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C-2606 CI-994, Free Base, >99%

[Acetyldinaline] [Goe 5549] [Gö 5549] [PD 123654] [Tacedinaline] [CI 994] [CI994] [PD-123654] [PD123654] [Gö-5549] [Gö5549]

M.W. 269.30

C15H15N3O2

[112522-64-2]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 66 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 25-100 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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• CI-994 is a histone deacetylase (HDAC) inhibitor and induces histone hyperacetylation in living cells.  CI-994 inhibited HDAC-1 and HDAC-2 but not the prototypical histone acetyltransferase GCN5.  Kraker, A.J., et al.  "Modulation of histone acetylation by [4-(acetylamino)-N-(2-amino-phenyl) benzamide] in HCT-8 colon carcinoma."  Mol. Cancer Ther. 2:  401-408 (2003).

• CI-994 in combination with traditional anti-cancer agents cytarabine (ara-C), daunorubicin and mitoxantrone resulted in a synergistic effect against acute myeloid leukemia (AML).  Hubeek, I., et al.  "CI-994 (N-acetyl-dinaline) in combination with conventional anti-cancer agents is effective against acute myeloid leukemia in vitro and in vivo."  Oncol. Rep. 19:  1517-1523 (2008).

• CI-994 is a novel antitumor agent and had activity against 8 solid tumors tested including pancreatic ductal adenocarcinoma #02, pancreatic adenocarcinoma #03, colon adenocarcinoma #38, colon adenocarcinoma #51, mammary adenocarcinoma #25, mammary adenocarcinoma #17/ADR, Dunning osteogenic sarcoma and the human prostate carcinoma LNCaP.  LoRusso, P.M., et al.  "Preclinical antitumor activity of CI-994."  Invest. New Drugs 14:  349-356 (1996).

• CI-994 inhibited the growth of two non-small cell lung cancer (NSCLC) cell lines, A-549 (adenocarcinoma) and LX-1 (squamous cell carcinoma), with an IC50 of 80 µM.  It also showed synergism with standard anticancer agents such as gemcitabine and docetaxel.  Loprevite, M., et al.  "in vitro study of CI-994, a histone deacetylase inhibitor, in non-small cell lung cancer cell lines."  Oncol. Res. 15:  39-48 (2005).

• 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.