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 分别为 5.3 nM 和 8.3 nM。

CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase (IC50s: 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases).

CHMFL-EGFR-202 exhibits ~10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 potently inhibits EGFR primary mutants (L858R, del19) and drug-resistant mutant L858R/T790M. CHMFL-EGFR-202 displays strong binding affinities against wild-type, L861Q, G719C/S, L858R/T790M, L858R, and T790M among EGFR wild-type and mutant kinases. 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). CHMFL-EGFR-202 strongly inhibits BLK, BTK, ERBB2 and ERBB4 (IC50s: of 8.1 nM, 24.5 nM, 8.1 nM and 3.2 nM). CHMFL-EGFR-202 moderately inhibits BMX and MEK1 kinases (IC50s: 111.0 nM and 161.0 nM)[1].

2089381-40-6

C25H24ClN7O2

489.96

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