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Chiauranib

Catalog No. T35570 CAS 1256349-48-0

Synonyms: CS2164

Chiauranib is a multi-target inhibitor against tumor angiogenesis and exhibits potent anticancer effects. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF1R, with IC50 values ranging from 1-9 nM.

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Chiauranib, CAS 1256349-48-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 83.00
5 mg	In stock	$ 197.00
10 mg	In stock	$ 322.00
25 mg	In stock	$ 547.00
50 mg	In stock	$ 788.00
100 mg	In stock	$ 1,080.00
1 mL * 10 mM (in DMSO)	In stock	$ 226.00

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Purity: 96.25%

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Storage & Solubility Information

Description	Chiauranib is a multi-target inhibitor against tumor angiogenesis and exhibits potent anticancer effects. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF1R, with IC50 values ranging from 1-9 nM.
Targets&IC50	KDR:7 nM, FLT4:9 nM, FLK1:8 nM, PDGFRα:1 nM
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[1].
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[1].

Synonyms	CS2164
Molecular Weight	435.47
Formula	C27H21N3O3
CAS No.	1256349-48-0

Storage

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

Solubility Information

DMSO: 60 mg/mL (137.78 mM), Sonification is recommended.

References and Literature

1. Zhou Y, 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cardiovascular Disease Compound Library Anti-Colorectal Cancer Compound Library Clinical Compound Library Anti-Lung Cancer Compound Library

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Keywords

Chiauranib 1256349-48-0 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic Tyrosine Kinase/Adaptors c-Fms VEGFR FLT PDGFR c-Kit Aurora Kinase CSF-1R VEGFR2 CSF1R Vascular endothelial growth factor receptor VEGFR3 anti-angiogenesis CD117 CS-2164 CSF-1 receptor colony stimulating factor 1 receptor PDGFRα Aurora-B anticancer inhibit SCFR Inhibitor CS2164 Platelet-derived growth factor receptor CS 2164 VEGFR1 inhibitor

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