EGFR-IN-48 是一种有效的且具有口服活性的EGFR抑制剂，对 EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWT的IC50值分别为 0.193 nM, 0.251 nM, 10.4 nM。EGFR-IN-48 抑制 BaF3EGFR del19/T790M/C797S和 PC-9EGFR del19/T790M/C797S细胞的增殖，IC50值分别为 1.526 nM 和 66.7 nM。

EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC 50 s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR d19/TM/CS, EGFR LR/TM/CS, EGFR WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3 EGFR del19/T790M/C797S and PC-9 EGFR del19/T790M/C797S cells with IC 50 s of 1.526, 66.7 nM, respectively [1].

EGFR-IN-48 (compound 23) (10 nM) shows anti-proliferative activities against BaF3 EGFR del19/T790M/C797S and PC-9 EGFR del19/T790M/C797S cells with IC 50 s of 1.526, 66.7 nM, respectively [1]. EGFR-IN-48 exhibits potent inhibitory activities against various clinically relevant EGFR mutants with IC 50 s of 10.4, 3.1, 0.9, 0.1, 0.2, 0.3, 0.2 nM for EGFR WT, EGFR LR, EGFR del19, EGFR del19/TM, EGFR LR/TM, EGFR LR/TM/CS, EGFR drl19/TM/CS, respectively [1]. Cell Proliferation Assay [1] Cell Line: BaF3 EGFR del19/T790M/C797S, PC-9 EGFR del19/T790M/C797S cells Concentration: 10 nM Incubation Time: Result: Showed anti-proliferative activities against BaF3 EGFR del19/T790M/C797S and PC-9 EGFR del19/T790M/C797S cells with IC 50 s of 1.526, 66.7 nM, respectively.

EGFR-IN-48 (2 mg/kg for i.v.; 10 mg/kg for o.p.) shows good oral bioavailability and high plasma exposure in CD-1 mouse [1]. Pharmacokinetic Parameters of EGFR-IN-48 in CD-1 mouse [1]. Route Dose (mg/kg) V dss (L/kg) T 1/2 (h) CL (L/h/kg) AUC 0-last (h*ng/mL) C max (ng/mL) T max (h) F (%) i.v. 2 0.7 3.3 2.4 13820.0 p.o. 10 33811.0 6600.0 0.5 48.9

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years