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Nanatinostat

编号: 25034
Cas号: 1256448-47-1
纯度: 98% Min.

Nanatinostat, also known as Tractinostat, CHR-3996 and VRx-3996, is an orally bioavailable, second-generation hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor CHR-3996 inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes; these events may result in the inhibition of tumor cell division and the induction of tumor cell apoptosis. This agent may upregulate HSP70 and downregulate anti-apoptotic Bcl-2 proteins more substantially than some first-generation HDAC inhibitors. HDACs, upregulated in many tumor cell types, are a family of metalloenzymes responsible for the deacetylation of chromatin histone proteins.

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化学信息

名称Nanatinostat
Iupac 化学名称2-((1R,5S,6s)-6-(((6-fluoroquinolin-2-yl)methyl)amino)-3-azabicyclo[3.1.0]hexan-3-yl)-N-hydroxypyrimidine-4-carboxamide
同义词CHR3996; CHR-3996; CHR 3996; VRx-3996; VRx3996; VRx 3996; Nanatinostat; Tractinostat;
英文同义词CHR3996; CHR-3996; CHR 3996; VRx-3996; VRx3996; VRx 3996; Nanatinostat; Tractinostat;
分子式C20H19FN6O2
分子量394.40
SmileFC1=CC=C2N=C(CN[C@H]3[C@]4([H])CN(C5=NC=CC(C(NO)=O)=N5)C[C@]34[H])C=CC2=C1
InChiKeyGTAUPYWUPNCTCZ-HWWDLCQESA-N
InChiInChI=1S/C20H19FN6O2/c21-12-2-4-16-11(7-12)1-3-13(24-16)8-23-18-14-9-27(10-15(14)18)20-22-6-5-17(25-20)19(28)26-29/h1-7,14-15,18,23,29H,8-10H2,(H,26,28)/t14-,15+,18+
Cas号1256448-47-1
相关CAS号

订购信息

包装价格库存纯度备货期
大货询价询价询价
Request Bulk Quote Download MSDS 电话 : +86-177 0271 9238   Email : sales@sun-shinechem.com
外观性状类白色固体
纯度98% Min.
存储 0-4℃,可保存几天到几周;-20℃,可保存 几个月。
可溶性溶于DMSO等有机溶剂
处理方式
运输条件可以在室温下进行运输。
海关编码
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study

1: Singh AN, Sharma N. Epigenetic Modulators as Potential Multi-targeted Drugs Against Hedgehog Pathway for Treatment of Cancer. Protein J. 2019 Oct;38(5):537-550. doi: 10.1007/s10930-019-09832-9. PMID: 30993446.


2: Garrido-Laguna I, Tometich D, Hu N, Ying J, Geiersbach K, Whisenant J, Wang K, Ross JS, Sharma S. N of 1 case reports of exceptional responders accrued from pancreatic cancer patients enrolled in first-in-man studies from 2002 through 2012. Oncoscience. 2015 Mar 14;2(3):285-93. doi: 10.18632/oncoscience.141. PMID: 25897431; PMCID: PMC4394134.


3: Smith EM, Zhang L, Walker BA, Davenport EL, Aronson LI, Krige D, Hooftman L, Drummond AH, Morgan GJ, Davies FE. The combination of HDAC and aminopeptidase inhibitors is highly synergistic in myeloma and leads to disruption of the NFκB signalling pathway. Oncotarget. 2015 Jul 10;6(19):17314-27. doi: 10.18632/oncotarget.1168. PMID: 26015393; PMCID: PMC4627310.


4: Banerji U, van Doorn L, Papadatos-Pastos D, Kristeleit R, Debnam P, Tall M, Stewart A, Raynaud F, Garrett MD, Toal M, Hooftman L, De Bono JS, Verweij J, Eskens FA. A phase I pharmacokinetic and pharmacodynamic study of CHR-3996, an oral class I selective histone deacetylase inhibitor in refractory solid tumors. Clin Cancer Res. 2012 May 1;18(9):2687-94. doi: 10.1158/1078-0432.CCR-11-3165. PMID: 22553374.


5: Moffat D, Patel S, Day F, Belfield A, Donald A, Rowlands M, Wibawa J, Brotherton D, Stimson L, Clark V, Owen J, Bawden L, Box G, Bone E, Mortenson P, Hardcastle A, van Meurs S, Eccles S, Raynaud F, Aherne W. Discovery of 2-(6-{[(6 -fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5- carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor. J Med Chem. 2010 Dec 23;53(24):8663-78. doi: 10.1021/jm101177s. Epub 2010 Nov 16. PMID: 21080647.


6: Al-Shamahi A, Murch L, Kirkham K. American Society of Clinical Oncology--46th annual meeting. IDrugs. 2010 Aug;13(8):506-9. PMID: 20721815.

化学结构

25034 - Nanatinostat | CAS 1256448-47-1

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