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
SMILES	O=C(C1=CC=CS1)NC2=CC3=C(C#N)C4=NC5=CC=CC=C5N=C4N3C=C2
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
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
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.).
Application1
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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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