2089381-40-6

2089381-40-6 structure

Name: CHMFL-EGFR-202
Chemical Name: CHMFL-EGFR-202
CAS Number: 2089381-40-6
Molecular Formula: C₂₅H₂₄ClN₇O₂
Molecular Weight: 489.96
Catalog: Signaling Pathways JAK/STAT Signaling EGFR
Create Date: 2019-08-04 02:31:58
Modify Date: 2024-01-09 10:24:55
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].

Name	CHMFL-EGFR-202

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> EGFR Signaling Pathways >> MAPK/ERK Pathway >> MEK Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> BMX Kinase Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk
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)
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].
References	[1]. Wang A, et al. Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.

Molecular Formula	C₂₅H₂₄ClN₇O₂
Molecular Weight	489.96

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