1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. PF-06826647

PF-06826647 

Cat. No.: HY-126290 Purity: 99.82%
Handling Instructions

PF-06826647 is an orally active and selective TYK2 inhibitor (IC50=17 nM), which binds to TYK2 catalytically active JH1 domain. PF-06826647 displays selectivity for TYK2 over JAK1 (IC50=383 nM) and JAK2 (74 nM). PF-06826647 can be used for the research of psoriasis, ulcerative colitis, and hidradenitis suppurativa.

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

PF-06826647 Chemical Structure

PF-06826647 Chemical Structure

CAS No. : 2127109-84-4

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5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 990 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2550 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

PF-06826647 is an orally active and selective TYK2 inhibitor (IC50=17 nM), which binds to TYK2 catalytically active JH1 domain. PF-06826647 displays selectivity for TYK2 over JAK1 (IC50=383 nM) and JAK2 (74 nM). PF-06826647 can be used for the research of psoriasis, ulcerative colitis, and hidradenitis suppurativa[1][2].

IC50 & Target

IC50: 17 nM (TYK2 JH1)[1]

In Vitro

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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-06826647 (30, 10, 3 mg/kg, p.o.; once per day) reduces clinical end points associated with the mouse imiquimod-induced skin inflammation model. The measured average unbound daily concentrations of 1, 3, 10, and 30 mg/kg are 14.5, 45.7, 225, and 668 nM, respectively, resulting in average IL-12 inhibition of 51, 77, 94, and 98%[2].
PF-06826647 (1 mg/kg; i.v.; sprague-Dawley rats) shows the systemic clearance is 12 (mL/min)/kg, the steady state volume of distribution (Vss) is 1.1 L/kg, and the AUCinf is 1380 ng•h/ mL[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

383.41

Formula

C₂₀H₁₇N₉

CAS No.

2127109-84-4

SMILES

N#CC[[email protected]@]1(N2N=CC(C3=NC(C4=CN(C)N=C4)=CN5C3=CC=N5)=C2)C[[email protected]@H](C#N)C1

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 : 16.67 mg/mL (43.48 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6082 mL 13.0409 mL 26.0817 mL
5 mM 0.5216 mL 2.6082 mL 5.2163 mL
10 mM 0.2608 mL 1.3041 mL 2.6082 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 1.67 mg/mL (4.36 mM); Clear solution

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

PF-06826647PF06826647PF 06826647JAKJanus kinasepsoriasisskininflammationselectiveoralInhibitorinhibitorinhibit

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Product Name:
PF-06826647
Cat. No.:
HY-126290
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