An MTA-cooperative PRMT5 inhibitor
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Vopimetostat

Item No. 46370

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(6-amino-5S-ethyl-3-pyridinyl)-5-methyl-2-[2R-(1-methyl-4-piperidinyl)-5-benzothiazolyl]-α-oxo-1-piperidineacetamide
CAS Number
2760483-96-1
Synonyms
  • TNG462
Molecular Formula
C28H36N6O2S
Formula Weight
520.7
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
CN(CC1)CCC1C2=NC3=CC([C@H]4CC[C@H](C)CN4C(C(NC5=CN=C(C(CC)=C5)N)=O)=O)=CC=C3S2
InChi Code
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
InChi Key
DHAGMIPSRSPWSH-GAJHUEQPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $98

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    10 mg

    $172

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    25 mg

    $306

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    Cayman Chemical
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    Product Description

    Vopimetostat is a methylthioadenosine-cooperative inhibitor of protein arginine methyltransferase 5 (PRMT5) that binds to the PRMT5-methylthioadenosine (MTA) complex (Ki = 300 fM).1 It decreases the viability of HAP1 chronic myeloid leukemia (CML) cells deficient in the gene encoding methylthioadenosine phosphorylase (MTAP; GI50 = 4 nM) with 30-fold selectivity over wild-type HAP1 cells. Vopimetostat decreases intratumoral protein-associated symmetric dimethylarginine levels and induces tumor regression in an MTAP-null Lu-99 non-small cell lung cancer (NSCLC) mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cottrell, K.M., Briggs, K.J., Tsai, A., et al. Discovery of TNG462: A highly potent and selective MTA cooperative PRMT5 inhibitor to target cancers with MTAP deletion. J Med. Chem. 68(5), 5097-5119 (2025).