Bioactivity:

Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFR_ and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects[1]. Chiauranib (CS2164; 3 _M; 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[1].In HUVEC and PDGFR_ phosphorylation in PDGFR_ overexpressed NIH3T3 cells, Chiauranib (CS2164; 0.03-3 _M) 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[1].. 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[1]. 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[1]. [1]. You Zhou, et al. CS2164, a novel multi-target inhibitor against tumor angiogenesis, mitosis and chronic inflammation with anti-tumor potency. Cancer Sci. 2017 Mar;108(3):469-477.

CAS nr:

1256349-48-0

Purity:

98%

Molecular Weight:

435,47

SMILES:

N/A

Formula:

C27H21N3O3

Pathway:

Angiogenesis,Tyrosine Kinase/Adaptors,Tyrosine Kinase/Adaptors,Angiogenesis,Chromatin/Epigenetic,Cell Cycle/Checkpoint,Tyrosine Kinase/Adaptors,Tyrosine Kinase/Adaptors,Angiogenesis,Tyrosine Kinase/Adaptors

Target:

PDGFR,PDGFR,VEGFR,VEGFR,Aurora Kinase,Aurora Kinase,c-Fms,c-Kit,FLT,FLT