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CHMFL-EGFR-202

CHMFL-EGFR-202

Item no.	HY-101522-1ea
Manufacturer	MedChem Express
CASRN	2089381-40-6
Amount	1 ea
Quantity options	100 mg 10 mM/1 mL 10 mg 1 ea 1 mg 25 mg 50 mg 5 mg
Category	Inhibitors & Compound Libraries Small Molecules
Type	Molecules
Specific against	other
Purity	99.75
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.
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
ECLASS 10.1	32169090
ECLASS 11.0	32169090
UNSPSC	12000000
Shipping Condition	Cool pack
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	Cancer-Kinase/protease
Manufacturer - Targets	BMX Kinase; Btk; EGFR; MEK
Shipping Temperature	Blue Ice
Storage Conditions	-20°C (Powder, protect from light, stored under nitrogen)
Molecular Weight	489.96
Product 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].
Manufacturer - Research Area	Cancer
Solubility	DMSO: ≥ 110 mg/mL
Manufacturer - Pathway	JAK/STAT Signaling; MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK
Isoform	EGFR/ErbB1/HER1; ErbB2/HER2; ErbB4/HER4; MEK1
Clinical information	No Development Reported

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HY-101522-1ea-safety-datasheet.pdf