Tazemetostat

Synopsis, Chemistry

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Also known as: 1467052-75-0, Tazemetostat monohydrobromide, Epz-6438 monohydrobromide, E-7438 hydrobromide, Ez438, Tazemetostat (hydrobromide)

Molecular Formula

C₃₄H₄₅BrN₄O₄

Molecular Weight

653.6 g/mol

InChI Key

UQRICAQPWZSJNF-UHFFFAOYSA-N

FDA UNII

6P89T5M073

Tazemetostat Hydrobromide is the hydrobromide salt form of tazemetostat, an orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyl transferase EZH2, with potential antineoplastic activity. Upon oral administration, tazemetostat selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased tumor cell proliferation in EZH2 mutated cancer cells. EZH2, which belongs to the class of histone methyltransferases (HMTs), is overexpressed or mutated in a variety of cancer cells and plays a key role in tumor cell proliferation.

1 2D Structure

Tazemetostat

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide;hydrobromide

2.1.2 InChI

InChI=1S/C34H44N4O4.BrH/c1-5-38(29-10-14-41-15-11-29)32-20-28(27-8-6-26(7-9-27)22-37-12-16-42-17-13-37)19-30(25(32)4)33(39)35-21-31-23(2)18-24(3)36-34(31)40;/h6-9,18-20,29H,5,10-17,21-22H2,1-4H3,(H,35,39)(H,36,40);1H

2.1.3 InChI Key

UQRICAQPWZSJNF-UHFFFAOYSA-N

2.1.4 Canonical SMILES

CCN(C1CCOCC1)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C4=CC=C(C=C4)CN5CCOCC5.Br

2.2 Other Identifiers

2.2.1 UNII

6P89T5M073

2.3 Synonyms

2.3.1 MeSH Synonyms

1. (1,1'-biphenyl)-3-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2h-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-, Hydrobromide (1:2)

2. (1,1'-biphenyl)-3-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2h-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-, Hydrochloride (1:1)

3. E 7438

4. E-7438 Hydrobromide

5. E7438

6. Epz-6438

7. Epz-6438 Dihydrobromide

8. Epz-6438 Monohydrobromide

9. Epz-6438 Monohydrochloride

10. Epz-6438 Trihydrochloride

11. Ez-438

12. Ez438

13. N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(oxan-4-yl)amino)-4-methyl-4'-((morpholin-4-yl)methyl)(1,1'-biphenyl)-3-carboxamide

14. N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(oxan-4-yl)amino)-4-methyl-4'-((morpholin-4-yl)methyl)(1,1'-biphenyl)-3-carboxamide Monohydrobromide

15. Tazemetostat

16. Tazemetostat Dihydrobromide

17. Tazemetostat Hydrochloride

18. Tazemetostat Monohydrobromide

19. Tazemetostat Monohydrochloride

20. Tazemetostat Trihydrochloride

21. Tazverik

2.3.2 Depositor-Supplied Synonyms

1. 1467052-75-0

2. Tazemetostat Monohydrobromide

3. Epz-6438 Monohydrobromide

4. E-7438 Hydrobromide

5. Ez438

6. Tazemetostat (hydrobromide)

7. Epz-6438 Hydrobromide

8. Tazemetostat Hydrobromide [usan]

9. Tazverik

10. Ez-438

11. 6p89t5m073

12. (1,1'-biphenyl)-3-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2h-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-, Hydrobromide (1:1)

13. N-[(4,6-dimethyl-2-oxo-1h-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide;hydrobromide

14. Unii-6p89t5m073

15. Tazverik (tn)

16. 1467052-77-2

17. Chembl4594260

18. Schembl15313373

19. Dtxsid101027715

20. Hy-13803c

21. Tazemetostat Hydrobromide (jan/usan)

22. Tazemetostat Hydrobromide [jan]

23. Tazemetostat Hydrobromide [who-dd]

24. Epz-6438 Hydrobromide; Tazemetostat Hbr

25. Cs-0101826

26. D11485

27. Tazemetostat Hydrobromide [orange Book]

28. Q27265267

29. N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(oxan-4-yl)amino)-4-methyl-4'-((morpholin-4-yl)methyl)(1,1'-biphenyl)-3-carboxamide Monohydrobromide

30. 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 Hydrobromide

31. 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-carboxamidehydrobromide

2.4 Create Date

2013-11-04

3 Chemical and Physical Properties

Molecular Formula	C₃₄H₄₅BrN₄O₄
Molecular Weight	653.6 g/mol
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	9
Exact Mass	652.26242 g/mol
Monoisotopic Mass	652.26242 g/mol
Topological Polar Surface Area	83.1 Å²
Heavy Atom Count	43
Formal Charge	0
Complexity	992
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	2