Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C24H27N5O3 |
| Molecular Weight | 433.5029 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
ONC(=O)CCCCCCNC(=O)C1=CN=C(N=C1)N(C2=CC=CC=C2)C3=CC=CC=C3
InChI
InChIKey=QGZYDVAGYRLSKP-UHFFFAOYSA-N
InChI=1S/C24H27N5O3/c30-22(28-32)15-9-1-2-10-16-25-23(31)19-17-26-24(27-18-19)29(20-11-5-3-6-12-20)21-13-7-4-8-14-21/h3-8,11-14,17-18,32H,1-2,9-10,15-16H2,(H,25,31)(H,28,30)
| Molecular Formula | C24H27N5O3 |
| Molecular Weight | 433.5029 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Ricolinostat is a selective inhibitor of HDAC6 with IC50 value of 4.7 nM. Ricolinostat demonstrated good anti-proliferative activity on different cell lines and clinical models of cancer. The drug is being tested in phase I/II for the treatment of multiple myeloma and lymphoid malignancies and in phase I in patients with breast cancer, gynecological cancer, cholangiocarcinoma, recurrent chronic lymphoid leukemia.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL1865 |
4.7 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
821 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27646843 |
160 mg 2 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
RICOLINOSTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1489 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27646843 |
160 mg 2 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
RICOLINOSTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.88 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27646843 |
160 mg 2 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
RICOLINOSTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Development and therapeutic implications of selective histone deacetylase 6 inhibitors. | 2013-08-22 |
|
| Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. | 2012-03-15 |
Patents
Sample Use Guides
Lymphoid Malignancies: Patients take 160 mg for 28 consecutive days on a 28-day treatment cycle. Multiple myeloma: Patients take 40-240 mg once daily to 160 mg twice daily
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26643555
MCF-7, MDA-MB-436, MDA-MB-231, T47D, SUM-190, IBC-3, SUM-149 cell lines were treated with increasing concentrations of ricolinostat (1, 2.5, 5 uM) to test drug-induced apoptosis.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 21:23:50 GMT 2025
by
admin
on
Mon Mar 31 21:23:50 GMT 2025
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| Record UNII |
WKT909C62B
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Validated (UNII)
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C1946
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ZZ-154
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C96431
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SUB181488
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DB12376
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CHEMBL2364628
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|---|---|---|---|---|
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IC50
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TARGET -> INHIBITOR |
IC50
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TARGET->WEAK INHIBITOR |
IC50
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TARGET->WEAK INHIBITOR | |||
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TARGET->WEAK INHIBITOR |
IC50
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ACTIVE MOIETY |