PCI-24781 (CRA-024781) , CAS 783355-60-2

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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.

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 Number: 783355-60-2

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.

Solubility: Soluble in DMSO

Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

Target: HDAC

Biosafety Level: Not applicable (BSL-1)

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.

• Artikelnummer: BPS27769-2
• Hersteller: BPS Bioscience
• Hersteller Artikelnummer: 27769-2
• Green Labware: Nein
• Verpackungseinheit: 50 mg
• Mengeneinheit: STK