RSM-932A

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性胆碱激酶 α (ChoKα) 抑制剂，IC50 为 1.0 uM。

A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 1.0 uM, 33-fold selectivity over ChoKβ; demonstrates potent in vitro antiproliferative (HT29 IC50=1.15 uM) and in vivo antitumoral activity against human xenografts in mice with low toxicity profiles.Solid Tumors Phase 1 Clinical.

Cell Proliferation Assay Cell Line:DLD-1, HT29, SW620 and HCT116 CRC cell lines and the non-tumourigenic CCD-841 cell line Concentration:2, 3, 4 μM Incubation Time:24 hours Result:Triggered to cell death.Western Blot Analysis Cell Line:DLD-1, HT29 and SW620 cell lines Concentration:2, 4, 6, 8, 10 uM Incubation Time:24 hours Result:A dosage-dependent decrease in the levels of thymidylate synthase (TS) and thymidine kinase (TK1) proteins.

Animal Model:Athymic nu/nu mice, CD1 nude mice, and BALB/c nude (six-week-old) bearing human tumor xenografts (colon adenocarcinoma HT29, non-small cell lung cancer (NSCLC) H-460, breast adenocarcinoma MDA-MB-231)Dosage:7.5 mg/kg, 6 mg/kg, 5 mg/kg, 3 mg/kg, 1 mg/kg, 0.3 mg/kg Administration:Administration routes (intraperitoneal or intravenous), treatment schedule (5 consecutive days, 3 days per week, 2 days per week, 1 day per week) Result:The LD50 was 10.9 mg/kg in mice. The effective dose used in the in vivo experiments was 7.5 mg/kg.

TCD-717 | TCD717 | RSM932A

Others

ChoK

ChoK

Cancer

Solid Tumors

850807-63-5

717.737

C46H38Cl2N42Br

>98% (HPLC)

In Vitro:?DMSO : 16.67 mg/mL (19.00 mM)

CN(C1=CC=C(Cl)C=C1)C(C2=C3C=CC=C2)=CC=[N+]3CC4=CC=C(C5=CC=C(C[N+]6=CC=C(N(C7=CC=C(Cl)C=C7)C)C8=C6C=CC=C8)C=C5)C=C4.[Br-].[Br-]

Quinolinium, 1,1'-[[1,1'-biphenyl]-4,4'-diylbis(methylene)]bis[4-[(4-chlorophenyl)methylamino]-, dibromide (9CI)

(-20℃)

With Ice Pack

≥ 2 years