CHMFL-EGFR-202
Product Specifications
UNSPSC 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].
Target Antigen
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 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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, protect from light, stored under nitrogen)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-101522/CHMFL-EGFR-202-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-101522/CHMFL-EGFR-202-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
2089381-40-6
Available Sizes
Curated Selection
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