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BMS-690514

Catalog No. T14677   CAS 859853-30-8
Synonyms: inhibit, ErbB-1, BMS690514, Vascular endothelial growth factor receptor, Epidermal growth factor receptor, Inhibitor, EGFR, BMS 690514, VEGFR, BMS-690514, HER1

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

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BMS-690514, CAS 859853-30-8
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR. It has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.
Targets&IC50 EGFR:5 nM, HER4:60 nM, HER2:20 nM
In vitro BMS-690514 inhibits members of the VEGFR family with IC50 values in the range of 25 to 50 nM. BMS-690514 targets several critical signaling pathways: human epidermal growth factor receptor (HER)/ErbB, angiogenesis signaling through VEGFR2, lymphangiogenesis through VEGFR3, respectively. It also shows activity against VEGFR1, Flt-3, and Lck. Permeability of BMS-690514 in Caco-2 cells is in the intermediate range with a moderate potential to be a P-gp substrate[2]. Non–small cell lung tumor cells with exon 19 deletion (HCC4006, HCC827, and PC9) are highly sensitive to BMS-690514, which inhibits their proliferation with IC50 values of 2 to 35 nM. Tumor cell lines with EGFR gene amplification (DiFi, NCI-H2073, A431) are also highly sensitive to inhibition by BMS-690514. Breast and gastric tumor cell lines that have HER2 gene amplification (N87, SNU-216, AU565, BT474, KPL4, and HCC202) are inhibited with IC50 values of 20 to 60 nM[1]. Tumor cell lines that are dependent on HER2 signaling are also found to be highly sensitive to BMS-690514.
In vivo BMS-690514 can cross the blood–brain barrier with a brain-to-plasma ratio of 1. 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 preclinical ADME properties of BMS-690514 suggest good oral bioavailability in humans and metabolism by multiple pathways including oxidation and glucuronidation[2]. The oral bioavailability of BMS-690514 is 78% in mice, 100% in rats, 8% in monkeys, and 29% in dogs.
Synonyms inhibit, ErbB-1, BMS690514, Vascular endothelial growth factor receptor, Epidermal growth factor receptor, Inhibitor, EGFR, BMS 690514, VEGFR, BMS-690514, HER1
Molecular Weight 368.43
Formula C19H24N6O2
CAS No. 859853-30-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 24 mg/mL (65.14 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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. 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.

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