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PF-06855800

Chemical Structure : PF-06855800

CAS No.: 1989620-04-3

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PF-06855800 (PF06855800)

Catalog No.: PC-35520Not For Human Use, Lab Use Only.

PF-06855800 (PF06855800) is a potent, selective, SAM competitive, BBB-penetrant, orally active inhibitor of protein arginine methyltransferase PRMT5 with Ki of 0.02 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PF-06855800 (PF06855800) is a potent, selective, SAM competitive, BBB-penetrant, orally active inhibitor of protein arginine methyltransferase PRMT5 with Ki of 0.02 nM.
PF-06855800 demonstrates antiproliferative activity in Z-138 cancer cells with IC50 of 1 nM,
PF-06855800 also shows anti-tumor activity in Z-138 mice xenograft models.

Physicochemical Properties

M.Wt 392.811
Formula C19H18ClFN2O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(2R,3S,4R,5R)-2-((R)-(4-chloro-3-fluorophenyl)(hydroxy)methyl)-5-(4-methyl-1H-pyrrolo[3,2-c]pyridin-1-yl)tetrahydrofuran-3,4-diol

References

1. Indrawan J. Mcalpine, et al. Abstract 4857: Discovery of PF-06855800, a SAM competitive PRMT5 inhibitor with potent antitumor activity. DOI: 10.1158/1538-7445.AM2018-4857. AACR 2018.

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