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

Abrocitinib (Synonyms: PF-04965842)

Cat. No.: HY-107429 Purity: 99.79%
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
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Based on 1 publication(s) in Google Scholar

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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.
Clinical Trial
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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (386.51 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0921 mL 15.4603 mL 30.9205 mL
5 mM 0.6184 mL 3.0921 mL 6.1841 mL
10 mM 0.3092 mL 1.5460 mL 3.0921 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (6.43 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.43 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.43 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.79%

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Abrocitinib
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HY-107429
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