DATASHEET
Formulation
Powder
Storage:
Store in dry, dark place at -20C for 1 year.
Product Information:
Molecular Weight: 376.41
Formula: C21 H20 N4 O3
CAS Number: 209783-80-2
InChi Key: INVTYAOGFAGBOE-UHFFFAOYSA-N
InChi: InChI=1S/C21H20N4O3/c22-18-5-1-2-6-19(18)25-20(26)17-9-7-15(8-10-17)13-24-21(27)28-14-16-4-3-11-23-12-16/h1-12H,13-14,22H2,(H,24,27)(H,25,26)
Smiles: NC1C=CC=CC=1NC(=O)C1C=CC(CNC(=O)OCC2=CC=CN=C2)=CC=1
Purity: 98.0
Solubility: DMSO up to 100 mM
Appearance: Solid Power.
Shelf Life: 1.0 years
Description:
Entinostat (MS-275) is a potent and selective HDAC inhibitor. It inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, but not the other HDACs 4, 6, 8, and 10 (IC50 > 100 µM). MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. It was shown to reduce S-phase cells and induce G1-phase cells in A2780 cells. MS-275 shows great inhibition to human leukemia and lymphoma cells, decreases expression of cyclin D1 and the anti-apoptotic proteins Mcl-1 and XIAP. In vivo MS-275 exhibits great antitumor activity against human tumor xenografts. Currently it is in Phase II/III clinical trials for Hodgkin's lymphoma and advanced breast cancer.