PCI-24781 is a broad spectrum hydroxamic acid-based inhibitor of HDAC that shows antitumor activity in vitro. PCI-24781 inhibited pure recombinant HDAC1 with a Ki of 0.007 Mmol/L, 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 μmol/L.
Soluble in water (<1 mg/ml at 25 °C), DMSO (80 mg/ml at 25 °C), ethanol (<1 mg/ml at 25 °C), and methanol (sparingly).
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Choy et alChoy et al. (PubMed ID 25536954) found that the HDAC inhibitor PCI-24781 (abexinostat) blocked histone acetylation in peripheral blood mononuclear cells of patients with metastatic sarcoma. -SCBT Publication Review
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