1. IRAK
  2. PF-06650833

PF-06650833 

Cat. No.: HY-19836 Purity: 99.71%
Handling Instructions

PF-06650833 is a potent, selective and orally active inhibitor of interleukin-1 receptor associated kinase 4 (IRAK4) with IC50s of 0.2 and 2.4 nM in the cell and PBMC assay, respectively. PF-06650833 is used to treat diseases such as rheumatoid arthritis, lupus, and lymphomas.

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

PF-06650833 Chemical Structure

PF-06650833 Chemical Structure

CAS No. : 1817626-54-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 86 In-stock
Estimated Time of Arrival: December 31
5 mg USD 78 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 648 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1152 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

PF-06650833 is a potent, selective and orally active inhibitor of interleukin-1 receptor associated kinase 4 (IRAK4) with IC50s of 0.2 and 2.4 nM in the cell and PBMC assay, respectively. PF-06650833 is used to treat diseases such as rheumatoid arthritis, lupus, and lymphomas[1][2].

IC50 & Target[1]

IRAK4

0.2 nM (IC50)

In Vitro

The kinome selectivity profile of PF-06650833 (Compound 40) is assessed in a panel of 278 kinases (Invitrogen) at 200 nM inhibitor concentration using the ATP Km for each kinase. Approximately 100% inhibition is observed for IRAK4[1].
Lactam PF-06650833 (Compound 40) is assessed in a whole cell functional VEGF2R assay (PAE-KDR cell line). No activity is observed at concentrations up to and including 30 μM. In a voltage clamp assay, PF-06650833 inhibits hERG current by 25% at 100 μM[1].
The ability of PF-06650833 (Compound 40) to inhibit five major CYP450 enzymes is assessed using pooled human liver microsomes and probe substrates for the CYP450 enzymes. At a concentration of 3 μM of PF-06650833, less than 5% inhibition of CYPs 1A2, 2C8, 2C9, 2D6, and 3A4 is observed. Lactam PF-06650833 is examined for time dependent inhibition effects on six major CYP450 enzymes (CYP1A2, 2B6, 2C8, 2C9, 2C19, and 2D6) using pooled human liver microsomes and probe substrates. At 100 μM of PF-06650833, no time dependent CYP inhibition is observed. The potential induction of CYP3A by PF-06650833 is assessed using cryopreserved human hepatocytes and afforded a 4.4-fold increase in mRNA at 10 μM[1].

In Vivo

PF-06650833 (Compound 40; 0.3-30 mg/kg; oral administration; for 2.5 hours; male Sprague-Dawley rats) treatment significantly inhibits LPS-induced TNF-α in a dose dependent manner. Mean exposures of PF-06650833 in plasma are 2.1 nM, 7.7 nM, 19 nM and 150 nM free, respectively, at 2.5 hours after oral administration of PF-06650833 at 0.3, 1, 3, and 30 mg/kg. The fraction unbound in rat plasma of PF-06650833 is 0.3[1].

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 0.1 mg/kg, 1 mg/kg, 3 mg/kg, 30 mg/kg
Administration: Oral administration; for 2.5 hours
Result: Significantly inhibited LPS-induced TNF-α in a dose dependent manner.
Clinical Trial
Molecular Weight

361.37

Formula

C₁₈H₂₀FN₃O₄

CAS No.

1817626-54-2

SMILES

NC(C1=C(OC)C=C2C(C=CN=C2OC[[email protected]@H]3[[email protected]](CC)[[email protected]](F)C(N3)=O)=C1)=O

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 : ≥ 100 mg/mL (276.72 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7672 mL 13.8362 mL 27.6725 mL
5 mM 0.5534 mL 2.7672 mL 5.5345 mL
10 mM 0.2767 mL 1.3836 mL 2.7672 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: ≥ 2.5 mg/mL (6.92 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.92 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.92 mM); Clear solution

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

PF-06650833PF06650833PF 06650833IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseInhibitorinhibitorinhibit

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Product Name:
PF-06650833
Cat. No.:
HY-19836
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