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.

CAS Number

783355-60-2

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.