Tivozanib
作者：齊岳
發(fā)布時間：2023-08-25
09:00:16
點擊數(shù)：
產(chǎn)品名稱：Tivozanib
產(chǎn)品描述：
| 產(chǎn)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. |
| 靶點活性 | PDGFRα:40 nM, EphB2:24 nM, VEGFR1:30 nM, VEGFR3:15 nM, VEGFR2:6.5 nM |
| 體外活性 | 在腫瘤異種移植物模型中,口服Tivozanib（1 mg / kg）能夠降低微血管密度并抑制VEGFR2磷酸化水平. |
| 體內(nèi)活性 | 在內(nèi)皮細(xì)胞中（IC 50 = 0.16 nM）,Tivozanib能夠抑制VEGF誘導(dǎo)的VEGFR2磷酸化 |
| 激酶實驗 | 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. |
| 細(xì)胞實驗 | 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) |
| 別名 | KRN951, AV-951, 替沃扎尼 |
| 分子量 | 454.87 |
| 分子式 | C22H19ClN4O5 |
| CAS No. | 475108-18-0 |
存儲
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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公司介紹：
西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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