2
NCT05083000	Unknown status	COVID-19 Respiratory Infection	National University Hospital Singapore\|Christian Medical College Vellore India	August 16 2021	Phase 1
NCT04156347	Active not recruiting	Retinoblastoma	Targeted Therapy Technologies LLC	June 16 2021	Phase 1
NCT04428879	Recruiting	Retinoblastoma	The Hospital for Sick Children	June 16 2020	Phase 1

Veelgestelde vragen (Frequently Asked Questions)

Vraag 1:
I would like to get it for mice intraperitoneally injection. What would you recommend to improve solubility? What could I use as solvent (%v?) that is nontoxic (unlike Methanol) and could be injected into mice intraperitoneally?

Antwoord:
It is generally prepared by Saline for I.P. administration.

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):