BMS-599626 (AC480)|1mg|K1291-上海高创化学科技有限公司

SKU:K1291		M. Wt:567.01
Formula:C27H27FN8O3.HCl		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:873837-23-1		Synonyms:N/A
Chemical NameN/A

Description	BMS-599626 (AC480)
Targets	HER1	HER2
IC50	20 nM	30 nM
In vitro	BMS-599626(AC480) inhibited HER1 and HER2 with IC50 of 20 and 30 nM. BMS-599626(AC480) is highly selective against a broad panel of diverse protein kinases. BMS-599626 abrogated HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50 in the range of 0.24 to 1 micromol/L. In tumor cells that are capable of forming HER1/HER2 heterodimers, BMS-599626 inhibited heterodimerization and downstream signaling. BMS-599626(AC480) significantly enhanced the radiosensitivity of HN-5 cells. In HN-5 cells, BMS-599626(AC480) inhibit the expression of pEGFR, pHER2, cyclins D and E, pRb, pAkt, pMAPK, pCDK1 and 2, CDK 6, and Ku70 proteins. BMS-599626(AC480) also induced accumulation of cells in the G1 cell cycle phase, inhibited cell growth, enhanced radiosensitivity, and prolonged the presence of gamma-H2AX foci up to 24 h after radiation.But BMS-599626(AC480) did not increase the percentage of cells undergoing radiation-induced apoptosis.
In vivo	BMS-599626 had antitumor activity in models that overexpress HER1 (GEO), as well as in models that have HER2 gene amplification (KPL4) or overexpression (Sal2), and there was good correlation between the inhibition of receptor signaling and antitumor activity. BMS-599626(AC480) was generally well tolerated, with disease stabilization across a range of tumor types and doses (100-660 mg/day).
Clinical Trials	N/A
Features	N/A

Description

BMS-599626 (AC480)

Targets

HER1

HER2

IC50

20 nM

30 nM

In vitro

BMS-599626(AC480) inhibited HER1 and HER2 with IC50 of 20 and 30 nM. BMS-599626(AC480) is highly selective against a broad panel of diverse protein kinases. BMS-599626 abrogated HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50 in the range of 0.24 to 1 micromol/L. In tumor cells that are capable of forming HER1/HER2 heterodimers, BMS-599626 inhibited heterodimerization and downstream signaling. BMS-599626(AC480) significantly enhanced the radiosensitivity of HN-5 cells. In HN-5 cells, BMS-599626(AC480) inhibit the expression of pEGFR, pHER2, cyclins D and E, pRb, pAkt, pMAPK, pCDK1 and 2, CDK 6, and Ku70 proteins. BMS-599626(AC480) also induced accumulation of cells in the G1 cell cycle phase, inhibited cell growth, enhanced radiosensitivity, and prolonged the presence of gamma-H2AX foci up to 24 h after radiation.But BMS-599626(AC480) did not increase the percentage of cells undergoing radiation-induced apoptosis.

In vivo

BMS-599626 had antitumor activity in models that overexpress HER1 (GEO), as well as in models that have HER2 gene amplification (KPL4) or overexpression (Sal2), and there was good correlation between the inhibition of receptor signaling and antitumor activity. BMS-599626(AC480) was generally well tolerated, with disease stabilization across a range of tumor types and doses (100-660 mg/day).

Clinical Trials

N/A

Features

N/A

工商信息

企业名称

上海高创化学科技有限公司

企业信息已认证

企业类型

信用代码

310228001353263

成立日期

2010-06-05

注册资本

经营范围

从事化学科技、计算机领域内技术开发、技术咨询、技术服务,从事生物科技领域内技术开发、技术咨询,化学试剂、化工原料及产品(除危险化学品、监控化学品、烟花爆竹、民用爆炸物品、易制毒化学品),实验室设备(除医疗器械),仪器仪表,Ⅰ类医疗器械,金属制品,电子产品,机电产品销售。【依法须经批准的项目,经相关部门批准后方可开展经营活动】

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