产品
编 号：F013655
分子式：C23H17FN6O
分子量：412.42
分子式：C23H17FN6O
分子量：412.42
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
695
In-stock
1mg
260
In-stock
5mg
630
In-stock
10mg
760
In-stock
25mg
1560
In-stock
50mg
2480
In-stock
100mg
3880
In-stock
200mg
5580
In-stock
结构图
CAS No: 1029712-80-8
产品详情
生物活性：
Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase.
体内研究：
Capmatinib (INCB28060) (1-30 mg/kg；PO，每天两次，持续 2 周) 对肿瘤生长具有剂量依赖性抑制作用，并且在处理期间对所有剂量均表现出良好的耐受性，没有明显的毒性或体重的的损失证据在 U-87MG 肿瘤小鼠模型。 Capmatinib (INCB28060) (0.03-10 mg/kg；PO，单剂量) 抑制 S114 肿瘤中的 c-MET 磷酸化小鼠模型。Animal Model:Female Balb/c nu/nu mice (inoculated subcutaneously with 5×106 U-87MG glioblastoma cells)
Dosage:1, 3, 10 and 30 mg/kg
Administration:PO, twice daily, for 2 weeks
Result:Exhibited dose-dependent inhibition of tumor growth with 35% and 76% at 1 and 3 mg/kg once daily; resulted in partial regressions in 6 of 10 U-87MG tumor-bearing mice at 10 mg/kg once daily; and showed well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss.
Animal Model:Female Balb/c nu/nu mice (inoculated subcutaneously with 4×106 S114 tumor cells)
Dosage:0.03, 0.1, 0.3, 1, 3 and 10 mg/kg
Administration:PO, single dosage
Result:Caused approximately 50% and 90% inhibition of c-MET phosphorylation at 0.03 and 0.3 mg/kg after administration of 30 min, and inhibition of phospho-c-MET exceeded 90% after 7 hours.
体外研究：
Capmatinib (INCB28060) 抑制 c-MET 磷酸化，IC50 值约为 1 nM，浓度约为 4 nM 时抑制 c-MET 超过 90%，这是可逆的，在去除化合物后的数小时内效果显著降低，48 小时后完全消失。 Capmatinib (INCB28060) (0-10000 nM；72 小时) 抑制 SNU-5，S114、H441 和 U-87MG 的增殖。 Capmatinib (INCB28060) (0.06-62.25 nM；2h) 有效抑制 c-MET 磷酸化以及 c-MET 通路下游效应子，例如 ERK1/2、AKT、FAK、GAB1 和 STAT3/5。 Capmatinib (INCB28060) (0.24-63 nM；过夜) 可防止 HGF 刺激的 H441 细胞迁移。 Capmatinib (INCB28060) (0.5-50 nM；20 分钟) 可快速抑制 EGFR 和 HER-3 的磷酸化。 Capmatinib (INCB28060) (0-333 nM；24 h) 诱导 SNU-5 细胞凋亡。
Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase.
体内研究：
Capmatinib (INCB28060) (1-30 mg/kg；PO，每天两次，持续 2 周) 对肿瘤生长具有剂量依赖性抑制作用，并且在处理期间对所有剂量均表现出良好的耐受性，没有明显的毒性或体重的的损失证据在 U-87MG 肿瘤小鼠模型。 Capmatinib (INCB28060) (0.03-10 mg/kg；PO，单剂量) 抑制 S114 肿瘤中的 c-MET 磷酸化小鼠模型。Animal Model:Female Balb/c nu/nu mice (inoculated subcutaneously with 5×106 U-87MG glioblastoma cells)
Dosage:1, 3, 10 and 30 mg/kg
Administration:PO, twice daily, for 2 weeks
Result:Exhibited dose-dependent inhibition of tumor growth with 35% and 76% at 1 and 3 mg/kg once daily; resulted in partial regressions in 6 of 10 U-87MG tumor-bearing mice at 10 mg/kg once daily; and showed well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss.
Animal Model:Female Balb/c nu/nu mice (inoculated subcutaneously with 4×106 S114 tumor cells)
Dosage:0.03, 0.1, 0.3, 1, 3 and 10 mg/kg
Administration:PO, single dosage
Result:Caused approximately 50% and 90% inhibition of c-MET phosphorylation at 0.03 and 0.3 mg/kg after administration of 30 min, and inhibition of phospho-c-MET exceeded 90% after 7 hours.
体外研究：
Capmatinib (INCB28060) 抑制 c-MET 磷酸化，IC50 值约为 1 nM，浓度约为 4 nM 时抑制 c-MET 超过 90%，这是可逆的，在去除化合物后的数小时内效果显著降低，48 小时后完全消失。 Capmatinib (INCB28060) (0-10000 nM；72 小时) 抑制 SNU-5，S114、H441 和 U-87MG 的增殖。 Capmatinib (INCB28060) (0.06-62.25 nM；2h) 有效抑制 c-MET 磷酸化以及 c-MET 通路下游效应子，例如 ERK1/2、AKT、FAK、GAB1 和 STAT3/5。 Capmatinib (INCB28060) (0.24-63 nM；过夜) 可防止 HGF 刺激的 H441 细胞迁移。 Capmatinib (INCB28060) (0.5-50 nM；20 分钟) 可快速抑制 EGFR 和 HER-3 的磷酸化。 Capmatinib (INCB28060) (0-333 nM；24 h) 诱导 SNU-5 细胞凋亡。
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