[CAS NO. 864814-88-0] Resminostat

Name: Resminostat
Brand: Arctom Scientific
SKU: AS938639

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PRODUCTS SPECIFICATIONS [864814-88-0]

Distributor

Catalog

AS938639

Brand

Arctom Scientific

CAS

864814-88-0

DESCRIPTION [864814-88-0]

Overview

MDL	MFCD18633257
Molecular Weight	349.4
Molecular Formula	C16H19N3O4S
SMILES	S(=O)(=O)(N1C=C(/C=C/C(NO)=O)C=C1)C2=CC=C(CN(C)C)C=C2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.8620 mL	14.3102 mL	28.6205 mL
5 mM	0.5724 mL	2.8620 mL	5.7241 mL
10 mM	0.2862 mL	1.4310 mL	2.8620 mL
50 mM	0.0572 mL	0.2862 mL	0.5724 mL

Description

Resminostat (RAS2410) dose-dependently and selectively inhibits with of 42.5 nM/50.1 nM/71.8 nM, less potent to with of 877 nM.

Targets

HDAC1 ^[1]	HDAC3 ^[1]	HDAC6 ^[1]
42.5 nM	50.1 nM	71.8 nM

In vitro

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.

In vivo

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 of oral resminostat ranged from 2.7 to 4.4 hours. The modulation of plasma biomarkers further indicates drug activity.

References

[1] Mandl-Weber S, et al. Br J Haematol, 2010, 149(4), 518-528.
[2] J.E. Ang, et al. EJC Supplements, 2008, 6(12), 123-124.

Synonyms

2-Propenamide, 3-[1-[[4-[(dimethylamino)methyl]phenyl]sulfonyl]-1H-pyrrol-3-yl]-N-hydroxy-, (2E)-

(2E)-3-[1-[[4-[(Dimethylamino)methyl]phenyl]sulfonyl]-1H-pyrrol-3-yl]-N-hydroxy-2-propenamide

(E)-3-[1-[[4-[(Dimethylamino)methyl]benzene]sulfonyl]-1H-pyrrol-3-yl]-N-hydroxyacrylamide

Resminostat

4SC 201