WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205787
CAS#: 864814-88-0 (free base)
Description: Resminostat, also known as 4S-201 and RAS2410, is an orally bioavailable inhibitor of histone deacetylases (HDACs) with potential antineoplastic activity. Resminostat binds to and inhibits HDACs leading to an accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, inhibition of the transcription of tumor suppressor genes, inhibition of tumor cell division and the induction of tumor cell apoptosis.
MedKoo Cat#: 205787
Name: Resminostat
CAS#: 864814-88-0 (free base)
Chemical Formula: C16H19N3O4S
Exact Mass: 349.10963
Molecular Weight: 349.40476
Elemental Analysis: C, 55.00; H, 5.48; N, 12.03; O, 18.32; S, 9.18
Related CAS #: 1187075-34-8 (HCl) 864814-88-0 (free base)
Synonym: 4SC201; 4SC-201; 4SC 201; RAS-2410; RAS2410; RAS 2410; Resminostat.
IUPAC/Chemical Name: (E)-3-(1-((4-((dimethylamino)methyl)phenyl)sulfonyl)-1H-pyrrol-3-yl)-N-hydroxyacrylamide.
InChi Key: FECGNJPYVFEKOD-VMPITWQZSA-N
InChi Code: InChI=1S/C16H19N3O4S/c1-18(2)11-13-3-6-15(7-4-13)24(22,23)19-10-9-14(12-19)5-8-16(20)17-21/h3-10,12,21H,11H2,1-2H3,(H,17,20)/b8-5+
SMILES Code: O=C(NO)/C=C/C1=CN(S(=O)(C2=CC=C(CN(C)C)C=C2)=O)C=C1
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 349.40476 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: Zhao J, Lawless MW. Resminostat: Opening the door to epigenetic treatments for liver cancer. Hepatology. 2016 Feb;63(2):668-9. doi: 10.1002/hep.27853. Epub 2015 May 29. PubMed PMID: 25891162.
2: Kitazono S, Fujiwara Y, Nakamichi S, Mizugaki H, Nokihara H, Yamamoto N, Yamada Y, Inukai E, Nakamura O, Tamura T. A phase I study of resminostat in Japanese patients with advanced solid tumors. Cancer Chemother Pharmacol. 2015 Jun;75(6):1155-61. doi: 10.1007/s00280-015-2741-8. Epub 2015 Apr 7. PubMed PMID: 25847480.
3: Brunetto AT, Ang JE, Lal R, Olmos D, Molife LR, Kristeleit R, Parker A, Casamayor I, Olaleye M, Mais A, Hauns B, Strobel V, Hentsch B, de Bono JS. First-in-human, pharmacokinetic and pharmacodynamic phase I study of Resminostat, an oral histone deacetylase inhibitor, in patients with advanced solid tumors. Clin Cancer Res. 2013 Oct 1;19(19):5494-504. doi: 10.1158/1078-0432.CCR-13-0735. Epub 2013 Sep 24. PubMed PMID: 24065624; PubMed Central PMCID: PMC3790647.
4: Rajak H, Singh A, Raghuwanshi K, Kumar R, Dewangan PK, Veerasamy R, Sharma PC, Dixit A, Mishra P. A structural insight into hydroxamic acid based histone deacetylase inhibitors for the presence of anticancer activity. Curr Med Chem. 2014;21(23):2642-64. PubMed PMID: 23895688.
5: Wörns MA. Systemic therapy and synergies by combination. Dig Dis. 2013;31(1):104-11. doi: 10.1159/000347202. Epub 2013 Jun 17. Review. PubMed PMID: 23797131.
6: Mandl-Weber S, Meinel FG, Jankowsky R, Oduncu F, Schmidmaier R, Baumann P. The novel inhibitor of histone deacetylase resminostat (RAS2410) inhibits proliferation and induces apoptosis in multiple myeloma (MM) cells. Br J Haematol. 2010 May;149(4):518-28. doi: 10.1111/j.1365-2141.2010.08124.x. Epub 2010 Mar 1. PubMed PMID: 20201941.
