1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
    MAPK/ERK Pathway
  2. EGFR
    BMX Kinase
    Btk
    MEK
  3. CHMFL-EGFR-202

CHMFL-EGFR-202 

目录号: HY-101522
产品使用指南

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。

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CHMFL-EGFR-202 Chemical Structure

CHMFL-EGFR-202 Chemical Structure

CAS No. : 2089381-40-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ∼10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (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 IC50 of 111.0 nM and 161.0 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

489.96

Formula

C25H24ClN7O2

CAS 号
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.

参考文献
  • 摩尔计算器

  • 稀释计算器

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产品名称:
CHMFL-EGFR-202
目录号:
HY-101522
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