现货,Vatalanib (PTK787),CAS号212141-51-0,美国进口,:受体酪氨酸激酶(RTK), VEGFR ,VEGFR 抑制剂和化合物,selleck,S1101

信号转导通路: 受体酪氨酸激酶(RTK) >> VEGFR >> VEGFR 抑制剂 >> Vatalanib dihydrochloride (PTK787)http://www.selleck.cn/vatalanib-S1101.html

技术数据:

分子量(MW): 419.73

化学式:

C20H15ClN4•2HCl

 

溶解度: DMSO ≥28mg/mL Water ≥10mg/mL Ethanol ≥6mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 212141-51-0

生物活性

 

 

Vatalanib dihydrochloride (PTK787) is a novel VEGFR and c-Kit tyrosine kinases and angiogenesis inhibitor with IC50 of 0.037, 0.077, 0.27 and 0.73 μM for KDR, Flt-1, Flk and c-Kit, respectively. Measurement of VEGF-induced autophosphorylation of KDR in a double antibody chemiluminescence assay, using either HUVECs or CHO cells transfected with the KDR receptor, showed that vatalanib dihydrochloride (PTK787) inhibits the VEGF-induced phosphorylation with an IC50 of 17 and 34 nM for the HUVECs and CHO cells , respectively. Selective inhibition of VEGFRs by vatalanib dihydrochloride (PTK787)leads to inhibition of primary tumor growth and development of metastases in murine renal cell carcinoma. Vatalanib dihydrochloride (PTK787) caused no obvious side effects in the RENCA model . Vatalanib dihydrochloride (PTK787) causes significant anti-arthritic effects in models of rheumatoid arthritis. [1][2][3]

 

 

 

参考文献

PTK787/ZK 222584, a Novel and Potent Inhibitor of Vascular Impairs Endothelial Growth Factor Receptor Tyrosine Kinases,Vascular Endothelial Growth Factor-induced Responses and Tumor Growth after Oral Administration Guido Bold, Elizabeth Buchdunger, et al. Cancer Res 2000;60:2178-2189

Effects of PTK787/ZK 222584, a Specific Inhibitor of Vascular Endothelial Growth Factor Receptor Tyrosine Kinases, on Primary Tumor, Metastasis, Vessel Density, and Blood Flow in a Murine Renal Cell Carcinoma Model Joachim Drevs, Inga Hofmann,et al. Cancer Res 2000;60:4819-4824

Angiogenesis inhibition by the novel VEGF receptor tyrosine kinase inhibitor, PTK787/ZK222584, causes significant anti-arthritic effects in models of rheumatoid arthritis K. Grosios,J.Wood,et al. Inflamm. res 2004;53:133–142

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