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c-Kit-IN-3 L-tartrate

CAS No. :

MCE 站：c-Kit-IN-3 L-tartrate

产品活性：c-Kit-IN-3 L-tartrate (Compound 18) 是一种有效的 c-KIT 激酶抑制剂，对 c-KIT wt 和 c-KIT T670I 的 IC₅₀ 分别为 4 nM 和 8 nM。c-Kit-IN-3 L-tartrate 对近膜结构域中的大多数功能获得性突变，ATP 结合口袋中的抗药性突变以及激活环显示出强大的效力。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：c-Kit

In Vitro: c-Kit-IN-3 L-tartrate (Compound 18; 0.1-10 μM; 6 days; primary GIST patient cells) exhibits dose-dependent antiproliferative effects.
c-Kit-IN-3 L-tartrate (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).
c-Kit-IN-3 L-tartrate (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.
c-Kit-IN-3 L-tartrate (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).
c-Kit-IN-3 L-tartrate potently inhibits the activity of CSF1R (IC₅₀: 18 nM), PDGFRα (IC₅₀: 25 nM), RET (IC₅₀: 34 nM), and it relatively less potently inhibits DDR1 (IC₅₀: 135 nM), FLT4 (IC₅₀: 121 nM), and PDGFRβ (IC₅₀: 97 nM).
c-Kit-IN-3 L-tartrate (0.006 μM-1.37 μM) potently inhibits the growth of c-KIT-dependent GIST cancer cells, such as GIST-T1 (IC₅₀: 0.006 μM); GIST-882 (IC₅₀: 0.013 μM); GIST-T1-T670I (IC₅₀: 0.011 μM); GIST-5R (IC₅₀: 0.073 μM); GIST-48B (IC₅₀: 1.37 μM), respectively.

In Vivo: c-Kit-IN-3 L-tartrate (Compound 18; oral gavage; 20-100 mg/kg/day; for 11 days; female BALB/C-nu mice) treatment dose dependently inhibits the tumor progression.
c-Kit-IN-3 L-tartrate (1 mg/kg (iv for mice, rats, dog); 10 mg/kg (p.o. for mice, rats ) and 5 mg/kg (p.o. for dog)) has T_1/2 of 4.5 h, 6.4 h, 19.4 h for mice, rats and dogs, respectively. And it possesses acceptable bioavailability in mice (F = 43%), rats (F = 50%), and dogs (F = 81%).

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