SML4043
PCI-24781
≥98% (HPLC)
别名:
3-[(Dimethylamino)methyl]-N-[2-[4-(hydroxycarbamoyl)phenoxy]ethyl]-1-benzofuran-2-carboxamide, 3-[(Dimethylamino)methyl]-N-[2-[4-[(hydroxyamino)carbonyl]phenoxy]ethyl]-2-benzofurancarboxamide, Abexinostat, CRA-024781
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to pink
溶解性
DMSO: 2 mg/mL, clear (Warmed)
储存温度
-10 to -25°C
SMILES字符串
N(O)C(=O)c1ccc(cc1)OCCNC(=O)c2[o]c3c(c2CN(C)C)cccc3
CN(C)CC1=C(C(NCCOC2=CC=C(C(NO)=O)C=C2)=O)OC3=CC=CC=C31
InChI
1S/C21H23N3O5/c1-24(2)13-17-16-5-3-4-6-18(16)29-19(17)21(26)22-11-12-28-15-9-7-14(8-10-15)20(25)23-27/h3-10,27H,11-13H2,1-2H3,(H,22,26)(H,23,25)
InChI key
MAUCONCHVWBMHK-UHFFFAOYSA-N
相关类别
生化/生理作用
Orally bioavailable, potent and selective pan-HDAC inhibitor.
PCI-24781 (Abexinostat) is an orally bioavailable, potent, and selective pan-HDAC inhibitor that exhibits potent antitumor activities. It inhibits all Class I and Class II HDAC isoforms (Ki = 7 nM HDAC1, 19 nM HDAC2, 8.2 nM HDAC3/SMRT, 17 nM HDAC6, 280 nM HDAC8, 24 nM HDAC10) although it is reported to be a more potent inhibitor of HDACs 1 and 3 at low concentrations.
PCI-24781 (Abexinostat) is an orally bioavailable, potent, and selective pan-HDAC inhibitor that exhibits potent antitumor activities. It inhibits all Class I and Class II HDAC isoforms (Ki = 7 nM HDAC1, 19 nM HDAC2, 8.2 nM HDAC3/SMRT, 17 nM HDAC6, 280 nM HDAC8, 24 nM HDAC10) although it is reported to be a more potent inhibitor of HDACs 1 and 3 at low concentrations.
储存分类代码
11 - Combustible Solids
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Sofia Rivera et al.
Oncotarget, 8(34), 56210-56227 (2017-09-17)
Despite prominent role of radiotherapy in lung cancer management, there is an urgent need for strategies increasing therapeutic efficacy. Reversible epigenetic changes are promising targets for combination strategies using HDAC inhibitors (HDACi). Here we evaluated on two NSCLC cell lines
Tianshu Yang et al.
Theranostics, 11(5), 2058-2076 (2021-01-28)
Histone deacetylases (HDACs) are involved in key cellular processes and have been implicated in cancer. As such, compounds that target HDACs or drugs that target epigenetic markers may be potential candidates for cancer therapy. This study was therefore aimed to
Joseph J Buggy et al.
Molecular cancer therapeutics, 5(5), 1309-1317 (2006-05-30)
CRA-024781 is a novel, broad spectrum hydroxamic acid-based inhibitor of histone deacetylase (HDAC) that shows antitumor activity in vitro and in vivo preclinically and is under evaluation in phase I clinical trials for cancer. CRA-024781 inhibited pure recombinant HDAC1 with
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