Entinostat (MS-275) -- HDAC Inhibitor


Catalog No. size PriceQuantity
M60174-5S 5mg solid $79
M60174-10S 10 mg solid $316

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.

Product information

CAS Number: 209783-80-2

Molecular Weight: 376.41

Formula: C21H20N4O3

Synonym:

MS-275

Chemical Name: pyridin-3-ylmethyl 4-((2-aminophenyl)carbamoyl)benzylcarbamate

Smiles: NC1=CC=CC=C1NC(=O)C1C=CC(CNC(=O)OCC2=CC=CN=C2)=CC=1

InChiKey: 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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Entinostat (MS-275) was used at 1 µM final concentration in vitro and in cellular assays.

In Vivo:

Entinostat (MS-275) was orally dosed to mice at 49 mg/kg once daily 5 days per week for 4 weeks in the xenograft tumor model.

References:

  1. Saito A, et al. A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors. (1999) Proc Natl Acad Sci USA. 96(8):4592-7.
  2. Rosato RR, et al.The histone deacetylase inhibitor MS-275 promotes differentiation or apoptosis in human leukemia cells through a process regulated by generation of reactive oxygen species and induction of p21CIP1/WAF1 1. (2003) Cancer Res. 63(13):3637-45.
  3. Kato Y, et al. Synergistic in vivo antitumor effect of the histone deacetylase inhibitor MS-275 in combination with interleukin 2 in a murine model of renal cell carcinoma. (2007) Clin Cancer Res. 13(15 Pt 1):4538-46.

Products are for research use only. Not for human use.


Documents

Payment & Security

American Express Diners Club Discover JCB Mastercard PayPal Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed