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c-Kit-IN-3 maleate

CAS No. :

MCE 站：c-Kit-IN-3 maleate

产品活性：c-Kit-IN-3 maleate (Compound 18) 是一种有效的 c-KIT 激酶抑制剂，IC₅₀ 为 4 nM。c-Kit-IN-3 maleate 在生化分析中显示出对 c-KIT 激酶和多种耐药突变体的强大效价，并具有很高的生物利用度。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：c-Kit

In Vitro: c-Kit-IN-3 (Compound 18; 0.1-10 μM; 6 days; primary GIST patient cells) exhibits dose-dependent antiproliferative effects.
c-Kit-IN-3 (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).
c-Kit-IN-3 (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.
c-Kit-IN-3 (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).
?c-Kit-IN-3 (Compound 18; 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 (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.

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