A bioavailable PRMT5 inhibitor
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EPZ015666

Item No. 17285

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-4-pyrimidinecarboxamide
CAS Number
1616391-65-1
Synonyms
  • GSK3235025
Molecular Formula
C20H25N5O3
Formula Weight
383.4
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 10 mg/ml
λmax
246, 304 nm
SMILES
O=C(NC[C@H](O)CN1CCC(C=CC=C2)=C2C1)C3=CC(NC4COC4)=NC=N3
InChi Code
InChI=1S/C20H25N5O3/c26-17(10-25-6-5-14-3-1-2-4-15(14)9-25)8-21-20(27)18-7-19(23-13-22-18)24-16-11-28-12-16/h1-4,7,13,16-17,26H,5-6,8-12H2,(H,21,27)(H,22,23,24)/t17-/m0/s1
InChi Key
ZKXZLIFRWWKZRY-KRWDZBQOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $238

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    10 mg

    $392

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    25 mg

    $783

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    Cayman Chemical
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    Product Description

    EPZ015666 is a potent, orally bioavailable inhibitor of PRMT5 (Ki = 5 nM).1 It displays more than 20,000-fold selectivity for PRMT5 over other PMTs. EPZ015666 acts by blocking the association of PRMT5 with methylosome protein 50, which is necessary for the formation of an active methyltransferase complex. EPZ015666 (100 mg/kg twice daily) blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chan-Penebre, E., Kuplast, K.G., Majer, C.R., et al. A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. Nat. Chem. Biol. 11(6), 432-437 (2015).