EGFR T790M/L858R-IN-2_product_DataBase

Bioactivity	EGFRT790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFRT790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFRT790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFRT790M/L858R-IN-2 shows anti-cancer activity[1].
Invitro	EGFRT790M/L858R-IN-2 (compound 28f) (0.1, 1, 10 µM; 4 h)以剂量依赖性方式降低 H1975、HCC827 细胞中 p-EGFR、P-AKT、P-ERK1/2 的表达[1].EGFRT790M/L858R-IN-2 (0.1、1、10 µM；48 小时) 在 H1975、HCC827 细胞中诱导细胞凋亡和细胞周期停滞于 G1 期[1]。EGFRT790M/L858R-IN-2 (0.1、1、10 µM；14 天) 以剂量依赖性方式抑制集落形成和细胞迁移[1]。 Western Blot Analysis[1] Cell Line:
In Vivo	EGFRT790M/L858R-IN-2 (5、10、20 mg/kg；i.p.；每天) 以剂量依赖性方式抑制肿瘤生长[1]。 Animal Model:
Name	EGFR T790M/L858R-IN-2
Formula	C28H28FN7O
Molar Mass	497.57
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]. Pei J, et al. Design, Synthesis, and Antitumor Activity of Potent and Selective EGFR L858R/T790M Inhibitors and Identification of a Combination Therapy to Overcome Acquired Resistance in Models of Non-small-cell Lung Cancer. J Med Chem. 2023 Apr 27;66(8):5719-5752.

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