c-Kit-IN-3 (hydrochloride)
- CAS号:
- 英文名:c-Kit-IN-3 (hydrochloride)
- 中文名:c-Kit-IN-3 (hydrochloride)
- CBNumber:CB85848748
- 分子式:
- 分子量:0
- MOL File:Mol file
c-Kit-IN-3 (hydrochloride)性质、用途与生产工艺
- 生物活性 c-Kit-IN-3 hydrochloride (Compound 18) 是一种有效的 c-KIT 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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靶点
IC50: 4 nM (BaF3-tel-c-KIT); 8 nM (BaF3-tel-c-KIT-T670I)
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体外研究
c-Kit-IN-3 hydrochloride (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. c-Kit-IN-3 hydrochloride(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 hydrochloride (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 hydrochloride (Compound 18; 0.1-10 μM; 6 days; primary GIST patient cells) exhibits dose-dependent antiproliferative effects. c-Kit-IN-3 hydrochloride (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 hydrochloride (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.
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体内研究
c-Kit-IN-3 hydrochloride (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.
Animal Model: Female BALB/C-nu mice bearing established BaF3-tel-c-KIT-T670I tumor xenografts Dosage: 40 mg/kg, 100 mg/kg Administration: Oral gavage; daily; for 11 days Result: Inhibited the BaF3-tel-c-KIT-T670I tumor progression and exhibited almost 100% TGI (tumor growth inhibition) at a dosage of 100 mg/kg/day.
- 公司名称:上海弘渠生物医药科技有限公司
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- 国家:中国
- 产品数:5132
- 优势度:58