Bioactivity | c-Met-IN-22 (compound 51am) is an orally active inhibitor against c-Met with an IC50 value of 2.54 nM. c-Met-IN-22 has antiproliferative and antitumor activities. c-Met-IN-22 induces cell apoptosis[1]. |
Invitro | c-Met-IN-22 在细胞 MNK-45,A-549,HT-29,MDA-MB-231,HUVEC 和 FHC 中具有抗增殖活性,IC50 值分别为0.092,0.83,0.68,3.94,2.54 和 8.63 μM[1]。c-Met-IN-22 对突变体 H1094R,D1228H,Y1230H,Y1235D 和 M1250T 仍具有抑制作用,IC50 值分别为 93.6,29.4,45.8,54.2 和 26.5 nM[1]。c-Met-IN-22(0,2.5, 5.0 和 10.0 μM; 24 h)具有剂量依赖性的抑制 MKN-45 中 c-Met 的磷酸化[1]。c-Met-IN-22(0.4,0.8 和 1.2 μM;24 h)诱导 MNK-45 细胞周期在 G2 阶段的阻滞和细胞凋亡,且具有剂量依赖性[1]。 0 --> c-Met-IN-22 相关抗体: Apoptosis Analysis[1] Cell Line: |
In Vivo | c-Met-IN-22(10mg/kg;口服;单剂量)在 BALB/c 小鼠中表现出良好的口服生物利用度(F=69%),清除半衰期是 5.6 小时,清除率是 0.87L/h•kg [1]。c-Met-IN-22(1.5mg/kg,静脉注射)在 BALB/c 小鼠中的清除半衰期是 3.2 小时[1]。c-Met-IN-22 在 BALB/c 小鼠体内的药代动力学分析[1]Route |
Name | c-Met-IN-22 |
Formula | C21H10Cl3F2N3O2S |
Molar Mass | 512.74 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Xiang Nan,et al. Design, synthesis, and biological evaluation of thiazole/thiadiazole carboxamide scaffold-based derivatives as potential c-Met kinase inhibitors for cancer treatment. J Enzyme Inhib Med Chem. 2023 Dec;38 |