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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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