Zimlovisertib (PF-06650833)

Catalog No.S8531

For research use only.

Zimlovisertib (PF-06650833) is a potent, selective inhibitor of IRAK4 with an IC50 of 0.2 nM.

Zimlovisertib (PF-06650833) Chemical Structure

CAS No. 1817626-54-2

Selleck's Zimlovisertib (PF-06650833) has been cited by 3 Publications

Purity & Quality Control

Choose Selective IRAK Inhibitors

Biological Activity

Description Zimlovisertib (PF-06650833) is a potent, selective inhibitor of IRAK4 with an IC50 of 0.2 nM.
Targets
IRAK4 [1]
(Cell-free assay)
0.2 nM
In vitro

The kinome selectivity profile of PF-06650833 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 while greater than 70% inhibition is observed for the following kinases, in order of potency: IRAK1, MNK2, LRRK2, CLK4, and CK1γ1. Lactam PF-06650833 is subsequently assessed in a whole cell functional VEGF2R assay (PAE-KDR cell line). No activity was observed at concentrations up to and including 30 µM. [1].

In vivo

PF-06650833 significantly inhibits LPS-induced TNF 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 mg/kg, 1 mg/kg, 3 mg/kg and 30 mg/kg. The fraction unbound in rat plasma of PF-06650833 is 0.3.[1]

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: Male Sprague Dawley rats
  • Dosages: 0.1 mg/kg, 1 mg/kg, 3 mg/kg, 30 mg/kg
  • Administration: Oral

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 361.37
Formula

C18H20FN3O4

CAS No. 1817626-54-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1C(NC(=O)C1F)COC2=NC=CC3=CC(=C(C=C32)OC)C(=O)N

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03308110 Completed Drug: PF-06650833 Healthy Pfizer September 8 2017 Phase 1
NCT02609139 Completed Drug: PF-06650833 Healthy Pfizer November 2015 Phase 1
NCT02485769 Completed Drug: PF-06650833|Drug: Placebo Healthy Pfizer June 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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