Description
An EGFR inhibitor (IC50 = 3 nM); selective for EGFR over HER2 (IC50 = 3,400 nM), as well as IGF-1R, β-InsRK, c-Met, c-Src, and VEGFR2 (IC50s = >10 µM); inhibits proliferation and colony formation in A549 cancer cells expressing mutant K-Ras, as well as FaDu cancer cells expressing wild-type K-Ras at 5 µM; enhances radiation-induced cytotoxicity in K-Ras-expressing A549 and MDA-MB-231 cancer cells, but not FaDu, HTB-35, or HH4dd cancer cells that express wild-type K-Ras; reduces tumor growth in A431 and FaDu mouse xenograft models at 70 and 60 mg/kg per day, respectively
Formal name: N8-(3-chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)-pyrimido[5,4-d]pyrimidine-2,8-diamine
Synonyms: BIBX 1382 BS
Molecular weight: 387.8
CAS: 196612-93-8
Purity: ≥98%
Formulation: A crystalline solid
