An inhibitor of the PRMT5/MTA complex
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MRTX-1719

Item No. 36563

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2R)-2-[4-[4-(aminomethyl)-1,2-dihydro-1-oxo-6-phthalazinyl]-1-methyl-1H-pyrazol-5-yl]-4-chloro-6-(cyclopropyloxy)-3-fluoro-benzonitrile
CAS Number
2630904-45-7
Synonyms
  • BMS-986504
  • (M)-27
  • Navlimetostat
Molecular Formula
C23H18ClFN6O2
Formula Weight
464.9
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleDMSO: Soluble
SMILES
O=C1C(C=CC(C2=[C@]([C@]3=C(C#N)C(OC4CC4)=CC(Cl)=C3F)N(N=C2)C)=C5)=C5C(CN)=NN1
InChi Code
InChI=1S/C23H18ClFN6O2/c1-31-22(20-15(8-26)19(33-12-3-4-12)7-17(24)21(20)25)16(10-28-31)11-2-5-13-14(6-11)18(9-27)29-30-23(13)32/h2,5-7,10,12H,3-4,9,27H2,1H3,(H,30,32)
InChi Key
BZKIOORWZAXIBA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $191

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    5 mg

    $905

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    10 mg

    $1,142

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    Cayman Chemical
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    Product Description

    MRTX-1719 is an inhibitor of the protein arginine methyltransferase 5 (PRMT5) and methylthioadenosine (MTA) complex.1 It selectively binds to the PRMT5/MTA complex over the PRMT5 and S-adenosyl-L-methionine (SAM) complex (Kds = 0.14 and 9.4 pM, respectively). MRTX-1719 selectively decreases protein dimethylarginine methylation levels in MTAP-/- HCT116 colon cancer cells, which lack methylthioadenosine phosphorylase (MTAP; IC50 = 8 nM), over wild-type HCT116 cells (IC50 = 653 nM), as well as selectively reduces the viability of MTAP-/- HCT116 cells (IC50 = 12 nM) over wild-type HCT116 cells (IC50 = 890 nM). In vivo, MRTX-1719 (12.5-100 mg/kg per day) reduces tumor volume in an MTAP-/- Lu-99 lung cancer mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Smith, C.R., Aranda, R., Bobinski, T.P., et al. Fragment-based discovery of MRTX1719, a synthetic lethal inhibitor of the PRMT5•MTA complex for the treatment of MTAP-deleted cancers. J. Med. Chem. 65(3), 1749-1766 (2022).