CHMFL-EGFR-202

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].

Product Specifications

CAS Number

[2089381-40-6]

UNSPSC

12352005

Target

BMX Kinase; Btk; EGFR; MEK

Type

Reference compound

Related Pathways

JAK/STAT Signaling; MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/chmfl-egfr-202.html

Purity

99.75

Solubility

DMSO : ≥ 110 mg/mL

Smiles

O=C(N(C1)CCC[C@H]1N2C3=NC=NC(N)=C3C(C4=CC(Cl)=C(OCC5=NC=CC=C5)C=C4)=N2)C=C

Molecular Formula

C25H24ClN7O2

Molecular Weight

489.96

References & Citations

[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.