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Naquotinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Naquotinib图片
CAS NO:1448232-80-1
包装:50mg
市场价:7800元

产品名称
ASP8273
产品介绍
Naquotinib (ASP8273) 是有口服活性,不可逆的EGFR突变体抑制剂;对EGFR突变体和EGFR的IC50值分别为8-33和230 nM。
生物活性

Naquotinib (ASP8273) is an orally available, mutant-selective and irreversibleEGFRinhibitor; withIC50s of 8-33 nM towardEGFRmutants and 230 nM forEGFR.

IC50& Target[1]

EGFR

230 nM (IC50)

EGFRT790M

 

EGFRL858R/T790M

 

EGFRL858R

 

EGFRExon 19 deletion/T790M

 

体外研究
(In Vitro)

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 down-stream 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 IC50value of 70nM while other EGFR-TKIs are only partially effective[2].

体内研究
(In Vivo)

Oral Naquotinib treatment dose dependently induces tumor regression in NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models. Dosing schedules does 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].

Clinical Trial
分子量

562.71

Formula

C30H42N8O3

CAS 号

1448232-80-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.