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BMS-690514
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS-690514图片
CAS NO:859853-30-8
包装与价格:
包装价格(元)
1 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
BMS-690514是可口服的EGFR和VEGFR抑制剂,对于EGFR、HER2和HER4的IC50值分别为5、9 和 60 nM。

产品描述

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.

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.

Cas No.

859853-30-8

分子式

C19H24N6O2

分子量

368.43

储存和溶解度

DMSO:24 mg/mL (65.14 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years