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Motesanib Diphosphate
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。
CAS NO:857876-30-3
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
AMG 706
Motesanib
二磷酸莫替沙尼
产品介绍
Motesanib Diphosphate 是一种有效的VEGFR1/2/3的 ATP 竞争性抑制剂,IC50值为 2 nM/3 nM/6 nM,与对 Kit 的选择性相似,是 PDGFR 和 Ret 的 10 倍多。

产品描述

Motesanib Diphosphate is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity.

体外活性

在大鼠角膜模型中,每天口服两次(ED50=2.1 mg/kg )或一次(ED50=4.9 mg/kg )Motesanib Diphosphate能够抑制血管内皮生长因子诱导的血管生成.在头部和颈部鳞状细胞癌移植瘤模型中,Motesanib Diphosphate和辐射治疗联用,显示出显著地抗癌活性.

体内活性

在VEGF诱导的HUVECs细胞中(IC50 =10 nM),Motesanib Diphosphate 明显抑制细胞增殖。对于血小板衍生因子诱导的增殖(IC50=207 nM)和SCF诱导的c-kit磷酸化(IC50=37 nM),Motesanib Diphosphate能够显著抑制。人脐静脉内皮细胞,Motesanib Diphosphate增强细胞对于放射性的敏感程度。对人VEGFR家族,Motesanib Diphosphate具有广谱活性。

激酶实验

In vitro kinase assays: Optimal enzyme, ATP, and substrate (gastrin peptide) concentrations are established for each enzyme using homogeneous time-resolved fluorescence (HTRF) assays. Motesanib Diphosphate is tested in a 10-point dose-response curve for each enzyme using an ATP concentration of two-thirds Km for each. Most assays consist of enzyme mixed with kinase reaction buffer [20 mM Tris-HCl (pH 7.5), 10 mM MgCl2, 5 mM MnCl2, 100 mM NaCl, 1.5 mM EGTA]. A final concentration of 1 mM DTT, 0.2 mM NaVO4, and 20 μg/mL BSA is added before each assay. For all assays, 5.75 mg/mL streptavidin-allophycocyanin and 0.1125 nM Eu-PT66 are added immediately before the HTRF reaction. Plates are incubated for 30 minutes at room temperature and read on a Discovery instrument. IC50 values are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equation.

细胞实验

Cells are preincubated for 2 hours with different concentrations of Motesanib Diphosphate, and exposed with 50 ng/mL VEGF or 20 ng/mL bFGF for an additional 72 hours. Cells are washed twice with DPBS, and plates are frozen at -70 °C for 24 hours. Proliferation is assessed by the addition of CyQuant dye, and plates are read on a Victor 1420 workstation. IC50 data are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equatio(Only for Reference)

Cas No.

857876-30-3

分子式

C22H23N5O·2H3PO4

分子量

569.44

别名

AMG 706;Motesanib;二磷酸莫替沙尼

储存和溶解度

Ethanol:<1 mgml
H2O:16 mg/mL (28.1 mM)
DMSO:93 mg/mL (163.3 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years