| Bioactivity | KRASG12C IN-1 is a potent and covalent KRASG12C inhibitor that traps KRASG12C in the GDP-bound state. KRASG12C IN-1 exhibits potent antitumor activity against KRAS-mutant non-small cell lung cancer[1]. |
| Invitro | KRASG12C IN-1 (化合物 20a) (72 h) 有效且选择性的抑制 KRASG12C NSCLC 细胞增殖，抑制 NCI-H358 和 NCI-H23 细胞的 IC50 值分别为 0.5 和 1.3 μM，选择性是 KRASG12S 和 KRASWT 细胞的 7 倍和 21 倍[1]。KRASG12C IN-1 (0.5-8.0 μM; 6 h) 降低 KRASG12C-突变型 NCIH358 细胞中 ERK 和 AKT 的磷酸化[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | KRASG12C IN-1 (化合物 20a) (10-15 mg/kg; 腹腔注射每2天一次共21天) 通过抑制 KRASG12C 信号抑制 H358 异种移植模型中的肿瘤生长[1]。 Animal Model: |
| Name | KRASG12C IN-1 |
| Formula | C19H18Cl2FN3O2 |
| Molar Mass | 410.27 |
| 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]. Cheng R, et, al. Design, synthesis, and evaluation of 4(1H)-quinolinone and urea derivatives as KRASG12C inhibitors with potent antitumor activity against KRAS-mutant non-small cell lung cancer. Eur J Med Chem. 2022 Dec 15;244:114808. |