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Motesanib Diphosphate

Motesanib Diphosphate (AMG 706) 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。

CAS号

857876-30-3

分子式

C22H23N5O·2H3PO4

主要靶点

VEGFR|c-Kit

仅限科研使用

Cat No : CM06858

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Synonyms

二磷酸莫替沙尼|AMG 706|Motesanib

验证数据展示

  • CAS No.: 857876-30-3

    Motesanib Diphosphate
    CAS#: 857876-30-3

产品信息

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

CAS号 857876-30-3
分子式 C22H23N5O·2H3PO4
主要靶点 VEGFR|c-Kit
主要通路 蛋白酪氨酸激酶|血管生成
分子量 569.44
纯度 99.76%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 二磷酸莫替沙尼|AMG 706|Motesanib

靶点活性

Kit:8 nM|VEGFR2/Flk1:6 nM|VEGFR1:2 nM|VEGFR2:3 nM|VEGFR3:6 nM

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。

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.

溶解度

DMSO:93 mg/mL (163.3 mM),H2O:16 mg/mL (28.1 mM),Ethanol:<1 mg/mL

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)

参考文献

1.Polverino A, et al. Cancer Res, 2006, 66(17), 8715-8721.
2.Kruser TJ, et al. Clin Cancer Res, 2010, 16(14), 3639-3647.
3.Coxon A, et al. Clin Cancer Res, 2009, 15(1), 110-118.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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C1   V1   C2   V2