Naquotinib 是一种口服的、突变体选择性和不可逆的 EGFR 抑制剂，对EGFR突变体和EGFR的IC50值分别为8-33和230 nM。

Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; (IC50s: 8-33 nM and 230 nM toward EGFR mutants and EGFR.

In assays using endogenously EGFR-dependent cells, Naquotinib inhibits the growth of PC-9(del ex19), HCC827(del ex19), NCI-H1975(del ex19/T790M) and PC-9ER(del ex19/T790M) with IC50s of 8-33 nM [1]. Naquotinib selectively inhibits phosphorylation of EGFR and its downstream signal pathway, ERK, and Akt from 10nM in HCC827 and NCI-H1975 while inhibitory effects are only detected at 1000nM in A431.In NCI-H1650 (del ex19), Naquotinib inhibits cell growth with an IC50 value of 70nM while other EGFR-TKIs are only partially effective [2].

In NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models, oral Naquotinib treatment dose-dependently induces tumor regression. Dosing schedules do not affect the efficacy of Naquotinib. In an NCI-H1975 xenograft model, complete regression of tumor is achieved after 14-days of Naquotinib treatment. Complete regression is maintained in 50% of mice more than 85 days after cessation of Naquotinib treatment [2].

1448232-80-1

C30H42N8O3

562.71

ASP8273

H2O:Insoluble
DMSO:40 mg/mL (71.08 mM)
H2O:Insoluble
Ethanol:80 mg/mL (142.16 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years