现货,Vatalanib dihydrochloride,selleck,VEGFR 抑制
产品报价:1323元
更新时间:2012/7/26 10:29:06
产地:美国
品牌:selleck
型号: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
潘贺华 : (13926198506) (400-168-1698)
(联系我时,请说明是在来宝网上看到的,谢谢!)产品报价:1323元
更新时间:2012/7/26 10:29:06
产地:美国
品牌:selleck
型号: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
潘贺华 : (13926198506) (400-168-1698)
(联系我时,请说明是在来宝网上看到的,谢谢!)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 |
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]
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). | |
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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