EAI045

DESCRIPTION

A potent inhibitor of mutant EGFRs (IC50s = 0.076, 0.049, 0.002, and 1.6 μM for recombinant EGFRL858R, EGFRT790M, EGFRL858R/T790M, and wild-type EGFR, respectively); inhibits phosphorylation of EGFR in a concentration-dependent manner in H1975 cells; reduces proliferation of Ba/F3 cells expressing EGFRL858R/T790M and EGFRL858R/T790M/I941R from 0.01-10 μM; induces tumor regression and reduces EGFR signaling in mice bearing EGFRL858R/T790M, EGFRExon19del/T790M, and EGFRL858R/T790M/C797S tumors at 60 mg/kg/day with cetuximab

DETAILS

Inchi: InChI=1S/C19H14FN3O3S/c20-12-5-6-15(24)14(9-12)16(17(25)22-19-21-7-8-27-19)23-10-11-3-1-2-4-13(11)18(23)26/h1-9,16,24H,10H2,(H,21,22,25)
Purity: ≥98%
Raptas: Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling
Smiles: FC1=CC=C(C(C(N2CC(C=CC=C3)=C3C2=O)C(NC4=NC=CS4)=O)=C1)O
Inchikey: YTUFHOKUFOQRDF-UHFFFAOYSA-N
Cas Number: 1942114-09-1
Formulation: A crystalline solid
Storage Temp: -20
Shipping Temp: -20
Formula Markup: C19H14FN3O3S
Formula Weight: 383.4
Shelf Life Days: 1460