HDAC-IN-2 - CAS 1316215-12-9
Catalog number: 1316215-12-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C24H26ClN5O3
Molecular Weight:
467.95
COA:
Inquire
Targets:
HDAC
Description:
HDAC-IN-2, a selective HDAC inhibitor, has been found to probably restrain the transcription and division of tumor oncogene and could also lead to the apoptosis of tumor cells.It is under Phase II trials against Multiple myeloma. IC50: 4 nM and 76 nM for
Purity:
98%
Appearance:
Powder
Synonyms:
HDAC-IN-2; 2-((2-Chlorophenyl)(phenyl)amino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide; UNII-441P620G3P; 441P620G3P; Citarinostat
Solubility:
DMSO: ≥ 30 mg/mL
Storage:
-20ºC Freeze
MSDS:
Inquire
Application:
HDAC-IN-2 is a selective HDAC inhibitor that has been found to probably restrain the transcription and division of tumor oncogene and could also lead to the apoptosis of tumor cells.It is under Phase II trials against Multiple myeloma.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
VLIUIBXPEDFJRF-UHFFFAOYSA-N
InChI:
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)
Canonical SMILES:
C1=CC=C(C=C1)N(C2=CC=CC=C2Cl)C3=NC=C(C=N3)C(=O)NCCCCCCC(=O)NO
Current Developer:
Acetylon Pharmaceuticals
1.Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models.
Huang P;Almeciga-Pinto I;Jarpe M;van Duzer JH;Mazitschek R;Yang M;Jones SS;Quayle SN Oncotarget. 2017 Jan 10;8(2):2694-2707. doi: 10.18632/oncotarget.13738.
ACY-241 is a novel, orally available and selective histone deacetylase (HDAC) 6 inhibitor in Phase 1b clinical development in multiple myeloma (;NCT 02400242;). Like the structurally related drug ACY-1215 (ricolinostat), ACY-241 has the potential for a substantially reduced side effect profile versus current nonselective HDAC inhibitor drug candidates due to reduced potency against Class I HDACs while retaining the potential for anticancer effectiveness. We now show that combination treatment of xenograft models with paclitaxel and either ricolinostat or ACY-241 significantly suppresses solid tumor growth. In cell lines from multiple solid tumor lineages, combination treatment with ACY-241 and paclitaxel enhanced inhibition of proliferation and increased cell death relative to either single agent alone. Combination treatment with ACY-241 and paclitaxel also resulted in more frequent occurrence of mitotic cells with abnormal multipolar spindles and aberrant mitoses, consistent with the observed increase of aneuploid cells. At the molecular level, multipolar mitotic spindle formation was observed to be NuMA-dependent and γ-tubulin independent, suggesting that treatment-induced multipolar spindle formation does not depend on centrosomal amplification.
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