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Description: AC480 (also known as BMS-599626) is a novel, potent, orally bioavailable, selective and efficacious inhibitor of HER1/2 (human epidermal growth factor receptors) with potential anticancer activity. It inhibits HER1/2 with IC50s of 20 nM and 30 nM, respectively. It shows ca.8-fold less potency against HER4, and is > 100-fold less active to VEGFR2, c-Kit, Lck, MET etc. Oral administration of AC480 has been demonstrated to suppress the growth of Sal2 tumor, GEO xenograft tumor, KPL-4 and BT474 breast tumors, N87 gastric tumor, A549 and L2987 non–small-cell lung tumors in nude mice.
References: Clin Cancer Res. 2006 Oct 15; 12(20 Pt 1):6186-93; Invest New Drugs. 2011 Aug; 29(4):554-61.
Related CAS: 714971-09-2 (free base); 873837-23-1 (HCl salt)
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