EGFR-IN-99 |CAS 2068806-31-3|DC Chemicals

Cas No.:	2068806-31-3
Chemical Name:	EGFR-HER2 Ex20Ins inhibitor 1a
Synonyms:	C(C=C)(=O)NC=1C=C(C=CC=1)N(C(OCC1=CC=C(C=C1)F)=O)C1=NC(=NC=C1)NC=1C=NN(C=1)C;EGFR-HER2 Ex20Ins inhibitor 1a
SMILES:	FC1C=CC(=CC=1)COC(N(C1C=CN=C(NC2C=NN(C)C=2)N=1)C1C=CC=C(C=1)NC(C=C)=O)=O
Formula:	C₂₅H₂₂FN₇O₃
M.Wt:	487.485687732697
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

EGFR-HER2 Ex20Ins inhibitor 1a is a highly potent, broadly effective EGFR and HER2 Exon 20 insertion mutant inhibitor with biochemical IC50 of <0.5 nM (wtEGFR, 100 uM ATP); exhibits superior inhibition of proliferation and signaling pathways in Ba/F3 cells harboring either EGFR or HER2 Ex20Ins mutations (IC50=7.5-35 nM), and in the EGFR P772_H773insPNP patient-derived lung cancer cell line DFCI127 compared with afatini; induces a dose-dependent reduction of EGFR and Erk phosphorylation in EGFR InsSVD transformed Ba/F3 cells with strong inhibition at 0.1 uM; displays broad and superior antiproliferative activities against EGFR and HER2 Ex20Ins mutants than currently approved 2nd and 3rd generation irreversible EGFR inhibitors.

MSDS

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2018-0101

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