1: Knutson SK, Kawano S, Minoshima Y, Warholic NM, Huang KC, Xiao Y, Kadowaki T, Uesugi M, Kuznetsov G, Kumar N, Wigle TJ, Klaus CR, Allain CJ, Raimondi A, Waters NJ, Smith JJ, Porter-Scott M, Chesworth R, Moyer MP, Copeland RA, Richon VM, Uenaka T, Pollock RM, Kuntz KW, Yokoi A, Keilhack H. Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma. Mol Cancer Ther. 2014 Apr;13(4):842-54. doi: 10.1158/1535-7163.MCT-13-0773. PubMed PMID: 24563539.
2: Kurmasheva RT, Sammons M, Favours E, Wu J, Kurmashev D, Cosmopoulos K, Keilhack H, Klaus CR, Houghton PJ, Smith MA. Initial testing (stage 1) of tazemetostat (EPZ-6438), a novel EZH2 inhibitor, by the Pediatric Preclinical Testing Program. Pediatr Blood Cancer. 2017 Mar;64(3). doi: 10.1002/pbc.26218. PubMed PMID: 27555605.
3: Wiese M, Schill F, Sturm D, Pfister S, Hulleman E, Johnsen SA, Kramm CM. No Significant Cytotoxic Effect of the EZH2 Inhibitor Tazemetostat (EPZ-6438) on Pediatric Glioma Cells with Wildtype Histone 3 or Mutated Histone 3.3. Klin Padiatr. 2016 Apr;228(3):113-7. doi: 10.1055/s-0042-105292. PubMed PMID: 27135271.
4: Baker T, Nerle S, Pritchard J, Zhao B, Rivera VM, Garner A, Gonzalvez F. Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors. Oncotarget. 2015 Oct 20;6(32):32646-55. doi: 10.18632/oncotarget.5066. PubMed PMID: 26360609; PubMed Central PMCID: PMC4741719.
5: Zhang P, de Gooijer MC, Buil LC, Beijnen JH, Li G, van Tellingen O. ABCB1 and ABCG2 restrict the brain penetration of a panel of novel EZH2-Inhibitors. Int J Cancer. 2015 Oct 15;137(8):2007-18. doi: 10.1002/ijc.29566. PubMed PMID: 25868794.
6: Xia B, Gerstin E, Schones DE, Huang W, Steven de Belle J. Transgenerational programming of longevity through E(z)-mediated histone H3K27 trimethylation in Drosophila. Aging (Albany NY). 2016 Nov 25;8(11):2988-3008. doi: 10.18632/aging.101107. PubMed PMID: 27889707; PubMed Central PMCID: PMC5191882.
7: Knutson SK, Warholic NM, Johnston LD, Klaus CR, Wigle TJ, Iwanowicz D, Littlefield BA, Porter-Scott M, Smith JJ, Moyer MP, Copeland RA, Pollock RM, Kuntz KW, Raimondi A, Keilhack H. Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas. PLoS One. 2014 Dec 10;9(12):e111840. doi: 10.1371/journal.pone.0111840. PubMed PMID: 25493630; PubMed Central PMCID: PMC4262195.
8: Adhikary G, Grun D, Balasubramanian S, Kerr C, Huang JM, Eckert RL. Survival of skin cancer stem cells requires the Ezh2 polycomb group protein. Carcinogenesis. 2015 Jul;36(7):800-10. doi: 10.1093/carcin/bgv064. PubMed PMID: 25969142; PubMed Central PMCID: PMC4580538.
9: Momparler RL, Côté S. Targeting of cancer stem cells by inhibitors of DNA and histone methylation. Expert Opin Investig Drugs. 2015;24(8):1031-43. doi: 10.1517/13543784.2015.1051220. Review. PubMed PMID: 26004134.
10: Edfeldt K, Hellman P, Westin G, Stalberg P. A plausible role for actin gamma smooth muscle 2 (ACTG2) in small intestinal neuroendocrine tumorigenesis. BMC Endocr Disord. 2016 Apr 23;16:19. doi: 10.1186/s12902-016-0100-3. PubMed PMID: 27107594; PubMed Central PMCID: PMC4841950.
11: Kim KH, Roberts CW. Targeting EZH2 in cancer. Nat Med. 2016 Feb;22(2):128-34. doi: 10.1038/nm.4036. Review. PubMed PMID: 26845405; PubMed Central PMCID: PMC4918227.
12: Huang Y, Zhang J, Yu Z, Zhang H, Wang Y, Lingel A, Qi W, Gu XJ, Zhao K, Shultz MD, Wang L, Fu X, Sun Y, Zhang Q, Jiang X, Zhang JW, Zhang C, Li L, Zeng J, Feng L, Zhang C, Liu Y, Zhang M, Zhang L, Zhao M, Gao Z, Liu X, Fang D, Guo H, Mi Y, Gabriel T, Dillon MP, Atadja P, Oyang C. Discovery of First-in-Class, Potent and Orally Bioavailable EED inhibitor with Robust Anti-cancer Efficacy. J Med Chem. 2017 Jan 16. doi: 10.1021/acs.jmedchem.6b01576. [Epub ahead of print] PubMed PMID: 28092155.
13: Fisher ML, Adhikary G, Grun D, Kaetzel DM, Eckert RL. The Ezh2 polycomb group protein drives an aggressive phenotype in melanoma cancer stem cells and is a target of diet derived sulforaphane. Mol Carcinog. 2016 Dec;55(12):2024-2036. doi: 10.1002/mc.22448. PubMed PMID: 26693692; PubMed Central PMCID: PMC4919248.
14: Chen JF, Luo X, Xiang LS, Li HT, Zha L, Li N, He JM, Xie GF, Xie X, Liang HJ. EZH2 promotes colorectal cancer stem-like cell expansion by activating p21cip1-Wnt/β-catenin signaling. Oncotarget. 2016 Jul 5;7(27):41540-41558. doi: 10.18632/oncotarget.9236. PubMed PMID: 27172794; PubMed Central PMCID: PMC5173077.
15: Yan W, Herman JG, Guo M. Epigenome-based personalized medicine in human cancer. Epigenomics. 2016 Jan;8(1):119-33. doi: 10.2217/epi.15.84. Review. PubMed PMID: 26344672.

Chemical
CAS Num	1403254-99-8
Chemical Formula	C34H44N4O4
Molecular Weight	572.74
IUPAC Chemical Name	N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide
Exact Mass	572.33626
Elemental Analysis	C, 71.30; H, 7.74; N, 9.78; O, 11.17
Synonym	EPZ-6438; EPZ 6438; EPZ6438; E7438; E-7438; E 7438; Tazemetostat
Solubility	Soluble in DMSO, not in water
SMILES Code	O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC(N(CC)C4CCOCC4)=C1C)NCC5=C(C)C=C(C)NC5=O
Biological
Targets and Effects	N/A
Pathways	Apoptosis
Physical
Appearance	Solid powder
Purity	>98% (or refer to the Certificate of Analysis)
Shipping Condition	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition	Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf Life	>2 years if stored properly