A PRMT5 inhibitor
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PF-06855800

Item No. 43630

Technical Information
Formal Name
7-[(5R)-5-C-(4-chloro-3-fluorophenyl)-β-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
CAS Number
1989620-04-3
Molecular Formula
C17H16ClFN4O4
Formula Weight
Purity
≥98%
A solid
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
[H][C@]([C@H](O)C1=CC(F)=C(Cl)C=C1)(O[C@H]2N3C=CC4=C(N)N=CN=C43)[C@H]([C@H]2O)O
InChi Code
InChI=1S/C17H16ClFN4O4/c18-9-2-1-7(5-10(9)19)11(24)14-12(25)13(26)17(27-14)23-4-3-8-15(20)21-6-22-16(8)23/h1-6,11-14,17,24-26H,(H2,20,21,22)/t11-,12+,13-,14-,17-/m1/s1
InChi Key
GTCYWLXMJRCJNE-QFRSUPTLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    PF-06855800 is an inhibitor of protein arginine methyltransferase 5 (PRMT5; Ki = 11 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-06855800 inhibits the proliferation of A2780 ovarian cancer cells (IC50 = 3.3 nM). It also inhibits the asexual growth of P. falciparum in vitro when used at a concentration of 100 µM.2

    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 alSAM-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).

    2. Min, H., Lucky, A.B., Madsen, J.J., et alOnametostat, a PfPRMT5 inhibitor, exhibits antimalarial activity to Plasmodium falciparum. Antimicrob. Agents Chemother. 68(10), e0017624 (2024).