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CHMFL-KIT-033 Sale

目录号 : GC35685

CHMFL-KIT-033 是一种有效、可选择性的 c-KIT T670I 突变型的抑制剂, IC50 值为 0.045 μM。用于胃肠道间质瘤 (GISTs) 的治疗。

CHMFL-KIT-033 Chemical Structure

Cas No.:2351801-41-5

规格 价格 库存 购买数量
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产品描述

CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM[1]. IC50: 0.045 μM (c-KIT T670I mutant)[1]

[1]. Liu X, et al. Discovery of ( E)- N1-(3-Fluorophenyl)- N3-(3-(2-(pyridin-2-yl)vinyl)-1 H-indazol-6-yl)malonamide (CHMFL-KIT-033) as a Novel c-KIT T670I Mutant Selective Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). J Med Chem. 2019 May 23;62(10):5006-5024.

Chemical Properties

Cas No. 2351801-41-5 SDF
Canonical SMILES O=C(CC(NC1=CC=CC(F)=C1)=O)NC2=CC(NN=C3/C=C/C4=CC=CC=N4)=C3C=C2
分子式 C23H18FN5O2 分子量 415.42
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.4072 mL 12.036 mL 24.072 mL
5 mM 0.4814 mL 2.4072 mL 4.8144 mL
10 mM 0.2407 mL 1.2036 mL 2.4072 mL
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Research Update

Discovery of ( E)- N1-(3-Fluorophenyl)- N3-(3-(2-(pyridin-2-yl)vinyl)-1 H-indazol-6-yl)malonamide (CHMFL-KIT-033) as a Novel c-KIT T670I Mutant Selective Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs)

J Med Chem 2019 May 23;62(10):5006-5024.PMID:31046271DOI:10.1021/acs.jmedchem.9b00176

Gain-of-function mutations of c-KIT kinase play crucial pathological roles for the gastrointestinal stromal tumors (GISTs). Despite the success of imatinib as the first-line treatment of GISTs, dozens of drug-acquired resistant mutations emerge, and c-KIT T670I is one of the most common mutants among them. Although several kinase inhibitors are capable of overcoming the T670I mutant, none of them can achieve the selectivity over the c-KIT wild-type (wt), which also plays important roles in a variety of physiological functions such as hematopoiesis. Starting from axitinib, through fragment hybrid type II kinase inhibitor design approach, we have discovered a novel inhibitor 24, which not only exhibits potent activity to c-KIT T670I mutant but also achieves 12-fold selectivity over c-KIT wt. Compound 24 displays good antiproliferative effects against c-KIT T670I mutant-driven GIST cell lines (GIST-T1/T670I and GIST-5R) and also exhibits suitable in vivo pharmacokinetic profiles as well as dose-dependent antitumor efficacy. This study provides a proof of concept for developing a c-KIT mutant selective inhibitor that theoretically can render a better therapeutic window.