CHMFL-EGFR-202,2089381-40-6

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CHMFL-EGFR-202

CAS No. : 2089381-40-6

MCE 国际站：CHMFL-EGFR-202

产品活性：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。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK  |  MAPK/ERK Pathway

作用靶点：EGFR  |  BMX Kinase  |  Btk  |  MEK

In Vitro: 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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