1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK

Abrocitinib (Synonyms: PF-04965842)

Cat. No.: HY-107429 Purity: 98.11%
Handling Instructions

Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease.

For research use only. We do not sell to patients.

Abrocitinib Chemical Structure

Abrocitinib Chemical Structure

CAS No. : 1622902-68-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Description

Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease[1].

IC50 & Target[1]

JAK1

29 nM (IC50)

JAK2

803 nM (IC50)

Tyk2

1253 nM (IC50)

In Vitro

Abrocitinib (Compound 25) inhibits IFNα-stimulated phosphorylation of STAT3, IFN-stimulated phosphorylation of STAT1 in human whole blood (HWB), as well as pSTAT5 in CD34+ spiked into HWB (JAK2), with IC50s of 189, 163 nM, 7.178 μM, respectively[1].

In Vivo

Abrocitinib (Compound 25; 5, 15, 50 mg/kg, p.o., daily for 7 days) significantly reduces paw swelling in rat adjuvant-induced arthritis model[1].

Animal Model: Female Lewis rats (8−10 weeks old)[1]
Dosage: 5, 15, 50 mg/kg
Administration: P.O. daily for 7 days
Result: Obviously reduced paw swelling at all doses.
References
Molecular Weight

323.41

Formula

C₁₄H₂₁N₅O₂S

CAS No.

1622902-68-4

SMILES

CN([[email protected]]1C[[email protected]@H](NS(CCC)(=O)=O)C1)C2=C3C(NC=C3)=NC=N2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Abrocitinib
Cat. No.:
HY-107429
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Abrocitinib

Cat. No.: HY-107429