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CHMFL-EGFR-202
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。
CHMFL-EGFR-202图片
CAS NO:2089381-40-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
CHMFL-EGFR-202 是一种有效、不可逆的表皮生长因子受体(EGFR)突变型激酶抑制剂, 对 耐药突变型 EGFR T790M 和 WT EGFR 激酶作用的IC50值分别为 5.3 nM 和 8.3 nM。在细胞中,CHMFL-EGFR-202 对 EGFR L858R/T790M 的选择性是 EGFR 野生型的 10 倍。CHMFL-EGFR-202 以 “DFG-in-C-helix-out” 的不活跃结合构象形式共价结合 EGFR,对 EGFR 突变体驱动的非小细胞肺癌 (NSCLC) 细胞株具有较强的抗增殖作用。
生物活性

CHMFL-EGFR-202 is a potent, irreversible inhibitor ofepidermal growth factor receptor (EGFR) mutant kinase, withIC50s of 5.3 nM and 8.3 nM for drug-resistant mutantEGFRT790M and WTEGFRkinases, respectively. CHMFL-EGFR-202 exhibits ~10-fold selectivity forEGFRL858R/T790M against theEGFRwild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation withEGFR, with strong antiproliferative effects againstEGFRmutant-driven nonsmall-cell lungcancer(NSCLC) cell lines[1].

IC50& Target

EGFRT790M

5.3 nM (IC50)

EGFR

8.3 nM (IC50)

ErbB2

8.1 nM (IC50)

ErbB4

3.2 nM (IC50)

MEK1

161 nM (IC50)

Btk

24.5 nM (IC50)

BLK

8.1 nM (IC50)

BMX

111 nM (IC50)

体外研究
(In Vitro)

CHMFL-EGFR-202 potently inhibits EGFR primary mutants (L858R, del19) and drug-resistant mutant L858R/T790M[1].
CHMFL-EGFR-202 displays strong binding affinities against wild-type, G719C/S, L858R, L858R/T790M, L861Q, and T790M among EGFR wild-type and mutant kinases[1].
CHMFL-EGFR-202 also exhibits strong binding affinities against BLK, BMX, BTK, ERBB2, ERBB4, LOK, MEK1, and MEK5 kinases (percent of control score less than 1% at 1 μM)[1].
CHMFL-EGFR-202 trongly inhibits BLK, BTK, ERBB2 and ERBB4 with IC50s of 8.1 nM, 24.5 nM, 8.1 nM and 3.2 nM, respectively[1].
CHMFL-EGFR-202 moderately inhibits BMX and MEK1 kinases with IC50of 111.0 nM and 161.0 nM[1].

分子量

489.96

Formula

C25H24ClN7O2

CAS 号

2089381-40-6

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.