PeptideDB

EGFR/C797S-IN-1

CAS: 2378188-21-5 F: C28H30N4O3 W: 470.56

EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferati
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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.