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CAS No. | 864814-88-0 | Cat. No. | BCP02538 |
Name | Resminostat | ||
Synonyms | RAS2410;4SC-201;RAS 2410;RAS-2410;4SC201; | ||
SMILES | |||
Chemical Name | |||
Formula | C16H19N3O4S | M. Wt | 349.4 |
Purity | 98% | Storage | Store at 4-8°C |
Description | in vitro: Resminostat strongly induced apoptosis (IC50=2.5-3 micromol/l in 3 out of 4 MM cell lines) in MM cell lines as well as primary MM cells. At 1micromol/l, resminostat inhibited proliferation and induced G0/G1 cell cycle arrest in 3 out of 4 MM cell lines accompanied with decreased levels of cyclin D1, cdc25a, Cdk4 and pRb as well as upregulation of p21. Resminostat decreased phosphorylation of 4E-BP1 and p70S6k indicating an interference with Akt pathway signalling. Treatment with resminostat resulted in increased protein levels of Bim and Bax and decreased levels of Bcl-xL. Caspases 3, 8 and 9 were activated by resminostat. 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 1/2 of oral resminostat ranged from 2.7 to 4.4 hours. The modulation of plasma biomarkers further indicates drug activity. |
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