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Pracinostat

Chemical Structure : Pracinostat

CAS No.: 929016-96-6

Pracinostat (SB939;SB-939;SB 939)

Catalog No.: PC-43492Not For Human Use, Lab Use Only.

Pracinostat (SB939) is a potent, orally active HDAC inhibitor that potently inhibits class I, II, and IV HDACsw with Ki of 15-100 nM, inhibits HDAC1 with IC50 of 77 nM.

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Biological Activity

Pracinostat (SB939) is a potent, orally active HDAC inhibitor that potently inhibits class I, II, and IV HDACsw with Ki of 15-100 nM, inhibits HDAC1 with IC50 of 77 nM.
Pracinostat (SB939) shows cellular potency against COLO 205 cells with IC50 of 0.56 uM.
Pracinostat (SB939) is highly efficacious in in vivo tumor models (HCT-116, PC-3, A2780, MV4-11, Ramos), and has high and dose-proportional oral exposures and very good ADME, safety, and pharmaceutical properties>
Pracinostat (SB939) also is a potent inhibitor of the growth of Plasmodium falciparum asexual-stage parasites in vitro (IC50=100 to 200 nM), causing hyperacetylation of parasite histone and nonhistone proteins.

Physicochemical Properties

M.Wt 358.48
Formula C20H30N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Propenamide, 3-[2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl]-N-hydroxy-, (2E)-

References

1. Wang H, et al. J Med Chem. 2011 Jul 14;54(13):4694-720.

2. Novotny-Diermayr V, et al. Mol Cancer Ther. 2011 Jul;10(7):1207-17.

3. Sumanadasa SD, et al. Antimicrob Agents Chemother. 2012 Jul;56(7):3849-56.

4. Razak AR, et al. Br J Cancer. 2011 Mar 1;104(5):756-62.

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