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现在位置首页>实验室原料试剂耗材>化学试剂>药物标准品>现货,Vatalanib dihydrochloride,selleck,VEGFR 抑制
现货,Vatalanib dihydrochloride,selleck,VEGFR 抑制
现货,Vatalanib dihydrochloride,selleck,VEGFR 抑制
  • 现货,Vatalanib dihydrochloride,selleck,VEGFR 抑制

现货,Vatalanib dihydrochloride,selleck,VEGFR 抑制

产品报价:1323元

更新时间:2012/7/26 10:29:06

地:美国

牌:selleck

号:CAS号: 212141-51-0

厂商性质: 生产型,贸易型,

公司名称: 赛导通生物科技(广州)有限公司

产品关键词:

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S1101 Vatalanib dihydrochloride (PTK787)
信号转导通路:  受体酪氨酸激酶(RTK) >> VEGFR >> VEGFR 抑制剂 >> 

技术数据:

分子量(MW): 419.73 Vatalanib dihydrochloride (PTK787) Chemical Structure
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

客户反馈数据

Vatalanib dihydrochloride (PTK787) Review Mechanisms of VEGF-activated Ca2 entry. All data were from HUVECs. a, Mean 100 ng/mL VEGF-evoked Ca2 entry in the presence of 100 nmol/L sorafenib (n/N3/40), 10 nmol/L vatalanib (n/N=3/24), or 10 mol/L U73122 (n/N=3/24) normalized to their matched controls. b and c, eYFP-STIM1 (green) before (control) (b) and after exposure to 100 ng/mL VEGF (c). d, Summary data for 100 ng/mL VEGF-evoked transient and sustained Ca2 signals after transfection with STIM1.si or sc.si (n/N3/64). e, Example merged image of a cell labeled with anti-VEGFR2 antibody (green), anti-Orai1 antibody (red), and the nuclear counter stain, DAPI (blue).
Vatalanib dihydrochloride (PTK787) Review Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.
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