2014年8月11日星期一

Resminostat|cas 864814-88-0| DC Chem|Supplier|Price|Buy 

Resminostat|cas 864814-88-0| DC Chem|Supplier|Price|Buy
DC Chemicals Supply: Resminostat|cas 864814-88-0,Purity: >98% ,Cat No. DC7261, In stock.

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Resminostat|cas 864814-88-0 ,Synonym: RAS2410; 4SC-201; RAS 2410; RAS-2410  ,Chemical name: 2-Propenamide,3-[1-[[4-[(dimethylamino)methyl]phenyl]sulfonyl]-1H-pyrrol-3-yl]-N-hydroxy-,(2E)- ,Molecular Formula: C16H19N3O4S ,MW:349.4

Resminostat, cas 864814-88-0,Purity: >98%, Best Price and quality from DC Chemicals. Resminostat(RAS2410; 4SC-201) is a potent inhibitor of HDAC1/3/6(IC50=43-72 nM); less potent to HDAC8 with IC50 of 877 nM.

Resminostat [HCl] is acting as a potent inhibitor of recombinant HDAC 1, 3 and 6 isoenzymes with a substrate competitive binding mode. It can induce hyperacetylation of histone H4 in MM cells. Low micromolar concentrations of resminostat abrogates cell growth and strongly induces apoptosis in MM cell lines (OPM-2, NCI-H929, U266 ) as well as primary MM cells. At 1 μM, resminostat inhibits proliferation and induces G0/G1 cell cycle arrest in OPM-2, NCI-H929, U266 MM cell lines accompanied with decreased levels of cyclin D1, cdc25a, Cdk4 and pRb as well as upregulation of p21. Resminostat decreases phosphorylation of 4E-BP1 and p70S6k indicating an interference with Akt pathway signalling. Treatment with resminostat results in increased protein levels of Bim and Bax and decreases levels of Bcl-xL. Caspases 3, 8 and 9 are activated by resminostat. Furthermore, synergistic effects are observed for combinations of resminostat with melphalan and the proteasome inhibitors bortezomib and S-2209. [1] Oral resminostat at 600 mg QD continuously d1?5 in a 14 day cycle is well-tolerated. Resminostat shows a favourable PK profile, with high bioavailability and low inter-pt variability. The apparent t 1/2 of oral resminostat ranged from 2.7 to 4.4 hours. The modulation of plasma biomarkers further indicates drug activity. [2]

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