Naquotinib mesylate 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 mesylate is an orally available, mutant-selective and irreversible inhibitor of EGFR(iC50s of 8-33 nM and 230 nM for toward EGFR mutants and EGFR).

In NCI-H1650 (del ex19), Naquotinib inhibits cell growth with an IC50 value of 70nM while other EGFR-TKIs are only partially effective.Naquotinib selectively inhibits phosphorylation of EGFR and its down-stream signal pathway, ERK and Akt from 10nM in HCC827 and NCI-H1975 while inhibitory effects are only detected at 1000nM in A431[2].

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].

1448237-05-5

C31H46N8O6S

658.81

ASP8273 (mesylate);Naquotinib mesylate

DMSO:12.5 mg/mL (18.97 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years