西奥罗尼 T35570

Product Introduction
Bioactivity


英文名: Chiauranib

描述: Chiauranib 是一种针对肿瘤血管生成的多靶点抑制剂，具有强大的抗癌作用。 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 CSF1R，IC50 值范围为 1-9 nM。

体外活性: 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].

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (137.78 mM)


关键字: CSF-1R | VEGFR2 | CSF1R | Vascular endothelial growth factor receptor | VEGFR3 | anti-angiogenesis | CD117 | Aurora Kinase | c-Kit | CS-2164 | CSF-1 receptor | colony stimulating factor 1 receptor | PDGFRα | PDGFR | Aurora-B | anticancer | inhibit | SCFR | Inhibitor | VEGFR | Chiauranib | Platelet-derived growth factor receptor | CS 2164 | VEGFR1 | c-Fms

相关产品: c-Fms-IN-2 | PF 477736 | cFMS Receptor Inhibitor IV | CSF1R-IN-2 | AEE788 | c-Fms-IN-14 | Onatasertib | c-Fms-IN-13 | Pazopanib Hydrochloride | Pexidartinib

相关库: Drug Repurposing Compound Library | Anti-Prostate Cancer Compound Library | Angiogenesis related Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途