Chiauranib

SKU: orb1304065

Description

Chiauranib

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1256349-48-0
• MW: 435.47
• Purity: 99.22% (May vary between batches)
• Formula: C₂₇H₂₁N₃O₃
• SMILES: COc1ccc2c(Oc3ccc4c(cccc4c3)C(=O)Nc3ccccc3N)ccnc2c1
• Target: c-Kit,PDGFR,Aurora Kinase,FLT,VEGFR,c-Fms
• Solubility: DMSO:60 mg/mL (137.78 mM);10% DMSO+90% Saline:2.5 mg/mL (5.74 mM)

Bioactivity

• Target IC50:
  KDR:7 nM|c-Kit:4 nM|Aurora B:9 nM|PDGFRα:1 nM|PDGFRβ:93 nM|FLK1:8 nM|FLT4:9 nM|CSF1R:7 nM
• In Vivo:
  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.
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• In Vitro:
  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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KDR, inhibit, PDGFR, Platelet-derived growth factor receptor, PDGFRα, Inhibitor, FLT4, FLT1, anti-angiogenesis, anticancer, Aurora-B, AuroraKinase, Aurora B, Aurora Kinase, CS 2164, CSF1R, CSF-1 receptor, CS2164, CS-2164, CSF-1R, CD117, Chiauranib, cFms, c-Fms, cKit, c-Kit, colony stimulating factor 1 receptor, SCFR, Vascular endothelial growth factor receptor, VEGFR3, VEGFR2, VEGFR1, VEGFR

Compound Identifiers

PubChem CID

49779393