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PF-06939999

Cat. No. M21075

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PF-06939999 Structure
Synonym:

PRMT5-IN-3

Price and Availability

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Quality Control & Documentation
Biological Activity

PF-06939999 (PRMT5-IN-3) is a PRMT5 inhibitor that is synthetically lethal to tumor cells in combination with DNA damaging agents.

Chemical Information
Molecular Weight 448.44
Formula C22H23F3N4O3
CAS Number 2159123-14-3
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Cen Guo, et al. CPT Pharmacometrics Syst Pharmacol. PK/PD model-informed dose selection for oncology phase I expansion: Case study based on PF-06939999, a PRMT5 inhibitor

[2] Kristen Jensen-Pergakes, et al. Mol Cancer Ther. SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance

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EPZ015666 is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.

SGC707

SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.

EPZ020411

EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has >10 fold selectivity for PRMT6 over PRMT1 and PRMT8.

XY1

XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), but XY1 is completely inactive.

  Catalog
Abmole Inhibitor Catalog




Keywords: PF-06939999, PRMT5-IN-3 supplier, PRMTs, inhibitors, activators

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