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Chiauranib
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Chiauranib
CAS No. : 1256349-48-0
MCE 站:Chiauranib
产品活性:Chiauranib (CS2164) 是一种针对肿瘤血管生成的具有口服活性的多靶点抑制剂。Chiauranib 有效抑制血管生成相关激酶 (VEGFR1,VEGFR2,VEGFR3,PDGFRα 和 c-Kit),有丝分裂相关激酶 Aurora B 和慢性炎症相关激酶 CSF-1R,IC50 值为 1-9 nM。Chiauranib 具有很强的抗癌作用。
研究领域:Protein Tyrosine Kinase/RTK | Epigenetics | Cell Cycle/DNA Damage
作用靶点:VEGFR | PDGFR | c-Kit | Aurora Kinase | c-Fms
In Vitro: Chiauranib (CS2164; 3 μM; 24 hours) shows induction of G2/M cell cycle arrest and suppression of cell proliferation in tumor tissues through the inhibition of Aurora B-mediated H3 phosphorylation.
In HUVEC and PDGFRβ phosphorylation in PDGFRβ overexpressed NIH3T3 cells, Chiauranib (CS2164; 0.03-3 μM) displays anti-angiogenic activities through suppression of VEGFR/PDGFR phosphorylation, inhibition of ligand-dependent cell proliferation and capillary tube formation, and prevention of vasculature formation in tumor tissues.
. Chiauranib (CS2164) inhibits CSF-1R phosphorylation that leads to the suppression of ligand-stimulated monocyte-to-macrophage differentiation and reduces CSF-1R+ cells in tumor tissues.
In Vivo: Chiauranib (CS2164; 0.5-40 mg/kg; oral administration; once daily; for 33 days or 43 days) treatment induces remarkable regression or complete inhibition of tumor growth at well-tolerated oral doses in several human tumor xenograft models. Chiauranib exhibits broad and potent in vivo anti-tumor activities.
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Orally Active Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Bevacizumab | Sunitinib | Imatinib | Semaxinib | SU 5402 | PD173074 | 5Z-7-Oxozeaenol | Cediranib | SAR131675 | GW2580 | AT9283 | Gandotinib | KW-2449 | GW806742X | Tanshi IIA | PF-03814735 | ZM-447439 | SNS-314 mesylate | Vatalanib dihydrochloride | CP-547632 | AST 487 | Tyrphostin A9 | Ki20227 | Motesanib | SU14813 | Ramucirumab | SU1498 | MAZ51
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