CHMFL-EGFR-202

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CHMFL-EGFR-202 是一种有效、不可逆的 EGFR 突变激酶抑制剂（对于耐药突变 EGFR T790M 和 WT EGFR 激酶，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).(In Vitro):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).

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, G719C/S, L858R, L858R/T790M, L861Q, 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 trongly inhibits BLK, BTK, ERBB2 and ERBB4 with IC50s of 8.1 nM, 24.5 nM, 8.1 nM and 3.2 nM, respectively.CHMFL-EGFR-202 moderately inhibits BMX and MEK1 kinases with IC50 of 111.0 nM and 161.0 nM.

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Angiogenesis

EGFR

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2089381-40-6

489.96

C25H24ClN7O2

>98% (HPLC)

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Nc1ncnc2n(nc(-c3ccc(OCc4ccccn4)c(Cl)c3)c12)[C@@H]1CCCN(C1)C(=O)C=C

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(-20℃)

With Ice Pack

≥ 2 years