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ACY-1215

ACY-1215 structure

ACY-1215 

structure
  • CAS No:

    1316214-52-4

  • Formula:

    C24H27N5O3

  • Chemical Name:

    ACY-1215

  • Synonyms:

    Rocilinostat (ACY-1215);2-(Diphenylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]-5-pyrimidinecarboxamide;ACY 63;2-(DiphenylaMino)-N-(7-(hydroxyaMino)-7-oxoheptyl)pyriMidine-5-carboxaMide;5-Pyrimidinecarboxamide, 2-(diphenylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]-;2-(Diphenylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]-5-pyrimidinecarboxamideACY 1215;Rocilinostat, >=99%;Ricolinostat

  • Categories:

    Biochemical Engineering  >  Inhibitors

Description

Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.


N-[7-(hydroxyamino)-7-oxoheptyl]-2-(N-phenylanilino)-5-pyrimidinecarboxamide is a pyrimidinecarboxylic acid.|Ricolinostat is under investigation for the treatment of Breast Carcinoma and Metastatic Breast Cancer.|Ricolinostat is an orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity. Ricolinostat selectively targets and binds to HDAC6, thereby disrupting the Hsp90 protein chaperone system through hyperacetylation of Hsp90 and preventing the subsequent aggresomal protein degradation. This leads to an accumulation of unfolded and misfolded ubiquitinated proteins and may eventually induce cancer cell apoptosis, and inhibition of cancer cell growth. HDAC6, a class II HDAC deacetylase located in the cytoplasm, appears to play a key role in the formation and activation of the aggresomes needed for degradation of misfolded proteins. Compared to non-selective HDAC inhibitor, ACY-1215 is able to reduce the toxic effects on normal, healthy cells.

ACY-1215 Basic Attributes

433.50288

433.211395

WKT909C62B

DTXSID40157148

C96431

2933599090

Characteristics

107

3.4

1.239±0.06 g/cm3(Predicted)

1.620

H2O: Insuluble (4.3E-3 g/L) (25 ºC)

Drug Information

Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)|Compounds that inhibit HISTONE DEACETYLASES. This class of drugs may influence gene expression by increasing the level of acetylated HISTONES in specific CHROMATIN domains. (See all compounds classified as Histone Deacetylase Inhibitors.)

2-(diphenylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide

ACY-1215 Use and Manufacturing

This compound acts as a selective HDAC-6 (histone deacetylase) inihibitor. HDAC is linked to the transcription of DNA in cancers, including multiple myeloma (MM).

Computed Properties

Molecular Weight:433.5
XLogP3:3.4
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:11
Exact Mass:433.21138974
Monoisotopic Mass:433.21138974
Topological Polar Surface Area:107
Heavy Atom Count:32
Complexity:538
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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