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PF-04965842

Cat. No. M8090
PF-04965842 Structure
Synonym:

Abrocitinib

Size Price Availability Quantity
5mg USD 250  USD250 In stock
10mg USD 405  USD405 In stock
25mg USD 720  USD720 In stock
50mg USD 1140  USD1140 In stock
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Quality Control & Documentation
Biological Activity

Abrocitinib is an orally active and selective JAK1 inhibitor with an IC50 value of 29 nM. Abrocitinib reversibly inhibits JAK1 kinase by blocking its ATP-binding site. Abrocitinib (PF-04965842) inhibited TYK2 activity (IC50, 1.253 μM) and phosphorylation of STAT1, STAT3, and STAT5 after stimulation. It can be used in the study of autoimmune diseases.

Chemical Information
Molecular Weight 323.41
Formula C14H21N5O2S
CAS Number 1622902-68-4
Solubility (25°C) DMSO ≥ 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] J I Silverberg, et al. Comparative efficacy and safety of systemic therapies used in moderate-to-severe atopic dermatitis: a systematic literature review and network meta-analysis

[2] Thomas Bieber, et al. Abrocitinib versus Placebo or Dupilumab for Atopic Dermatitis

[3] Novin Nezamololama, et al. Emerging systemic JAK inhibitors in the treatment of atopic dermatitis: a review of abrocitinib, baricitinib, and upadacitinib

[4] Krzysztof Szalus, et al. JAK-STAT Inhibitors in Atopic Dermatitis from Pathogenesis to Clinical Trials Results

[5] Megan Newsom, et al. New and Emerging Systemic Treatments for Atopic Dermatitis

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  Catalog
Abmole Inhibitor Catalog




Keywords: PF-04965842, Abrocitinib supplier, JAK, inhibitors, activators


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