Chiauranib also known as orally available, small molecule inhibitor of select serine-threonine kinases, including aurora kinase B (aurora B), vascular endothelial growth factor receptors (VEGFRs), stem cell factor receptor (c-KIT), and platelet-derived growth factor receptors (PDGFRs), with potential antineoplastic activity. Upon oral administration, chiauranib binds to and inhibits the activity of aurora B, VEGFRs, c-kit and PDGFRs, which may result in a decrease in the proliferation of tumor cells that overexpress these kinases. These kinases are overexpressed by a variety of cancer cell types.
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Name | Chiauranib |
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Iupac Chemical Name | N-(2-aminophenyl)-6-((7-methoxyquinolin-4-yl)oxy)-1-naphthamide |
Synonyms | Chiauranib; CS2164; CS-2164; CS 2164; Ibcasertib |
Molecular Formula | C27H21N3O3 |
Molecular Weight | 435.47 |
Smile | O=C(C1=C2C=CC(OC3=CC=NC4=CC(OC)=CC=C43)=CC2=CC=C1)NC5=CC=CC=C5N |
InChiKey | BRKWREZNORONDU-UHFFFAOYSA-N |
InChi | InChI=1S/C27H21N3O3/c1-32-18-9-12-22-25(16-18)29-14-13-26(22)33-19-10-11-20-17(15-19)5-4-6-21(20)27(31)30-24-8-3-2-7-23(24)28/h2-16H,28H2,1H3,(H,30,31) |
CAS Number | 1256349-48-0 |
Related CAS |
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Formulation | Off-white solid |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
Solubility | Soluble in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
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Clinical study |
1: Deng M, Shi Y, Chen K, Zhao H, Wang Y, Xie S, Zhao J, Luo Y, Fang Z, Fan Y, Xu
B. CS2164 exerts an antitumor effect against human Non-Hodgkin's lymphomas in
vitro and in vivo. Exp Cell Res. 2018 Aug 15;369(2):356-362. doi:
10.1016/j.yexcr.2018.05.038. Epub 2018 Jun 1. PubMed PMID: 29864401.
2: Zhou Y, Shan S, Li ZB, Xin LJ, Pan DS, Yang QJ, Liu YP, Yue XP, Liu XR, Gao
JZ, Zhang JW, Ning ZQ, Lu XP. 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. doi: 10.1111/cas.13141. Epub 2017 Mar 7.
PubMed PMID: 28004478; PubMed Central PMCID: PMC5378272.