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Brepocitinib (P-Tosylate)

Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. Brepocitinib P-Tosylate also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively[1].

Product Specifications

CAS Number

2140301-96-6

Product Name Alternative

PF-06700841 (P-Tosylate)

UNSPSC

12352005

Target

JAK

Type

Reference compound

Related Pathways

Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/PF-06700841_P-Tosylate.html

Concentration

10mM

Purity

99.98

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : 2 mg/mL (ultrasonic)

Smiles

O=C([C@H]1C(F)(F)C1)N2C3CN(C4=NC(NC5=CN(C)N=C5)=NC=C4)CC2CC3.O=S(C6=CC=C(C)C=C6)(O)=O

Molecular Formula

C25H29F2N7O4S

Molecular Weight

561.60

References & Citations

[1]Fensome A, et al. Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((S) -2,2-Difluorocyclopropyl) ((1 R,5 S) -3- (2- ((1-methyl-1 H-pyrazol-4-yl) amino) pyrimidin-4-yl) -3,8-diazabicyclo[3.2.1]octan-8-yl) methanone (PF-06700841) . J Med Chem. 2018 Oct 11;61 (19) :8597-8612.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

JAK1; JAK2; JAK3

Citation 01

Inflamm Bowel Dis. 2021 Oct 18;27 (10) :1674-1683.|Heliyon. 2023 Jan 13;9 (1) :e12958.|J Exp Clin Cancer Res. 2024 May 30;43 (1) :152.

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