Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pazopanib Hydrochloride (Votrient HCl) 是一种多靶点抑制剂,抑制 VEGFR1、VEGFR2、VEGFR3、PDGFRβ、c-Kit、FGFR1和c-Fms 的IC50分别为10、30、47、84、74、140和146 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 424 | 现货 | ||
50 mg | ¥ 931 | 现货 | ||
100 mg | ¥ 1,339 | 现货 | ||
200 mg | ¥ 2,263 | 现货 | ||
500 mg | ¥ 3,775 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 298 | 现货 |
产品描述 | Pazopanib Hydrochloride (Votrient HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. |
靶点活性 | VEGFR2:30 nM, FGFR:74 nM, VEGFR3:47 nM, c-Fms:146 nM, VEGFR1:10 nM, PDGFR:84 nM, c-Kit:140 nM |
体外活性 | Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM. [1] Pazopanib shows dose-dependent growth inhibition in all synovial sarcoma cell lines including SYO-1 and HS-SY-II cells. Proliferation of SYO-1 and HS-SY-II cells is inhibited even at 1?μg/mL of Pazopanib and is completely abolished at 5?μg/mL. Pazopanib induces G1 arrest, and thereby suppresses the growth of synovial sarcoma cells. Phosphorylation of Akts, GSK-3β, JNKs, p70 S6 Kinase, and mTOR is suppressed in Pazopanib-treated SYO-1 cells compared with that in the vehicle-treated cells. [2] Pazopanib between 20 m g/mL and 22.5 m g/mL shows an increasing reduction of RPE cell viability. [3] |
体内活性 | The mice treated with 30 mg/kg or 100?mg/kg Pazopanib reveals a significant decrease in tumor burden compared with the mice treated with vehicle or 10?mg/kg Pazopanib. Treatment with Pazopanib is well-tolerated and there is no significant difference in the body weight among the mice in each group. [2] |
激酶实验 | Kinase enzyme assays: VEGFR enzyme assays for VEGGR1, VEGFR2, and VEGFR3 are run in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein encoding the catalytic c-terminus of human VEGFR receptor kinases 1, 2, or 3. Reactions are initiated by the addition of 10 μL of activated VEGFR2 kinase solution [final concentration, 1 nM enzyme in 0.1 M HEPES, pH 7.5, containing 0.1 mg/mL bovine serum albumin (BSA), 300 μM dithiothreitol (DTT)] to 10 μL substrate solution [final concentration, 360 nM peptide, (biotin-aminohexyl-EEEEYFELVAKKKK-NH2), 75 μM ATP, 10 μM MgCl2], and 1 μL of titrated Pazopanib in DMSO. Plates are incubated at room temperature for 60 min, and then the reaction is quenched by the addition of 20 μL of 100 mM ethylene diamine tetraacetic acid (EDTA). After quenching, 20 μL HTRF reagents (final concentration, 15 nM Streptavidin-linked allophycocyanin, 1 nM Europium-labeled antiphosphotyrosine antibody diluted in 0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5) is added and the plates incubated for a minimum of 10 min. The fluorescence at 665 nM is measured with a Wallac Victor plate reader using a time delay of 50 μs. |
细胞实验 | Phosphorylation of VEGFR2 is assessed in HUVEC stimulated with VEGF. HUVEC are plated in type-I collagen-coated 10 cm plates in Clonetics EGM-MV medium at 1.0-1.5 × 106 cells/plate. After 24 hours, the confluent cells are serum starved overnight by replacing the growth medium with Clonetics EBM medium containing 0.1% BSA, 500 μg/mL hydrocortisone. Cells are treated with Pazopanib at various concentrations for 1 hour, followed by addition of 10 ng/mL VEGF or vehicle for 10 min. Cells are solubilized in lysis buffer. VEGFR2 is immunoprecipitated using antiflk-1 antibody and analyzed by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) followed by Western blotting and detection with antiflk-1 or with antiphosphotyrosine (anti-P-tyr-biotin) antibody. The VEGFR2 phosphorylation level is quantified by densitometry and normalized to the total VEGFR2 level. (Only for Reference) |
别名 | GW786034, Pazopanib HCl, GW786034 HCl, 盐酸帕唑帕尼, Votrient HCl, Armala |
分子量 | 473.98 |
分子式 | C21H23N7O2S·HCl |
CAS No. | 635702-64-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 7.5 mg/mL (15.82 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1098 mL | 10.549 mL | 21.0979 mL | 52.7448 mL |
5 mM | 0.422 mL | 2.1098 mL | 4.2196 mL | 10.549 mL | |
10 mM | 0.211 mL | 1.0549 mL | 2.1098 mL | 5.2745 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Pazopanib Hydrochloride 635702-64-6 Angiogenesis Autophagy Tyrosine Kinase/Adaptors c-Fms FGFR VEGFR c-Kit PDGFR inhibit CD117 CSF1R Vascular endothelial growth factor receptor colony stimulating factor 1 receptor Platelet-derived growth factor receptor GW 786034 GW786034 CSF-1R Pazopanib HCl SCFR GW-786034 GW786034 HCl Inhibitor Pazopanib 盐酸帕唑帕尼 Votrient HCl Fibroblast growth factor receptor Armala CSF-1 receptor inhibitor