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- CAS号：
475108-18-0
- 规格：
1mLx10mM(inDMSO)/1mg/2mg/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥470.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥205.0 |
| 规格： | 2mg | 产品价格： | ￥279.0 |
| 规格： | 5mg | 产品价格： | ￥426.0 |
| 规格： | 10mg | 产品价格： | ￥660.0 |
| 规格： | 25mg | 产品价格： | ￥1192.0 |
| 规格： | 50mg | 产品价格： | ￥2048.0 |
| 规格： | 100mg | 产品价格： | ￥3032.0 |
| 规格： | 200mg | 产品价格： | ￥4376.0 |
Product Introduction
Bioactivity
| 名称 | Tivozanib |
| 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. |
| 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) |
| 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. |
| 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 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+90% Saline : < 3.83 mg/mL (8.42 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.83 mg/mL (8.42 mM), Suspension. DMSO : 38.33 mg/mL (84.27 mM), Sonication is recommended. |
| 关键字 | VEGFR3 | VEGFR2 | VEGFR1 | VEGFR | vascular permeability | Vascular endothelial growth factor receptor | Tivozanib | renal cell carcinoma | PDGFRα | orally active | KRN-951 | KRN 951 | Inhibitor | inhibit | EphrinReceptor | Ephrin Receptor | EphB2 | AV951 | AV 951 | antitumor | angiogenesis |
| 相关产品 | glycine | Ribociclib | Lenvatinib | Chloramphenicol | Thymoquinone | Regorafenib | Pazopanib | Ethyl cinnamate | Sorafenib | Regorafenib monohydrate | Nintedanib esylate | Albendazole |
| 相关库 | Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | EMA Approved Drug Library | Failed Clinical Trials Compound Library | Kinase Inhibitor Library | FDA-Approved Drug Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Tyrosine Kinase Inhibitor Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library |
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替沃扎尼【475108-18-0】
￥205 - 4376
