WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206471
CAS#: 1316215-12-9
Description: Citarinostat, also known as ACY-241, is a potent, selective and orally available histone deacetylase (HDAC) inhibitor, with potential antineoplastic activity. Upon oral administration, ACY-241 inhibits the activity of HDACs; this results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. This leads to the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes, which inhibit tumor cell division and induce tumor cell apoptosis.
MedKoo Cat#: 206471
Name: Citarinostat
CAS#: 1316215-12-9
Chemical Formula: C24H26ClN5O3
Exact Mass: 467.1724
Molecular Weight: 467.954
Elemental Analysis: C, 61.60; H, 5.60; Cl, 7.58; N, 14.97; O, 10.26
Related CAS #: 1316215-12-9
Synonym: ACY-241; ACY 241; ACY241; HDAC-IN-2; Citarinostat.
IUPAC/Chemical Name: 2-((2-chlorophenyl)(phenyl)amino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide
InChi Key: VLIUIBXPEDFJRF-UHFFFAOYSA-N
InChi Code: InChI=1S/C24H26ClN5O3/c25-20-12-7-8-13-21(20)30(19-10-4-3-5-11-19)24-27-16-18(17-28-24)23(32)26-15-9-2-1-6-14-22(31)29-33/h3-5,7-8,10-13,16-17,33H,1-2,6,9,14-15H2,(H,26,32)(H,29,31)
SMILES Code: ClC1=CC=CC=C1N(C2=CC=CC=C2)C3=NC=C(C=N3)C(NCCCCCCC(NO)=O)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 467.954 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Laino AS, Betts BC, Veerapathran A, Dolgalev I, Sarnaik A, Quayle SN, Jones SS, Weber JS, Woods DM. HDAC6 selective inhibition of melanoma patient T-cells augments anti-tumor characteristics. J Immunother Cancer. 2019 Feb 6;7(1):33. doi: 10.1186/s40425-019-0517-0. PubMed PMID: 30728070; PubMed Central PMCID: PMC6366050.
2: Lorenzo Pisarello M, Masyuk TV, Gradilone SA, Masyuk AI, Ding JF, Lee PY, LaRusso NF. Combination of a Histone Deacetylase 6 Inhibitor and a Somatostatin Receptor Agonist Synergistically Reduces Hepatorenal Cystogenesis in an Animal Model of Polycystic Liver Disease. Am J Pathol. 2018 Apr;188(4):981-994. doi: 10.1016/j.ajpath.2017.12.016. Epub 2018 Jan 31. PubMed PMID: 29366679; PubMed Central PMCID: PMC5963486.
3: Lernoux M, Schnekenburger M, Dicato M, Diederich M. Anti-cancer effects of naturally derived compounds targeting histone deacetylase 6-related pathways. Pharmacol Res. 2018 Mar;129:337-356. doi: 10.1016/j.phrs.2017.11.004. Epub 2017 Nov 11. Review. PubMed PMID: 29133216.
4: Ray A, Das DS, Song Y, Hideshima T, Tai YT, Chauhan D, Anderson KC. Combination of a novel HDAC6 inhibitor ACY-241 and anti-PD-L1 antibody enhances anti-tumor immunity and cytotoxicity in multiple myeloma. Leukemia. 2018 Mar;32(3):843-846. doi: 10.1038/leu.2017.322. Epub 2017 Nov 6. PubMed PMID: 29104288; PubMed Central PMCID: PMC5842120.
5: North BJ, Almeciga-Pinto I, Tamang D, Yang M, Jones SS, Quayle SN. Enhancement of pomalidomide anti-tumor response with ACY-241, a selective HDAC6 inhibitor. PLoS One. 2017 Mar 6;12(3):e0173507. doi: 10.1371/journal.pone.0173507. eCollection 2017. PubMed PMID: 28264055; PubMed Central PMCID: PMC5338861.
6: Huang P, Almeciga-Pinto I, Jarpe M, van Duzer JH, Mazitschek R, Yang M, Jones SS, Quayle SN. Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models. Oncotarget. 2017 Jan 10;8(2):2694-2707. doi: 10.18632/oncotarget.13738. PubMed PMID: 27926524; PubMed Central PMCID: PMC5356834.
7: Richardson PG, Moreau P, Laubach JP, Maglio ME, Lonial S, San-Miguel J. Deacetylase inhibitors as a novel modality in the treatment of multiple myeloma. Pharmacol Res. 2017 Mar;117:185-191. doi: 10.1016/j.phrs.2016.11.020. Epub 2016 Nov 21. Review. PubMed PMID: 27884726.
