| Identification | Back Directory | [Name]
BMS-690514 | [CAS]
859853-30-8 | [Synonyms]
CS-472
BMS-690514
BMS-6690514
BMS690514/BMS-690514
BMS-690514(BMS-6690514)
(3R,4R)-4-Amino-1-[[4-[(3...
(3R,4R)-4-Amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo-[2,1-f][1,2,4]triazin-5-yl]methyl]piperi
(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]piperidin
(3R,4R)-4-Amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol
3-Piperidinol, 4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]-, (3R,4R)- | [EINECS(EC#)]
200-528-9 | [Molecular Formula]
C19H24N6O2 | [MDL Number]
MFCD18633295 | [MOL File]
859853-30-8.mol | [Molecular Weight]
368.43 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
NCE Biomedical Co.,Ltd.
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| Tel: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
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