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BMS-690514

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BMS-690514 Basic information

Product Name:
BMS-690514
Synonyms:
  • BMS-690514
  • (3R,4R)-4-Amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol
  • BMS-6690514
  • (3R,4R)-4-amino-1-[[4-(3-methoxyanilino)pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol
  • (3R,4R)-4-Amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo-[2,1-f][1,2,4]triazin-5-yl]methyl]piperi
  • 3-Piperidinol, 4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]-, (3R,4R)-
  • (3R,4R)-4-Amino-1-[[4-[(3...
  • BMS-690514(BMS-6690514)
CAS:
859853-30-8
MF:
C19H24N6O2
MW:
368.43
EINECS:
200-528-9
Mol File:
859853-30-8.mol
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BMS-690514 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
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BMS-690514 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

BMS-690514Supplier

Shanghai Boyle Chemical Co., Ltd.
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