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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-PF-06700841 tosylate
PF-06700841 tosylate

Chemical Structure : PF-06700841 tosylate

CAS No.: 2140301-96-6

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PF-06700841 tosylate (Brepocitinib tosylate, PF-6700841, PF-841)

货号: PC-61818Not For Human Use, Lab Use Only.

PF-06700841 tosylate (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.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PF-06700841 tosylate (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.

物理化学性质&存储条件

分子量 561.609
分子式 C25H29F2N7O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
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 4-methylbenzenesulfonate

参考文献

1. Banfield C, et al. J Clin Pharmacol. 2017 Dec 21. doi: 10.1002/jcph.1046.

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