c-Kit-IN-3 D-tartrate

c-Kit-IN-3 (D-tartrate) (Compound 18) 是一种有效的 c-KIT kinase 激酶抑制剂，对 BaF3-tel-c-KIT (IC50 为 4 nM) 和广泛的耐药性突变体 (对 BaF3-tel-c-KIT-T670I 的IC50为 8 nM)，具有很高的生物利用度。

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库存: 现货

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5mg

￥1300.00

1040.00

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10mg

￥2175.00

1740.00

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50mg

￥8637.00

6910.00

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100mg

￥14100.00

11280.00

- +
200mg

￥0.00

0.00

- +
500mg

￥0.00

0.00

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Background

c-Kit-IN-3 (D-tartrate) (Compound 18) is a potent c-KIT kinase inhibitor, which is potent and selective against BaF3-tel-c-KIT (IC50 of 4 nM) and a broad spectrum of drug-resistant mutants (IC50 of 8 nM for BaF3-tel-c-KIT-T670I) with improved bioavailability[1].

c-Kit-IN-3 (D-tartrate) (Compound 18; 0.006 μM-1.37 μM) potently inhibits the growth of c-KIT-dependent GIST cancer cells, such as GIST-T1 (GI50: 0.006 μM); GIST-882 (GI50: 0.013 μM); GIST-T1-T670I (GI50 : 0.011 μM); GIST-5R (GI50: 0.073 μM); GIST-48B (GI50: 1.37 μM), respectively[1].c-Kit-IN-3 (D-tartrate) (Compound 18; 0.01-1 μM; 24 hours; GIST-T1, GIST-T1-T670I, and GIST-5R cells) treatment induces dose-dependent cell apoptotic death (by examining the cleaved PARP and cleaved caspase 3)[1].c-Kit-IN-3 (D-tartrate) (Compound 18; 0.01-1 μM; 24 hours; GIST-T1, GIST-T1-T670I, and GIST-5R cells) treatment arrests the cell cycle into the G0/G1 phase in all of these three cell lines[1].c-Kit-IN-3 (D-tartrate) (Compound 18; 0.1-10 μM; 6 days; primary GIST patient cells) exhibits dose-dependent antiproliferative effects[1].c-Kit-IN-3 (D-tartrate) (Compound 18; 0-1 μM; 24 hours) blocks the autophosphorylation of c-KIT pY703, pY719, and pY823 in GIST-T1, GIST-T1-T670I, and GIST-5R, respectively, cells at a concentration of 30 nM and inhibits the downstream signaling mediators pAKT (T308/S473), pS6 (S235/236), and pERK (T202/204)[1].c-Kit-IN-3 (D-tartrate) (Compound 18; 0-1 μM; 2 hours) induces dose-dependent cell apoptotic death (by examining the cleaved PARP and cleaved caspase 3) and arrest the cell cycle into the G0/G1 phase in all of these three cell lines[1].

c-Kit-IN-3 (D-tartrate) (Compound 18; 40-100 mg/kg; oral gavage; daily; for 11 days; for 4 weeks; female BALB/C-nu mice) treatment dose dependently inhibits the BaF3-tel-c-KIT-T670I tumor progression and exhibited almost 100% TGI (tumor growth inhibition) at a dosage of 100 mg/kg/day. And do not affect the animal weights[1]. Animal Model: Female BALB/C-nu mice bearing established BaF3-tel-c-KIT-T670I tumor xenograft[1]

[1]. Wu Y, et al. Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors. J Med Chem. 2019 Jul 11;62(13):6083-6101.