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Chemical Structure : PF-06939999
CAS No.: 2159123-14-3
Catalog No.: PC-72513Not For Human Use, Lab Use Only.
PF-06939999 (PF06939999) is a potent, selective, S-adenosylmethionine (SAM) competitive PRMT5 inhibitor with SPR Kd of 5.8 pM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $188 | In stock | |
| 5 mg | $298 | In stock | |
| 10 mg | $478 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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PF-06939999 (PF06939999) is a potent, selective, S-adenosylmethionine (SAM) competitive PRMT5 inhibitor with SPR Kd of 5.8 pM.
PF-06939999 displays at least one million-fold selective for PRMT5 over a panel of protein methyltransferases and 20 diverse protein kinases.
PF-06939999 demonstrates dose-dependent reduction of symmetric dimethyl arginine (SDMA) and an antiproliferative response in A2780 cells (IC50=3.3 nM).
PF-06939999 showed dose-dependent loss of SDMA on several proteins, with a cellular IC50 1.1 nM in A427 cells.
PF-06939999 demonstrates tumor growth inhibition in splicing mutant NSCLC (oral 3, 10, and 30 mg/kg).
| M.Wt | 448.446 | |
| Formula | C22H23F3N4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(1S,2S,5R)-3-((6-(difluoromethyl)-5-fluoro-1,2,3,4-tetrahydroisoquinolin-8-yl)oxy)-5-(4-methyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol |
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1. Kristen Jensen-Pergakes, et al. Mol Cancer Ther. 2022 Jan;21(1):3-15.
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