Chiauranib
作者：齊岳
發布時間：2023-08-23
09:20:18
點擊數：
產品名稱：Chiauranib
產品描述：
| 產品描述 | Chiauranib is a multi-target inhibitor against tumor angiogenesis and exhibits potent anticancer effects. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF1R, with IC50 values ranging from 1-9 nM. |
| 靶點活性 | KDR:7 nM, Flt4:9 nM, Flt1:8 nM, PDGFRα:1 nM |
| 體外活性 | In HUVEC and PDGFRβ phosphorylation in PDGFRβ overexpressed NIH3T3 cells, Chiauranib (CS2164; 0.03-3 μM) suppressed VEGFR/PDGFR phosphorylation, inhibited ligand-dependent cell proliferation, and capillary tube formation, and prevented vasculature formation in tumor tissues. Chiauranib (CS2164) inhibited CSF-1R phosphorylation that lead to the suppression of ligand-stimulated monocyte-to-macrophage differentiation and reduced CSF-1R+ cells in tumor tissues. Chiauranib (3 μM; 24 hours) showed induction of G2/M cell cycle arrest and suppression of cell proliferation in tumor tissues through the inhibition of Aurora B-mediated H3 phosphorylation[1]. |
| 體內活性 | Chiauranib exhibited broad and potent anti-tumor activities in vivo. Chiauranib (2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg; oral) induced remarkable regression or complete inhibition of tumor growth at well-tolerated oral doses in several human tumor xenograft models[1]. |
| 別名 | CS2164, 西奧羅尼 |
| 分子量 | 435.47 |
| 分子式 | C27H21N3O3 |
| CAS No. | 1256349-48-0 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 60 mg/mL (137.78 mM),Need ultrasonic
( < 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科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
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