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Also known as: Tng-462, 2760483-96-1, Tng462, A1bv0, N-(6-amino-5-ethylpyridin-3-yl)-2-[(2r,5s)-5-methyl-2-[2-(1-methylpiperidin-4-yl)-1,3-benzothiazol-5-yl]piperidin-1-yl]-2-oxoacetamide, N-(6-amino-5-ethylpyridin-3-yl)-2-{(2r,5s)-5-methyl-2-[2-(1-methylpiperidin-4-yl)-1,3-benzothiazol-5-yl]piperidin-1-yl}-2-oxoacetamide

Molecular Formula

C₂₈H₃₆N₆O₂S

Molecular Weight

520.7 g/mol

InChI Key

DHAGMIPSRSPWSH-GAJHUEQPSA-N

FDA UNII

54P82QYL4L

Vopimetostat is an orally bioavailable small molecule inhibitor of protein arginine methyltransferase 5 (PRMT5), with potential antiproliferative and antineoplastic activities. Upon oral administration, vopimetostat selectively targets, binds to, and inhibits the activity of PRMT5. By inhibiting its methyltransferase activity, levels of both monomethylated and dimethylated arginine residues in histones H2A, H3 and H4 are decreased. This modulates the expression of genes involved in several cellular processes, including cellular proliferation. This may increase the expression of antiproliferative genes and/or decrease the expression of genes that promote cell proliferation, which may lead to decreased growth of rapidly proliferating cells, including cancer cells. PRMT5, a type II methyltransferase that catalyzes the formation of both omega-N monomethylarginine (MMA) and symmetric dimethylarginine (sDMA) on histones and a variety of other protein substrates involved in signal transduction and cellular transcription, is overexpressed in several neoplasms and is essential for the viability of cancer and normal cells. Elevated levels are associated with decreased patient survival. Methylthioadenosine phosphorylase (MTAP) is deleted in certain cancer cells leading to an accumulation of methylthioadenosine (MTA). As MTA binds to and partially inhibits PRMT5, MTAP-null cancer cells are specifically sensitive to PRMT5 inhibitors. This may spare normal, healthy cells that are without MTAP-deletions and lower systemic toxicity.

1 2D Structure

Vopimetostat

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

N-(6-amino-5-ethyl-3-pyridinyl)-2-[(2R,5S)-5-methyl-2-[2-(1-methylpiperidin-4-yl)-1,3-benzothiazol-5-yl]piperidin-1-yl]-2-oxoacetamide

2.1.2 InChI

InChI=1S/C28H36N6O2S/c1-4-18-13-21(15-30-25(18)29)31-26(35)28(36)34-16-17(2)5-7-23(34)20-6-8-24-22(14-20)32-27(37-24)19-9-11-33(3)12-10-19/h6,8,13-15,17,19,23H,4-5,7,9-12,16H2,1-3H3,(H2,29,30)(H,31,35)/t17-,23+/m0/s1

2.1.3 InChI Key

DHAGMIPSRSPWSH-GAJHUEQPSA-N

2.2 Other Identifiers

2.2.1 UNII

54P82QYL4L

2.3 Synonyms

2.3.1 Depositor-Supplied Synonyms

1. Tng-462

2. 2760483-96-1

3. Tng462

4. A1bv0

5. N-(6-amino-5-ethylpyridin-3-yl)-2-[(2r,5s)-5-methyl-2-[2-(1-methylpiperidin-4-yl)-1,3-benzothiazol-5-yl]piperidin-1-yl]-2-oxoacetamide

6. N-(6-amino-5-ethylpyridin-3-yl)-2-{(2r,5s)-5-methyl-2-[2-(1-methylpiperidin-4-yl)-1,3-benzothiazol-5-yl]piperidin-1-yl}-2-oxoacetamide

7. Vopimetostat [inn]

8. 54p82qyl4l

9. Orb2277604

10. Schembl24364686

11. Schembl31057907

12. Gtpl12902

13. Glxc-27708

14. Ex-a7971

15. Nsc856534

16. At42401

17. Nsc-856534

18. Da-68242

19. Sy370249

20. Hy-156680

21. Cs-0889154

22. (2r,5s)-n-(6-amino-5-ethyl-3-pyridinyl)-5-methyl-2-[2-(1-methyl-4-piperidinyl)- 5-benzothiazolyl]-+/--oxo-1-piperidineacetamide

23. (2r,5s)-n-(6-amino-5-ethyl-3-pyridinyl)-5-methyl-2-[2-(1-methyl-4-piperidinyl)-5-benzothiazolyl]-alpha-oxo-1-piperidineacetamide

24. 1-piperidineacetamide, N-(6-amino-5-ethyl-3-pyridinyl)-5-methyl-2-[2-(1-methyl-4-piperidinyl)-5-benzothiazolyl]-alpha-oxo-, (2r,5s)-

25. N-(6-amino-5-ethyl-3-pyridyl)-2-[(2r,5s)-5-methyl-2-[2-(1-methyl-4-piperidyl)benzo[d]thiazol-5-yl]-1-piperidyl]-2-oxoacetamide

2.4 Create Date

2022-08-27

3 Chemical and Physical Properties

Molecular Formula	C₂₈H₃₆N₆O₂S
Molecular Weight	520.7 g/mol
XLogP3	4.3
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	4
Exact Mass	Da
Monoisotopic Mass	Da
Topological Polar Surface Area	133
Heavy Atom Count	37
Formal Charge	0
Complexity	808
Isotope Atom Count	0
Defined Atom Stereocenter Count	2
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1