Bioactivity | KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis[1]. |
Invitro | KRAS G12C inhibitor 57 (Compound 50) (0-10 μM; 3 days) 对 KRAS 和 KRAS 驱动的细胞系有选择性抑制,以及对下游信号的强烈抑制[1]。KRAS G12C inhibitor 57 (0.1-1 μM; 24 h) 诱导 H358 细胞凋亡[1]。KRAS G12C inhibitor 57 (0.1-1 μM; 48 h) 抑制 H358 细胞肿瘤转移[1]。 Western Blot Analysis[1] Cell Line: |
In Vivo | KRAS G12C inhibitor 57 (Compound 50) (10 and 30 mg/kg; p.o.; daily for 20 days) 对 H358异种移植模型小鼠有抗肿瘤作用。Pharmacokinetic data of KRAS G12C inhibitor 57 (Compound 50) in ICR mice. [1] Parameter |
Name | KRAS G12C inhibitor 57 |
CAS | 2821863-70-9 |
Formula | C35H38FN7O2 |
Molar Mass | 607.72 |
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]. Song Z, et al. Identification of novel Pyrrolo [2, 3-d] Pyrimidine-based KRAS G12C inhibitors with anticancer effects. European Journal of Medicinal Chemistry, 2022: 114907. |