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Product IntroductionBioactivity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
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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
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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