PCI-24781
PCI-24781 (formerly CRA-024781) is a broad spectrum phenyl hydroxamic acid-based, orally bioavailable compound currently in phase I clinical trials for the treatment of neoplastic diseases. The compound is a specific inhibitor of multiple HDAC isoforms that potently inhibits tumor growth in vivo.
IUPAC Name:
3-(dimethylaminomethyl)-N-[2-[4-(hydroxycarbamoyl)phenoxy]ethyl]-1-benzofuran-2-carboxamide
Molecular Weight: 397,43 g/mol
Molecular Formula: C21H23N3O5
SMILES: CN(C)Cc1c2ccccc2oc1C(=O)NCCOc3ccc(C(=O)NO)cc3
Canonical SMILES: CN(C)CC1=C(OC2=CC=CC=C21)C(=O)NCCOC3=CC=C(C=C3)C(=O)NO
InChIKey Identifier: MAUCONCHVWBMHK-UHFFFAOYSA-N
CAS Number: 783355-60-2
Melting point: n/a °C
Solubility: soluble in DMSO
2D Molfile: Get the molfile
Synonyms: CRA-02478; CRA024781; CRA-024781
PCI-24781 has an optimized half life, oral bioavailability, potency, and duration of exposure compared to competitor drugs (e.g. Zolinza or LBH-589) to achieve an ideal balance of efficacy with minimal toxicity.
References:
1) Nilsa Rivera-Del Valle, et al. PCI-24781, a Novel Hydroxamic Acid HDAC Inhibitor, Exerts Cytotoxicity and Histone Alterations via Caspase-8 and FADD in Leukemia Cells. International Journal of Cell Biology, Volume 2010, Article ID 207420.
2) Adimoolam et al. HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination. PNAS December 4, 2007 vol. 104 no. 49 19482-19487.
3) Carmen A. Banuelos et al. Radiosensitization by the Histone Deacetylase Inhibitor PCI-24781. Clinical Cancer Research November 2007 13; 6816.
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