MGCD-265

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MGCD-265

品牌： Absin

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参数

分子式：

C₂₆H₂₀FN₅O₂S₂

分子量：

517.6

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产品介绍

产品信息

抗原名称

Met,RON,VEGFR1,VEGFR2,VEGFR3,,

商品描述

MGCD-265是一种有效的，多靶点，及ATP竞争性的c-Met和VEGFR1/2/3抑制剂，IC50分别为1 nM， 3 nM/3 nM/4 nM，也抑制Ron和Tie2。MGCD-265是多靶点受体酪氨酸激酶抑制剂。MGCD-265有效抑制 Met, Met^Y1235D, Met^M1250T, VEGFR1, VEGF2, VEGF3, Ron, 和Tie2, IC50为 1 nM到7 nM。MGCD-265 作用于c-Met驱动的肿瘤细胞 (MKN45, MNNG-HOS, 和SNU-5)和非c-Met-驱动的肿瘤细胞(HCT116和MDA-MB-231)，抑制细胞增殖，IC50分别为6 nM-30 nM 和1 μM-3 μM。

分子量

517.6

纯度

98%

可溶性

DMSO ：96 mg/mL (185.5 mM)

In vitro(体外研究)

MGCD-265 is a multi-target inhibitor of receptor tyrosine kinases. MGCD-265 potently inhibits Met, MetY1235D, MetM1250T, VEGFR1, VEGF2, VEGF3, Ron, and Tie2, with IC50 values ranging from 1 nM to 7 nM. MGCD-265 inhibits cell proliferation both in c-Met-driven tumor cells (MKN45, MNNG-HOS, and SNU-5) and in non-c-Met-driven tumor cells (HCT116 and MDA-MB-231), with IC50 values of 6 nM–30 nM and 1 μM–3 μM, respectively. In serum starved MKN45 cells, MGCD-265 (40 nM–5 μM) effectively inhibits c-Met phosphorylation and its downstream signaling pathways, including Erk, Akt, Stat3, and Fak. MGCD-265 (6 nM–1 μM) also induces apoptosis in MKN45 cells.

In vivo(体内研究)

In c-Met-driven or non-c-Met-driven mice xenograft models of MKN45, U87MG, MDA-MB-231, COLO205, and A549 tumor cells, MGCD-265 (20 mg/kg–60 mg/kg) inhibits tumor growth and c-Met signaling. MGCD-265 (40 mg/kg) also downregulates genes involved in angiogenesis, including VEGF and IL-8, both in tumor and plasma of mice with U87MG xenograft. MGCD-265 also inhibits the plasma level of shed-Met.

背景

别名

MGCD 265

分子式

C₂₆H₂₀FN₅O₂S₂

CAS号

875337-44-3

制备和贮存

保存方式

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

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货号：

abs813281-10mg

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