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PCI-24781 (CRA-024781)

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.

Product Specifications

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.

Solubility

Soluble in DMSO

Molecular Formula

C21H23N3O5

Shipping Conditions

Room Temperature (continental US) or Gel Packs

Storage Conditions

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.

Calculated Molecular Weight

397.4 Da

CAS Number

783355-60-2

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