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CAS No. : 2140301-96-6
MCE 国际站:Brepocitinib P-Tosylate
产品活性:Brepocitinib (PF-06700841) P-Tosylate 是一种有效的 JAK1 和 TYK2 双重抑制剂, IC50 值分别为 17 nM 和 23 nM。Brepocitinib P-Tosylate 还分别以 IC50 值为 77 nM 和 6.49 μM 抑制 JAK2 和 JAK3。
研究领域:Epigenetics | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Stem Cell/Wnt
作用靶点:JAK
In Vitro: Brepocitinib (Compound 23) potently inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (human whole blood (HWB) IC50s of 65 and 120 nM, respectively). Brepocitinib has good potency against IL6/pStat1 in the CD3+ cellular subset (IC50 of 81 nM), but lower inhibition of IL6/pSTAT3, again in the CD3+ cellular subset (IC50 of 641 nM). Brepocitinib also inhibits the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency (HWB IC50s of 238 and 204 nM, respectively). Brepocitinib inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34+ progenitor cells (IC50 of 577 nM). IL10/pSTAT3 (TYK2/JAK1) and IL27/pSTAT3 (JAK1/JAK2/TYK2) are also inhibited by Brepocitinib with IC50s of 305 nM and 86 nM, respectively.
In Vivo: Brepocitinib (Compound 23; 3-30 mg/kg; oral administration; for 7 consecutive days; female Lewis rats) treatment significantly reduces paw volume increase in a dose-dependent manner. The plasma concentrations in animals dosed with Brepocitinib at peak (30 min) and trough (24 h) time intervals post final dose respectively are as follows: 3 mg/kg, 3.54 μM, 0.0221 μM; 10 mg/kg, 10.95 μM, 0.06 μM; and 30 mg/kg, 23.89 μM, 0.06 μM.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Epigenetics Compound Library | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Stem Cell Signaling Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Obesity Compound Library | Anti-Liver Cancer Compound Library | Rare Diseases Drug Library | Anti-Prostate Cancer Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Pain-Related Compound Library | JAK-IN-20 | JAK1-IN-9 | AT9283 | RO495 | TK4b | JAK-IN-17 | (E/Z)-Zotiraciclib | JAK-IN-10 | (3R,4S)-Tofacitinib | JAK3/BTK-IN-6 | Tyk2-IN-5 | Brevilin A | Broussonin E | Itacnosertib | RO8191 | Axltide | Fosifidancitinib | JAK3-IN-6 | Upadacitinib | JAK-IN-24 | AZD-1480 | Baricitinib-d3 | Tofacitinib-13C3 | AZ-3 | Delphinidin chloride | TK4g | Tofacitinib Prodrug-1
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