Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C16H19N3O4S |
| Molecular Weight | 349.405 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)CC1=CC=C(C=C1)S(=O)(=O)N2C=CC(\C=C\C(=O)NO)=C2
InChI
InChIKey=FECGNJPYVFEKOD-VMPITWQZSA-N
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+
| Molecular Formula | C16H19N3O4S |
| Molecular Weight | 349.405 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Optical Activity | NONE |
Resminostat (4SC-201) is a hydroxamate HDAC inhibitor (a novel class I, IIb, and IV histone deacetylase inhibitor). Resminostat inhibits proliferation of a large variety of rodent and human cancer cell lines, likely via the Akt signalling pathway. Phase I and II clinical trials have evaluated the efficacy and safety of resminostat in the treatment of relapsed or refractory Hodgkin's Lymphoma, hepatocellular carcinoma, advanced colorectal carcinoma, and in patients with advanced stage mycosis fungoides or Sezary syndrome (an aggressive form of blood cancer). Results in patients with hepatocellular carcinoma showed that resminostat (combined with sorafenib) was safe, well-tolerated and displayed early signs of efficacy.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: Q13547 Gene ID: 3065.0 Gene Symbol: HDAC1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/20201941 |
42.5 nM [IC50] | ||
Target ID: O15379 Gene ID: 8841.0 Gene Symbol: HDAC3 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/20201941 |
50.1 nM [IC50] | ||
Target ID: Q9UBN7 Gene ID: 10013.0 Gene Symbol: HDAC6 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/20201941 |
71.8 nM [IC50] |
PubMed
| Title | Date | PubMed |
|---|---|---|
| First-in-human, pharmacokinetic and pharmacodynamic phase I study of Resminostat, an oral histone deacetylase inhibitor, in patients with advanced solid tumors. | 2013-10-01 |
|
| The novel inhibitor of histone deacetylase resminostat (RAS2410) inhibits proliferation and induces apoptosis in multiple myeloma (MM) cells. | 2010-05 |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:35:01 GMT 2025
by
admin
on
Mon Mar 31 18:35:01 GMT 2025
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| Record UNII |
1578EUB98L
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| Record Status |
Validated (UNII)
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FDA ORPHAN DRUG |
345511
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FDA ORPHAN DRUG |
351411
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NCI_THESAURUS |
C1946
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EU-Orphan Drug |
EU/3/11/913
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SUB120712
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C84856
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1578EUB98L
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864814-88-0
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C550599
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100000143986
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11609955
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RESMINOSTAT
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DTXSID50235587
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DB12392
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9239
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