Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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1 mg | 在庫あり | ¥ 19,000 | |||
5 mg | 在庫あり | ¥ 45,500 | |||
10 mg | 在庫あり | ¥ 74,000 | |||
25 mg | 在庫あり | ¥ 125,500 | |||
50 mg | 在庫あり | ¥ 181,000 | |||
100 mg | 在庫あり | ¥ 248,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 52,000 |
説明 | 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. |
ターゲット&IC50 | PDGFRα:1 nM, FLK1:8 nM, FLT4:9 nM, KDR:7 nM |
In vitro | 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]. |
In vivo | 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 |
分子量 | 435.47 |
分子式 | C27H21N3O3 |
CAS No. | 1256349-48-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (137.78 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Chiauranib 1256349-48-0 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic Tyrosine Kinase/Adaptors c-Fms VEGFR FLT PDGFR c-Kit Aurora Kinase CSF-1R VEGFR2 CSF1R Vascular endothelial growth factor receptor VEGFR3 anti-angiogenesis CD117 CS-2164 CSF-1 receptor colony stimulating factor 1 receptor PDGFRα Aurora-B anticancer inhibit SCFR Inhibitor CS2164 Platelet-derived growth factor receptor CS 2164 VEGFR1 inhibitor