SMILES string
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
assay
≥98% (HPLC)
form
powder
color
white to pink
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
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.
存储类别
11 - Combustible Solids
法规信息
新产品
此项目有
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
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
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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