产品
编 号：F039430
分子式：C25H23FN8O2S2
分子量：550.63
分子式：C25H23FN8O2S2
分子量：550.63
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1116743-46-4
产品详情
生物活性：
SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC50 is 4.2 nM and Ki is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer.
体内研究：
SAR125844 (45 mg/kg，静脉注射，单次剂量) 可使 SNU-5 和 Hs 746T 荷瘤小鼠的肿瘤消退。SAR125844 (20 mg/kg，静脉注射，单次剂量) 纳米制剂在 MET 扩增的胃肿瘤模型中产生长时间的药效学影响和肿瘤消退。SAR125844 (20 mg/kg，静脉注射，单次剂量) 在荷瘤小鼠体内显示 MET 激酶在 4 小时完全抑制 (96%)，24 小时显著抑制 (80%)，48 小时部分抑制 (61%)。Animal Model:SNU-5 and Hs 746T tumor-bearing mice
Dosage:45 mg/kg
Administration:Intravenous injection (i.v.)
Result:Resulted in complete and almost complete tumor regression in 3 of 8 mice and 5 of 8 mice, respectively.
Animal Model:MET-amplified gastric tumor model mice
Dosage:5 mg/kg, 11 mg/kg, 21 mg/kg, 53 mg/kg, 106 mg/kg, 213 mg/kg
Administration:Intravenous injection (i.v.)
Result:Resulted complete tumor regression in 7 of 8 of mice at 53, 106, and 213 mg/kg and partial regression at 11 and 21 mg/kg.Showed more than 80% MET inhibition at all doses and maintained for 96 hours at 213 mg/kg, 72 hours at106 mg/kg, and 48 hours at 53 mg/kg.Showed complete or near-complete regression (92%–99%) and maintained for 7 days at 106 mg/kg, and 48 hours at 53 mg/kg.
体外研究：
SAR125844 (1-10000 nM, 96 h) 抑制 H-460 细胞、HCT116 细胞、H1993 细胞、EBC-1 细胞、SNU-5细胞、OE33 细胞、Hs 746T 细胞和 MKN-45 细胞的增殖。SAR125844 (1-300 nM, 24 72 h) 促进 SNU-5 细胞凋亡。SAR125844 (3-1000 nM, 20 h) 抑制 HGF 介导的 PC-3 细胞迁移。
SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC50 is 4.2 nM and Ki is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer.
体内研究：
SAR125844 (45 mg/kg，静脉注射，单次剂量) 可使 SNU-5 和 Hs 746T 荷瘤小鼠的肿瘤消退。SAR125844 (20 mg/kg，静脉注射，单次剂量) 纳米制剂在 MET 扩增的胃肿瘤模型中产生长时间的药效学影响和肿瘤消退。SAR125844 (20 mg/kg，静脉注射，单次剂量) 在荷瘤小鼠体内显示 MET 激酶在 4 小时完全抑制 (96%)，24 小时显著抑制 (80%)，48 小时部分抑制 (61%)。Animal Model:SNU-5 and Hs 746T tumor-bearing mice
Dosage:45 mg/kg
Administration:Intravenous injection (i.v.)
Result:Resulted in complete and almost complete tumor regression in 3 of 8 mice and 5 of 8 mice, respectively.
Animal Model:MET-amplified gastric tumor model mice
Dosage:5 mg/kg, 11 mg/kg, 21 mg/kg, 53 mg/kg, 106 mg/kg, 213 mg/kg
Administration:Intravenous injection (i.v.)
Result:Resulted complete tumor regression in 7 of 8 of mice at 53, 106, and 213 mg/kg and partial regression at 11 and 21 mg/kg.Showed more than 80% MET inhibition at all doses and maintained for 96 hours at 213 mg/kg, 72 hours at106 mg/kg, and 48 hours at 53 mg/kg.Showed complete or near-complete regression (92%–99%) and maintained for 7 days at 106 mg/kg, and 48 hours at 53 mg/kg.
体外研究：
SAR125844 (1-10000 nM, 96 h) 抑制 H-460 细胞、HCT116 细胞、H1993 细胞、EBC-1 细胞、SNU-5细胞、OE33 细胞、Hs 746T 细胞和 MKN-45 细胞的增殖。SAR125844 (1-300 nM, 24 72 h) 促进 SNU-5 细胞凋亡。SAR125844 (3-1000 nM, 20 h) 抑制 HGF 介导的 PC-3 细胞迁移。
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