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M-2433 Mocetinostat, Free Base, >99%      PLEASE INQUIRE FOR AVAILABILITY

[MG-0103] [MGCD0103] [MG 0103] [MG0103] [MGCD-0103] [MGCD 0103]

M.W. 396.44

C23H20N6O

[726169-73-9]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO.  Disposal:  A

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• Mocetinostat selectively inhibits histone deacetylases (HDACs) 1-3 and 11 at submicromolar concentrations.  It blocks cancer cell proliferation in vitro and has significant antitumor activity in vivo.  Zhou, N., et al.  "Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor."  J. Med. Chem. 51:  4072-4075 (2008).

• Mocetinostat induces hyperacetylation of histones, causes expression of the tumor suppressor protein p21(WAF1/CIP1), and inhibits proliferation of human cancer cells growing in culture.  Raeppel, S., et al.  "SAR and biological evaluation of analogues of a small molecule histone deacetylase inhibitor N-(2-aminophenyl)-4-((4-(pyridin-3-yl)pyrimidin-2-ylamino)methyl)benzamide (MGCD0103)."  Bioorg. Med. Chem. Lett. 19:  644-649 (2009).

• Mocetinostat demonstrated antitumor activity against hematological and lymphoproliferative cancers.  Le Tourneau, C. and Siu, L.L.  "Promising antitumor activity with MGCD0103, a novel isotype-selective histone deacetylase inhibitor."  Expert Opin. Investig. Drugs 17:  1247-1254 (2008).

• Mocetinostat dose-dependently inhibited HDAC activity in several human cancer cell lines and in human peripheral white blood cells.  The inhibitory effect of mocetinostat lasted for at least 8 hours in mice and 48 hours in patients with solid tumors.  Bonfils, C., et al.  "Evaluation of the pharmacodynamic effects of MGCD0103 from preclinical models to human using a novel HDAC enzyme assay."  Clin. Cancer Res. 14:  3441-3449 (2008).

• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.