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PF-06826647

Cat. No. M9930
PF-06826647 Structure
Synonym:

Tyk2-IN-8

Size Price Availability Quantity
5mg USD 490.5  USD545 In stock
10mg USD 765  USD850 In stock
25mg USD 1287  USD1430 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PF-06826647, also known as Tyk2-IN-8, is a selective and orally administered tyrosine kinase 2 (TYK2) inhibitor, with IC50 of 17 nM. PF-06826647 inhibits a panel of 231 kinases at non-physiologically conditions for each kinase Km showed 21 non-JAK kinases with >50% at 1 μM dose. PF-06826647 inhibits ear swelling in the imiquimod-induced skin inflammation model.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 383.41
Formula C20H17N9
CAS Number 2127109-84-4
Purity >99%
Solubility DMSO 20 mg/mL
Storage at -20°C
References

Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases
Brian S Gerstenberger, et al. J Med Chem. 2020 Nov 25;63(22):13561-13577. PMID: 32787094.

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165
Stephen T Wrobleski, et al. J Med Chem. 2019 Oct 24;62(20):8973-8995. PMID: 31318208.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-06826647, Tyk2-IN-8 supplier, JAK, inhibitors

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