Amuvatinib (MP-470)|2mg|K1295-上海高创化学科技有限公司

SKU:K1295		M. Wt:447.51
Formula:C23H21N5O3S		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:850879-09-3		Synonyms:N/A
Chemical NameN/A

Description	Amuvatinib (MP-470)
Targets	c-Kit	PDGF-alpha	Flt3
IC50	10 nM	40 nM	81 nM
In vitro	MP470 exhibits low microM IC50 in prostate cancer cell lines. MP470 in combination with Erlotinib shows additive effects on both cytotoxicity and induction of apoptosis. MP470 reduced c-Met phosphorylation and enhanced radiation-induced cell kill by 0.4 logs in SF767 cells. MP470 was shown to inhibit dsDNA break repair and increase apoptosis. MP470 influences various survival and DNA repair related proteins such as pAKT, RAD51 and GSK3beta. Amuvatinib shows in vitro inhibitory activity against multiple human tyrosine kinases including mutant KIT and PDGFRalpha. Amuvaninib inhibited RAD51 protein expression and HR, which is associated with reduced ribosomal protein S6 phosphorylation and inhibition of global translation. Amuvatinib can sensitize cells to IR and MMC, agents that are selectively toxic to HR-deficient cells.
In vivo	In vivo, the addition of MP470 to radiation resulted in a tumor-growth-delay enhancement ratio of 2.9 over radiation alone and extended survival time. In human xenograft models in mice, amuvatinib is active as a DNA repair protein Rad51 inhibitor.The amuvatinib DPC formulation was well tolerated up to 1,500 mg/day. While exposures were low and variable, a transient response in a refractory GIST patient warrants further investigation into single-agent amuvatinib in refractory GIST. MP470 (Amuvatinib) can Downregulate and reverse EMT in mesenchymal normal human mammary epithelial cells and murine BCSCs attenuating self-renewal and restored chemosensitivity of the BCSCs.
Clinical Trials	N/A
Features	N/A

Description

Amuvatinib (MP-470)

Targets

c-Kit

PDGF-alpha

Flt3

IC50

10 nM

40 nM

81 nM

In vitro

MP470 exhibits low microM IC50 in prostate cancer cell lines. MP470 in combination with Erlotinib shows additive effects on both cytotoxicity and induction of apoptosis. MP470 reduced c-Met phosphorylation and enhanced radiation-induced cell kill by 0.4 logs in SF767 cells. MP470 was shown to inhibit dsDNA break repair and increase apoptosis. MP470 influences various survival and DNA repair related proteins such as pAKT, RAD51 and GSK3beta. Amuvatinib shows in vitro inhibitory activity against multiple human tyrosine kinases including mutant KIT and PDGFRalpha. Amuvaninib inhibited RAD51 protein expression and HR, which is associated with reduced ribosomal protein S6 phosphorylation and inhibition of global translation. Amuvatinib can sensitize cells to IR and MMC, agents that are selectively toxic to HR-deficient cells.

In vivo

In vivo, the addition of MP470 to radiation resulted in a tumor-growth-delay enhancement ratio of 2.9 over radiation alone and extended survival time. In human xenograft models in mice, amuvatinib is active as a DNA repair protein Rad51 inhibitor.The amuvatinib DPC formulation was well tolerated up to 1,500 mg/day. While exposures were low and variable, a transient response in a refractory GIST patient warrants further investigation into single-agent amuvatinib in refractory GIST. MP470 (Amuvatinib) can Downregulate and reverse EMT in mesenchymal normal human mammary epithelial cells and murine BCSCs attenuating self-renewal and restored chemosensitivity of the BCSCs.

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】

Amuvatinib (MP-470)由上海高创化学科技有限公司为您提供，货号K1295，规格：2mg，CAS号：，如您想了解更多关于Amuvatinib (MP-470)价格、Amuvatinib (MP-470)结构式、批发、用途等信息，欢迎咨询。除供应Amuvatinib (MP-470)外，还可为您提供JNJ-7706621（细胞周期蛋白依赖激酶抑制剂）、WZ4002（表皮生长因子受体抑制剂）、SNS-314（极光激酶抑制剂）等试剂，公司有专业的客户服务团队，是您值得信赖的合作伙伴，上海高创客户服务电话，售前、售后均可联系。