Pracinostat Property

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)

color 

White to light brown

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

Pracinostat Chemical Properties,Usage,Production

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