Pracinostat Chemical Properties

Density 

1.11

storage temp. 

Store at -20°C

solubility 

insoluble in H2O; ≥11.4 mg/mL in DMSO; ≥24.8 mg/mL in EtOH with ultrasonic

form 

solid

pka

8.67±0.23(Predicted)

Pracinostat Usage And Synthesis

Uses

Pracinostat is a potent and orally active histone deacetylase (HDAC) inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer. The selectivity of Pracinostat for tumor tissues makes it a promising therapeutic candidate for use in patients with advanced solid malignancies. Potent Histone deacetylase inhibitor.

Definition

ChEBI: Pracinostat is a hydroxamic acid that is N-hydroxyacrylamide which is substituted at position 3 by a 2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl group (the E isomer). An orally available pan-histone deacetylase inhibitor with demonstrated activity in the treatment of advanced solid tumours. It has a role as an EC 3.5.1.98 (histone deacetylase) inhibitor, an antineoplastic agent, an apoptosis inducer and an antimalarial. It is an olefinic compound, a hydroxamic acid, a benzimidazole and a tertiary amino compound.

Biological Activity

pracinostat, also known as sb939, is a potent and orally available inhibitor of histone deacetylase (hdac) with a relatively stronger selectivity (more than 1000-fold) for class i, class ii and class iv hdacs rather than class iii hdacs. pracinostat potently suppresses proliferation in a wide range of cancer cell lines, including colon cancer, ovarian cancer, prostate carcinomas, acute myeloid leukaemia (aml) and b cell lymphoma. recent study results have shown that sb939 induces the accumulation of acetylated histone h3 (ach3) and acetylated α-tubulin and increases the expression of the cyclin dependent kinase inhibitor p21 in cancer cells.razak ar, hotte sj, siu ll, chen ex, hirte hw, powers j, walsh w, stayner la, laughlin a, novotny-diermayr v, zhu j, eisenhauer ea. phase i clinical, pharmacokinetic and pharmacodynamic study of sb939, an oral histone deacetylase (hdac) inhibitor, in patients with advanced solid tumours. br j cancer. 2011;104(5):756-762.

target

HDAC1

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