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PF-06939999

Cat. No. M21075
PF-06939999 Structure
Synonym:

PRMT5-IN-3

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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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

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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  Catalog
Abmole Inhibitor Catalog




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


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