ACY-1215 Chemical Properties

Melting point:

189 - 191°C

Density 

1.239±0.06 g/cm3(Predicted)

storage temp. 

-20°C Freezer

solubility 

DMSO (Slightly), Methanol (Slightly)

pka

9.47±0.20(Predicted)

form 

Solid

color 

White to Off-White

ACY-1215 Usage And Synthesis

Description

ACY-1215 is an inhibitor of histone deacetylase 6 (HDAC6; IC₅₀ = 5 nM). It is at least 10-fold less active against other HDACs in enzymatic assays. ACY-1215 shows synergistic activity with the proteasome inhibitor bortezomib against multiple myeloma (MM) cells, inducing protracted endoplasmic reticulum stress and apoptosis. ACY-1215 combined with proteasome inhibitors suppresses tumor growth and increases survival in mice with MM and mantle cell lymphoma xenografts. A multicenter phase I trial examining ACY-1215 combined with the E3 ligase inhibitor lenalidomide and dexamethasone in multiple myeloma found inhibition of HDAC6 in vivo. ACY-1215 also diminishes liver cyst development and fibrosis in a rat model of polycystic liver disease.

Uses

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).

Definition

ChEBI: N-[7-(hydroxyamino)-7-oxoheptyl]-2-(N-phenylanilino)-5-pyrimidinecarboxamide is a pyrimidinecarboxylic acid.

target

HDAC6

ACY-1215(1316214-52-4)Related Product Information

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