Resminostat HCl

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MedKoo CAT#: 562169

CAS#: 1187075-34-8 (HCl)

Description: Resminostat is an orally bioavailable inhibitor of histone deacetylase 1 (HDAC1), HDAC3, and HDAC6 (IC50s = 43-72 nM),

Chemical Structure

Resminostat HCl
CAS# 1187075-34-8 (HCl)

Theoretical Analysis

MedKoo Cat#: 562169
Name: Resminostat HCl
CAS#: 1187075-34-8 (HCl)
Chemical Formula: C16H20ClN3O4S
Exact Mass: 385.0863
Molecular Weight: 385.86
Elemental Analysis: C, 49.80; H, 5.22; Cl, 9.19; N, 10.89; O, 16.59; S, 8.31

Price and Availability

Size Price Availability Quantity
50.0mg USD 450.0 2 Weeks
100.0mg USD 750.0 2 Weeks
200.0mg USD 1350.0 2 Weeks
500.0mg USD 2850.0 2 Weeks
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Related CAS #: 1187075-34-8 (HCl)   864814-88-0 (free base)    

Synonym: Resminostat Hydrochloride; Resminostat HCl; 4SC-201; 4SC-201; 4SC-201; RAS2410; RAS-2410; RAS 2410;

IUPAC/Chemical Name: (E)-3-[1-[4-[(Dimethylamino)methyl]phenyl]sulfonylpyrrol-3-yl]-N-hydroxyprop-2-enamide;hydrochloride


InChi Code: InChI=1S/C16H19N3O4S.ClH/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);1H/b8-5+;

SMILES Code: O=C(NO)/C=C/C1=CN(S(=O)(C2=CC=C(CN(C)C)C=C2)=O)C=C1.[H]Cl

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

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

Preparing Stock Solutions

The following data is based on the product molecular weight 385.86 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.

Recalculate based on batch purity %
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

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1: Soukupova J, Bertran E, Peñuelas-Haro I, Urdiroz-Urricelqui U, Borgman M, Kohlhof H, Fabregat I. Resminostat induces changes in epithelial plasticity of hepatocellular carcinoma cells and sensitizes them to sorafenib-induced apoptosis. Oncotarget. 2017 Nov 30;8(66):110367-110379. doi: 10.18632/oncotarget.22775. eCollection 2017 Dec 15. PubMed PMID: 29299154; PubMed Central PMCID: PMC5746389.

2: Enzenhofer E, Kadletz L, Stanisz I, Kotowski U, Seemann R, Schmid R, Thurnher D, Heiduschka G. Effect of the histone deacetylase inhibitor resminostat on head and neck squamous cell carcinoma cell lines. Head Neck. 2017 May;39(5):900-907. doi: 10.1002/hed.24699. Epub 2017 Feb 7. PubMed PMID: 28170128.

3: Tambo Y, Hosomi Y, Sakai H, Nogami N, Atagi S, Sasaki Y, Kato T, Takahashi T, Seto T, Maemondo M, Nokihara H, Koyama R, Nakagawa K, Kawaguchi T, Okamura Y, Nakamura O, Nishio M, Tamura T. Phase I/II study of docetaxel combined with resminostat, an oral hydroxamic acid HDAC inhibitor, for advanced non-small cell lung cancer in patients previously treated with platinum-based chemotherapy. Invest New Drugs. 2017 Apr;35(2):217-226. doi: 10.1007/s10637-017-0435-2. Epub 2017 Jan 30. PubMed PMID: 28138828.

4: Ellerhoff TP, Berchtold S, Venturelli S, Burkard M, Smirnow I, Wulff T, Lauer UM. Novel epi-virotherapeutic treatment of pancreatic cancer combining the oral histone deacetylase inhibitor resminostat with oncolytic measles vaccine virus. Int J Oncol. 2016 Nov;49(5):1931-1944. doi: 10.3892/ijo.2016.3675. Epub 2016 Aug 31. PubMed PMID: 27601235.

5: Peng X, Zhang D, Li Z, Fu M, Liu H. mTOR inhibition sensitizes human hepatocellular carcinoma cells to resminostat. Biochem Biophys Res Commun. 2016 Sep 2;477(4):556-562. doi: 10.1016/j.bbrc.2016.06.060. Epub 2016 Jun 14. PubMed PMID: 27311860.

6: Fu M, Shi W, Li Z, Liu H. Activation of mPTP-dependent mitochondrial apoptosis pathway by a novel pan HDAC inhibitor resminostat in hepatocellular carcinoma cells. Biochem Biophys Res Commun. 2016 Sep 2;477(4):527-533. doi: 10.1016/j.bbrc.2016.04.147. Epub 2016 May 1. PubMed PMID: 27144317.

7: Bitzer M, Horger M, Giannini EG, Ganten TM, Wörns MA, Siveke JT, Dollinger MM, Gerken G, Scheulen ME, Wege H, Zagonel V, Cillo U, Trevisani F, Santoro A, Montesarchio V, Malek NP, Holzapfel J, Herz T, Ammendola AS, Pegoraro S, Hauns B, Mais A, Lauer UM, Henning SW, Hentsch B. Resminostat plus sorafenib as second-line therapy of advanced hepatocellular carcinoma - The SHELTER study. J Hepatol. 2016 Aug;65(2):280-8. doi: 10.1016/j.jhep.2016.02.043. Epub 2016 Mar 4. PubMed PMID: 26952006.

8: 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.

9: 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.

10: Ruf B, Berchtold S, Venturelli S, Burkard M, Smirnow I, Prenzel T, Henning SW, Lauer UM. Combination of the oral histone deacetylase inhibitor resminostat with oncolytic measles vaccine virus as a new option for epi-virotherapeutic treatment of hepatocellular carcinoma. Mol Ther Oncolytics. 2015 Oct 7;2:15019. doi: 10.1038/mto.2015.19. eCollection 2015. PubMed PMID: 27119111; PubMed Central PMCID: PMC4782956.

11: 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.

12: 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.

13: 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.

14: 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.