Motesanib (AMG-706)

Motesanib (AMG-706)
分子式: C22H23N5O分子量:373.45

简介: Motesanib (AMG-706)是一种具有口服生物活性的受体酪氨酸激酶 (receptor tyrosine kinase)抑制剂,对VEGFR1, VEGFR2, VEGFR3, Kit, PDGFR和Ret的IC50值分别为2、3、6、8、84和59 nM。 
物理性状及指标: 
外观:……………………粉末 
溶解性:…………………H2O :Insoluble;Ethanol:8 mg/mL (21.42 mM);DMSO: 75 mg/mL (200.83 mM) 
含量:……………………>98% 
储存温度:-20℃,避光防潮密闭干燥

运输条件:2~8℃运输

生物活性

描述

Motesanib (AMG-706)是一种具有口服生物活性的受体酪氨酸激酶 (receptor tyrosine kinase)抑制剂,对VEGFR1, VEGFR2, VEGFR3, Kit, PDGFR和Ret的IC50值分别为2、3、6、8、84和59 nM。

IC50 & Target

VEGFR1  (Cell-free assay)

VEGFR2  (Cell-free assay)

VEGFR3 (Cell-free assay)

c-Kit  (Cell-free assay)

c-Kit  (Cell-free assay)

 

2 nM

3 nM

6 nM

8 nM

8 nM

体外

Motesanib has broad activity against the human VEGFR family, and displays > 1000 selectivity against EGFR, Src, and p38 kinase. Motesanib significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC50 of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC50 of >3,000 nM. Motesanib also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC50 of 207 nM and 37 nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells Althouth displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib treatment significantly sensitizes the cells to fractionated radiation. 

体内

Motesanib (100 mg/kg) significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib twice daily or once daily potently inhibits, in a dose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ED50 of 2.1 mg/kg and 4.9 mg/kg, respectively. Motesanib induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells. Motesanib in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models. Motesanib treatment also induces significant dose-dependent reductions in tumor growth and blood vessel density of MCF-7, MDA-MB-231, or Cal-51 xenografts, which can be markedly enhanced when combined with docetaxel or tamoxifen 

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储液配置及储存: 按表中溶解性配置;如溶解困难,可以通过快速搅拌,超声或温和加热(在45-60°C下水浴)。液体稳定性报道的很少,建议现配现用,如需储存,建议:-20℃1-3月;-80℃ 3-6月。

Motesanib (AMG-706)

1 mg

5 mg

10 mg

1 mM

2.6777 mL

13.3887 mL

26.7773 mL

5 mM

0.5355 mL

2.6777 mL

5.3555 mL

10 mM

0.2678 mL

1.3389 mL

2.6777 mL

50 mM

0.0536 mL

0.2678 mL

0.5355 mL

【注意 】
●我司产品为非无菌包装,若用于细胞培养,请提前做预处理,除去热原细菌,否则会导致染菌。

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CAS 号:453562-69-1
英文名字:Motesanib (AMG-706)
质量标准:>98%,BR
分子式:C22H23N5O
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