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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

MS-275

Cayman Chemical Item Number 13284

Entinostat; SNDX 275 (CAS 209783-80-2)

MS-275 (CAS 209783-80-2)

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Description

MS-275 is an inhibitor of histone deacetylases (HDACs) that preferentially inhibits HDAC1 (IC50 = 300 nM) over HDAC3 (IC50 = 8 μM).1 However, it does not inhibit HDAC8 (IC50 > 100 μM).1 MS-275 induces cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1), slowing cell growth, differentiation, and tumor development in vivo.23 Recent studies suggest that MS-275 may be particularly useful as an antineoplastic agent when combined with other drugs, like adriamycin,4 inhibitors of poly (ADP-ribose) polymerase (PARP),5 or inhibitors of heat shock protein 90 (Hsp90).6

1 Hu, E., Dul, E., Sung, C., et al. Identification of novel isoform-selective inhibitors within class I histone deacetylases. J Pharmacol Exp Ther 307 720-728 (2003).

2 Saito, A., Yamashita, T., Mariko, Y., et al. A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors. Proc Natl Acad Sci USA 96 4592-4597 (1999).

3 Jaboin, J., Wild, J., Hamidi, H., et al. MS-27-275, an inhibitor of histone deacetylase, has marked in vitro and in vivo antitumor activity against pediatric solid tumors. Cancer Res 62 6108-6115 (2002).

4 Xu, J., Zhou, J., Wei, W., et al. Sp1-mediated TRAIL induction in chemosensitization. Cancer Res 68(16) 6718-6726 (2008).

5 Gaymes, T.J., Shall, S., Macpherson, L.J., et al. Inhibitors of poly ADP-ribose polymerase (PARP) induce apoptosis of myeloid leukemic cells: potential for therapy of myeloid leukemia and myelodysplastic syndromes. Haematologica 94 638-646 (2009).

6 Nguyen, A., Su, L., Campbell, B., et al. Synergism of heat shock protein 90 and histone deacetylase inhibitors in synovial sarcoma. Sarcoma (2009).

Synonyms
  • Entinostat
  • SNDX 275
Formal Name N-​[[4-​[[(2-​aminophenyl)amino]carbonyl]phenyl]methyl]-​3-​pyridinylmethyl ester,​ carbamic acid
CAS Number 209783-80-2
Molecular Formula C21H20N4O3
Formula Weight 376.4
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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O=C(NCC1=CC=C(C(NC2=C(N)​C=CC=C2)​=O)​C=C1)​OCC3=CC=CN=C3

MS-275 is available in the following screening libraries:

Size Price Quantity Subtotal
1 mg $16.00 $0.00
5 mg $64.00 $0.00
10 mg $96.00 $0.00
25 mg $180.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-02-11. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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