M-2433 Mocetinostat, Free Base, >99%

Synonyms : [MG-0103] [MGCD0103]

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  • 25 mg
  • 58
  • 47
  • 42
  • 6,000
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  • 50 mg
  • 99
  • 81
  • 72
  • 10,300
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  • 100 mg
  • 159
  • 131
  • 116
  • 16,500
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  • 200 mg
  • 287
  • 236
  • 210
  • 29,800
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  • 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, medical, 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.
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