Bioactivity | EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner[1]. |
Invitro | EGFR/C797S-IN-1 (compound 14d) (0-10 µM; 72 h) 显示抗增殖活性,对BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S 的 IC50 值分别为 0.75、0.09 µM [1]。EGFR/C797S-IN-1 (1-10000 nM; 24 h) 以剂量依赖性降低 p-EGFR、p-AKT、p-ERK 蛋白的表达[1]。 Cell Proliferation Assay[1] Cell Line: |
In Vivo | EGFR/C797S-IN-1 (10、30 mg/kg;每日一次,持续 14 天) 呈剂量依赖性显著降低小鼠体内的肿瘤生长[1]。 Animal Model: |
Name | EGFR/C797S-IN-1 |
CAS | 2378188-21-5 |
Formula | C28H30N4O3 |
Molar Mass | 470.56 |
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]. Dou D, et al. Discovery and optimization of 4-anilinoquinazoline derivatives spanning ATP binding site and allosteric site as effective EGFR-C797S inhibitors. Eur J Med Chem. 2022 Dec 15;244:114856. |