A PRMT5 inhibitor
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PF-06939999 (hydrochloride)

Item No. 44357

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1S,2S,3S,5R)-3-[[6-(difluoromethyl)-5-fluoro-1,2,3,4-tetrahydro-8-isoquinolinyl]oxy]-5-(4-methyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-1,2-cyclopentanediol, dihydrochloride
Synonyms
  • PRMT5-IN-3
  • PRMT5 Inhibitor 3
  • Protein Arginine Methyltransferase 5-IN-3
  • Protein Arginine Methyltransferase 5 Inhibitor 3
Molecular Formula
C22H23F3N4O3 • 2HCl
Formula Weight
521.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlWater: Slightly soluble: 0.1-1 mg/ml
SMILES
O[C@H]1[C@@H](C[C@@H]([C@H]1O)OC2=C3C(CCNC3)=C(C(C(F)F)=C2)F)N4C5=NC=NC(C)=C5C=C4.Cl.Cl
InChi Code
InChI=1S/C22H23F3N4O3.2ClH/c1-10-11-3-5-29(22(11)28-9-27-10)15-7-17(20(31)19(15)30)32-16-6-13(21(24)25)18(23)12-2-4-26-8-14(12)16;;/h3,5-6,9,15,17,19-21,26,30-31H,2,4,7-8H2,1H3;2*1H/t15-,17+,19+,20-;;/m1../s1
InChi Key
UGQRIWIWRZAVBW-LACPWWQDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $132

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    1 mg

    $251

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    Cayman Chemical
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    Product Description

    PF-06939999 is an inhibitor of protein arginine methyltransferase 5 (PRMT5; Ki = <5 pM).1 It is selective for PRMT5 over a panel of 22 additional protein methyltransferases and a panel of 40 kinases at 10 µM. PF-06939999 decreases global symmetric dimethyl arginine levels (IC50 = 1.1 nM) but does not affect histone methylation levels in A-427 non-small cell lung cancer (NSCLC) cells. In vivo, PF-06939999 (3, 10, and 30 mg/kg) reduces tumor volume in an A-427 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jensen-Pergakes, K., Tatlock, J., Maegley, K.A., et al. SAM-competitive PRMT5 inhibitor PF-06939999 demonstrates antitumor activity in splicing dysregulated NSCLC with decreased liability of drug resistance. Mol. Cancer Ther. 21(1), 3-15 (2022).