487020-03-1|HI-TOPK-032|N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)thiophene-2-carboxamide|-范德生物科技公司

HI-TOPK-032

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names：
N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)thiophene-2-carboxamide
CAS号：
487020-03-1
MDL Number：
MF(分子式)： C20H11N5OS MW(分子量)： 369.2
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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询价

中文别名	HI-TOPK-032
英文别名	HI-TOPK-032; HI-TOPK032; HI-TOPK 032.
CAS号	487020-03-1
Inchi	InChI=1S/C20H11N5OS/c21-11-13-16-10-12(22-20(26)17-6-3-9-27-17)7-8-25(16)19-18(13)23-14-4-1-2-5-15(14)24-19/h1-10H,(H,22,26)
InchiKey	BCSBXWKRZUPFHW-UHFFFAOYSA-N
分子式 Formula	C20H11N5OS
分子量 Molecular Weight	369.2
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	HI-TOPK-032(CAS:487020-03-1):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	HI-TOPK-032 is a potent and selective TOPK inhibitor. In vitro, HI-TOPK-032 strongly suppressed TOPK kinase activity but had little effect on extracellular signal–regulated kinase 1 (ERK1), c-jun—NH2—kinase 1, or p38 kinase activities. HI-TOPK-032 also inhibited anchorage-dependent and -independent colon cancer cell growth by reducing ERK-RSK phosphorylation as well as increasing colon cancer cell apoptosis through regulation of the abundance of p53, cleaved caspase-7, and cleaved PARP. In vivo, administration of HI-TOPK-032 suppressed tumor growth in a colon cancer xenograft model. HI-TOPK-032 may be further developed as a potential therapeutic against colorectal cancer. The serine-threonine mitogen-activated protein kinase kinase family member T-LAK cell–originated protein kinase (TOPK/PBK) is heavily involved in tumor development, cancer growth, apoptosis, and inflammation ( Cancer Res; 72(12); 3060–8.).
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警示图
危险性	Warning
危险性警示
安全声明
安全防护
备注

[1]Joel M, Mughal AA, Grieg Z, Murrell W, Palmero S, Mikkelsen B, Fjerdingstad HB, Sandberg CJ, Behnan J, Glover JC, Langmoen IA, Stangeland B. Targeting PBK/TOPK decreases growth and survival of glioma initiating cells in vitro and attenuates tumor growth in vivo. Mol Cancer. 2015 Jun 17;14(1):12[1]doi: 10.1186/s12943-015-0398-x. PubMed PMID: 26081429; PubMed Central PMCID: PMC4470057.

[2]Kim DJ, Li Y, Reddy K, Lee MH, Kim MO, Cho YY, Lee SY, Kim JE, Bode AM, Dong Z. Novel TOPK inhibitor HI-TOPK-032 effectively suppresses colon cancer growth. Cancer Res. 2012 Jun 15;72(12):3060-8. doi: 10.1158/0008-5472.CAN-11-3851. Epub 2012 Apr 20. PubMed PMID: 22523035.

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