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E-3866 Entinostat, Free Base, >99%

[MS-27-275] [MS 275-27] [MS-275] [Histone Deacetylase Inhibitor I] [SNDX-275] [MS 275] [MS275] [PD-123654] [SNDX 275] [SNDX275]

M.W. 376.41

C21H20N4O3

[209783-80-2]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 25 mg/mL with slight warming; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20 µM buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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• Entinostat is a synthetic benzamide derivative that inhibited partially purified human histone deacetylase (HDA) with an IC50 of 2 µM and induced hyperacetylation of nuclear histones in tumor cell lines.  Entinostat inhibited the proliferation of various human tumor cell lines such as A2780, Calu-3, HL-60, and K562 (IC50 values were 0.0415 µM, 0.195 µM, 0.212 µM, and 0.589 µM, respectively).  Entinostat also inhibited the growth of human tumor xenografts in nude mouse.  Saito, A., 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).

• Entinostat inhibits tumor growth by inducing tumor suppressors p21WAF1/CIP1 and gelsolin through acetylation of histones and changing the cell cycle distribution, decrease of S-phase cells and increase of G1-phase cells.  Saito, A., 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).

• Entinostat inhibited the proliferation of human breast cancer cells by inducing the expression of transforming growth factor (TGF)-β type II receptor (TβRII) mRNA, but not TGF-beta type I receptor mRNA.  Lee, B.I., et al.  "MS-275, a histone deacetylase inhibitor, selectively induces transforming growth factor beta type II receptor expression in human breast cancer cells."  Cancer Res. 61:  931-934 (2001).

• Entinostat inhibited the proliferation of four glioma cell lines (U87MG, C6, F98, and SMA-560) with an IC90 of 3.75 µM.  Its antiproliferative effect was mediated by G0-G1 cell cycle arrest and apoptosis.  Eyüpoglu, I.Y., et al.  "Experimental therapy of malignant gliomas using the inhibitor of histone deacetylase MS-275."  Mol. Cancer Ther. 5:  1248-1255 (2006).

• The toxicities of entinostat in patients included infections and neurologic toxicity, fatigue, anorexia, nausea, vomiting, hypoalbuminemia, and hypocalcemia.  Gojo, I., et al.  "Phase 1 and pharmacologic study of MS-275, a histone deacetylase inhibitor, in adults with refractory and relapsed acute leukemias."  Blood 109:  2781-2790 (2007).

• Entinostat demonstrated dramatic anti-rheumatic activities in both mouse and rat collagen induced arthritis (CIA) models.  Lin, H.S., et al.  "Anti-rheumatic activities of histone deacetylase (HDAC) inhibitors in vivo in collagen-induced arthritis in rodents."  Br. J. Pharmacol. 150:  862-872 (2007).

• The combination treatment of PC-3 prostate cancer cells or tumors with retinoic acid metabolism-blocking agent (RAMBA) VN/66-1 and entinostat resulted in a significant inhibition in cell proliferation and tumor volume compared with control and was more effective than either drug alone.  Khandelwal, A., et al.  "MS-275 synergistically enhances the growth inhibitory effects of RAMBA VN/66-1 in hormone-insensitive PC-3 prostate cancer cells and tumours."  Br. J. Cancer 98:  1234-1243 (2008).

• Another CAS number previously assigned to entinostat, 442532-99-2, has been deleted by CAS and is no longer in use.

• 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.