| Bioactivity | CFL-137 is a potent KRasG12C inhibitor. CFL-137 shows an antiproliferative effect. CFL-137 shows anticancer activity. CFL-137 has the potential for the research of lung cancer[1]. |
| Invitro | CFL-137 (72 h) 显示出抗增殖作用，对 H1792, SW1573, MiaPaca2, H358, A549, SW480, PANC-1, LCLC-103H, BxPC3, HCA-7, MRC-5, HUVEC-TERT, CCD-986Sk 细胞的 IC50 值分别为 11.4, 24.2, 24.5, 12.3, 43.3, 44.5, 27.63, 32.4, 46.9, 26.2, 25.0, 10.8, 66.2 µM[1]。 |
| In Vivo | CFL-137 (5 mg/kg，5 次治疗；15 mg/kg，5 次治疗；30 mg/kg，3 次治疗；i.p.) 减少皮下人肺癌 H1792 (KRasG12C 突变体) 和 LCLC-103H (KRasWT) 小鼠肿瘤模型的生长[1]。 Animal Model: |
| Name | CFL-137 |
| CAS | 708-06-5 |
| Formula | C11H8O2 |
| Molar Mass | 172.18 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [1]. Orgován Z, et al. Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency. Eur J Med Chem. 2023 Mar 15;250:115212. |