现货,Motesanib Diphosphate (AMG-706) ,CAS号:857876-30-3,美国进口,受体酪氨酸激酶(RTK) , VEGFR , VEGFR 抑制剂,selleck,S1032

信号转导通路: 受体酪氨酸激酶(RTK) >> VEGFR >> VEGFR 抑制剂 >> Motesanib Diphosphate (AMG-706)http://selleck.cn/motesanib-diphosphate-S1032.html

技术数据:

分子量(MW): 569.44

化学式:

C22H23N5O.2H3PO4

 

溶解度: DMSO ≥114mg/mL Water ≥114mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 857876-30-3

生物活性

 

 

Motesanib (AMG-706) is an orally bioavailable diphosphate salt of a multiple receptor tyrosine kinase inhibitor with potential antineoplastic activity[1]. This reagent selectively targets and inhibits VEGFR1/2/3(IC50: 2 nM /3 nM /6 nM), PDGFR (84nM), kit (8nM), and Ret (59nM)receptors, thereby inhibiting angiogenesis and cellular proliferation. Oral administration of AMG 706 potently inhibited VEGF-induced angiogenesis in the rat corneal model and induced regression of established A431 xenografts [1] .This compound also performed antitumor activity in breast cancer xenografts and was currently being studied in clinical trials for the treatment of thyroid cancer and other advanced solid tumors[2,3,4]

 

 

 

 

参考文献

AMG 706, an Oral, Multikinase Inhibitor that Selectively Targets Vascular Endothelial Growth Factor,Platelet-Derived Growth Factor, and Kit Receptors, Potently Inhibits Angiogenesis and Induces Regression in Tumor Xenografts Angela Coxon, Charlie Starnes, et al. Cancer Res 2006;66:8715-8721

Broad Antitumor Activity in Breast Cancer Xenografts by Motesanib, a Highly Selective, Oral Inhibitor of Vascular Endothelial Growth Factor, Platelet-Derived Growth Factor,and Kit Receptors Tammy Bush, Douglas Saffran, et al. Clin Cancer Res 2009;15:110-118

Motesanib Diphosphate in Progressive Differentiated Thyroid Cancer Steven I. Sherman, Lori J. Wirth,et al. N Engl J Med 2008;359:31-42

Safety, Pharmacokinetics, and Efficacy of AMG 706, an Oral Multikinase Inhibitor, in PatientsWith Advanced Solid Tumors Lee S. Rosen, Razelle Kurzrock,et al. J Clin Oncol 2007;25:2369-2376.

 

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