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Chemical Structure : PF-06700841
CAS No.: 1883299-62-4
Catalog No.: PC-61819Not For Human Use, Lab Use Only.
PF-06700841 (Brepocitinib, PF 06700841) is a potent dual JAK1/TYK2 inhibitor with IC50 of 17/23 nM, inhibits JAK2 and JAK3 with IC50=77 and 6494 nM, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $188 | In stock | |
| 25 mg | $328 | In stock | |
| 100 mg | $858 | In stock | |
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| 1 g | Get quote |
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PF-06700841 (Brepocitinib, PF 06700841) is a potent dual JAK1/TYK2 inhibitor with IC50 of 17/23 nM, inhibits JAK2 and JAK3 with IC50=77 and 6494 nM, respectively.
PF-06700841 potently inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (HWB IC50=65 and 120 nM, respectively).
PF-06700841 has good potency against IL6/pStat1 in the CD3+ cellular subset (IC50 = 81 nM), but lower inhibition of IL6/pSTAT3, again in the CD3+ cellular subset (IC50=641 nM).
PF-06700841 inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34+ progenitor cells (IC50=577 nM).
IL10/pSTAT3 (TYK2/JAK1) and IL27/pSTAT3 (JAK1/JAK2/TYK2) are also inhibited by PF-06700841 with IC50=305 nM and 86 nM, respectively.
PF-06700841 shows good selectivity against a broad panel of receptors with exception for kinase insert domain receptor (KDR) (VEGFR2) (IC50=1600 nM); shows therapeutic eggect in the rat adjuvant induced arthritis (AIA) following oral dosing.
| M.Wt | 389.411 | |
| Formula | C18H21F2N7O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
((S)-2,2-difluorocyclopropyl)(3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone |
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1. Banfield C, et al. J Clin Pharmacol. 2017 Dec 21. doi: 10.1002/jcph.1046.
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