Tivozanib
作者：齐岳
发布时间：2023-08-25
09:00:16
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产品名称：Tivozanib
产品描述：
| 产品描述 | Tivozanib 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 | KRN951, AV-951, 替沃扎尼 |
| 分子量 | 454.87 |
| 分子式 | C22H19ClN4O5 |
| CAS No. | 475108-18-0 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: <1 mg/mL
DMSO: 16 mg/mL (35.2 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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