BMS-690514
作者：齐岳
发布时间：2023-08-23
09:21:39
点击数：
产品名称：BMS-690514
产品描述：
| 产品描述 | BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR. Ithas IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively. |
| 靶点活性 | EGFR:5 nM, HER2:20 nM, HER4:60 nM |
| 体外活性 | 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. |
| 体内活性 | 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. |
| 分子量 | 368.43 |
| 分子式 | C19H24N6O2 |
| CAS No. | 859853-30-8 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 24 mg/mL (65.14 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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