PCI-24781 (CRA-024781)

Catalog #

27769-1

$230 *

Size: 10 mg

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Description

PCI-24781 (also known as CRA-024781) is a novel, broad spectrum inhibitor of HDACs that shows antitumor activity in vitro. PCI-24781 primarily targets HDAC1 (Ki = 7 nM). It also exhibits modest potenty toward HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8.

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Synonyms

PCI-24781; CRA-024781; Abexinostat

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Product Info

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Citations

Target(s)

HDAC

Formula

C₂₁H₂₃N₃O₅

397.4 Da

Solubility

Soluble in DMSO

Biological Activity

PCI-24781 inhibited pure recombinant HDAC1 with a Ki of (Ki = 7 nM), as well as HDAC2, HDAC3/SMRT, HDAC6, HDAC8, and HDAC10 in the nanomolar range. Antitumor activity of PCI-24781 was observed in all 10 tumor cell lines tested, with GI50% values ranging from 0.15 to 3.09 µM.

CAS Registry #

783355-60-2

Background

PCI-24781 is a pan-HDAC inhibitor that shows antitumor activity in vitro and in vivo preclinically and is under evaluation in phase I clinical trials for cancer, particularly B-cell lymphoma. PCI-24781 induces caspase and reactive oxygen species-dependent apoptosis through NF-?B mechanisms in Hodgkin lymphoma and non-Hodgkin lymphoma cell lines.

References

1. Buggy JJ, et al. Mol Cancer Ther, 2006, 5(5), 1309-1317.
2. Bhalla S, et al. Clin Cancer Res, 2009, 15(10), 3354-3365.

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PCI-24781 (CRA-024781)

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