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    Vopimetostat

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    2D Structure
    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

    2D Structure

    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 Weight 520.7 g/mol
    Molecular Formula C28H36N6O2S
    XLogP34.3
    Hydrogen Bond Donor Count2
    Hydrogen Bond Acceptor Count7
    Rotatable Bond Count4
    Exact Mass Da
    Monoisotopic Mass Da
    Topological Polar Surface Area133
    Heavy Atom Count37
    Formal Charge0
    Complexity808
    Isotope Atom Count0
    Defined Atom Stereocenter Count2
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1