BMS-690514

Product NameBMS-690514
CAS859853-30-8
MFC19H24N6O2
MW368.43
EINECS200-528-9
MOL File859853-30-8.mol

Chemical Properties

Density	1.41
storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	Powder
pka	14.41±0.40(Predicted)
color	White to off-white

Usage And Synthesis

Uses

BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.

in vivo

BMS-690514 has been shown to be efficacious in a broad spectrum of tumor xenografts. At doses that are efficacious and well tolerated in the animal models, BMS-690514 inhibits tumor cell proliferation and tumor blood flow^[1]. The oral bioavailability of BMS-690514 is 78% in mice, 100% in rats, 8% in monkeys, and 29% in dogs. BMS-690514 is able to cross the blood–brain barrier with a brain-to-plasma ratio of 1. The preclinical ADME properties of BMS-690514 suggest good oral bioavailability in humans and metabolism by multiple pathways including oxidation and glucuronidation^[2].

IC 50

EGFR: 5 nM (IC₅₀); HER2: 20 nM (IC₅₀); HER4: 60 nM (IC₅₀); VEGFR1; VEGFR2; VEGFR3

References

[1] Wong TW, et al. Antitumor and antiangiogenic activities of BMS-690514, an inhibitor of human EGF and VEGF receptor kinase families. Clin Cancer Res. 2011 Jun 15;17(12):4031-41. DOI:10.1158/1078-0432.CCR-10-3417
[2] Marathe P, et al. Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93. DOI:10.1002/jps.22099