替沃扎尼 T2456

Product Introduction
Bioactivity


英文名: Tivozanib

描述: 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。

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

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 16 mg/mL (35.2 mM)


关键字: VEGFR | antitumor | vascular permeability | renal cell carcinoma | AV951 | angiogenesis | AV 951 | Inhibitor | Tivozanib | Vascular endothelial growth factor receptor | KRN 951 | orally active | inhibit | KRN-951

相关产品: Cediranib | AMG-47a | Dovitinib | Ningetinib Tosylate | AST 487 | Sorafenib tosylate | N-Desethyl Sunitinib | Chiauranib | VEGFR-3-IN-1 | AMPK-IN-3

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library

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