Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tivozanib (KRN951) 是一种选择性的 VEGFR 1/2/3抑制剂,它们的 IC50值分别为0.21 nM、0.16 nM、0.24 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 237 | 现货 | ||
2 mg | ¥ 329 | 现货 | ||
5 mg | ¥ 533 | 现货 | ||
10 mg | ¥ 825 | 现货 | ||
25 mg | ¥ 1,490 | 现货 | ||
50 mg | ¥ 2,560 | 现货 | ||
100 mg | ¥ 3,790 | 现货 | ||
200 mg | ¥ 5,470 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 588 | 现货 |
产品描述 | Tivozanib (KRN951) is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities. |
靶点活性 | PDGFRα:40 nM, EphB2:24 nM, VEGFR1:30 nM, VEGFR3:15 nM, VEGFR2:6.5 nM |
体外活性 | 在肿瘤异种移植物模型中,口服Tivozanib(1 mg / kg)能够降低微血管密度并抑制VEGFR2磷酸化水平. |
体内活性 | 在内皮细胞中(IC 50 = 0.16 nM),Tivozanib能够抑制VEGF诱导的VEGFR2磷酸化 |
激酶实验 | Kinase Assays: Cell-free kinase assays are done in quadruplicate with 1 μM ATP to determine the IC50 values of AV-951 against a variety of recombinant receptor and nonreceptor tyrosine kinases including VEGFR1, VEGFR2, VEGFR3, c-Kit, PDGFRβ, Flt-3 and FGFR1. |
细胞实验 | Human umbilical vein endothelial cells (HUVEC) and normal human dermal fibroblasts-based assays are done to determine the ability of AV-951 to inhibit ligand-dependent phosphorylation of tyrosine kinase receptors. The cells are starved overnight in appropriate basic medium containing 0.5% fetal bovine serum (FBS). The cells are incubated for 1 hour following the addition of AV-951 or 0.1% DMSO, and then stimulated with the cognate ligand at 37 °C. Receptor phosphorylation is induced for 5 minutes except for VEGFR3 (10 minutes), c-Met (10 minutes), and c-Kit (15 minutes). All the ligands used in the assays are human recombinant proteins, except for VEGF-C, a rat recombinant protein. Following cell lysis, receptors are immunoprecipitated with appropriate antibodies and subjected to immunoblotting with phosphotyrosine. Quantification of the blots and calculation of IC50 values are carried ou(Only for Reference) |
别名 | 替沃扎尼, AV-951, KRN951 |
分子量 | 454.86 |
分子式 | C22H19ClN4O5 |
CAS No. | 475108-18-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 16 mg/mL (35.2 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1985 mL | 10.9924 mL | 21.9848 mL | 54.962 mL |
5 mM | 0.4397 mL | 2.1985 mL | 4.397 mL | 10.9924 mL | |
10 mM | 0.2198 mL | 1.0992 mL | 2.1985 mL | 5.4962 mL | |
20 mM | 0.1099 mL | 0.5496 mL | 1.0992 mL | 2.7481 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。
Tivozanib 475108-18-0 Angiogenesis Tyrosine Kinase/Adaptors VEGFR PDGFR Ephrin Receptor antitumor vascular permeability renal cell carcinoma 替沃扎尼 AV951 AV-951 angiogenesis AV 951 Inhibitor Vascular endothelial growth factor receptor KRN951 KRN 951 orally active inhibit KRN-951 inhibitor