Home Immunology & Inflammation IRAK inhibitor Zimlovisertib (PF-06650833) For research use only.

Zimlovisertib (PF-06650833)

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

Zimlovisertib (PF-06650833) Chemical Structure

Zimlovisertib (PF-06650833) Chemical Structure

CAS No. 1817626-54-2

Purity & Quality Control

Zimlovisertib (PF-06650833) Related Products

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
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
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]
Animal Research Animal Models Male Sprague Dawley rats
Dosages 0.1 mg/kg, 1 mg/kg, 3 mg/kg, 30 mg/kg
Administration Oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03308110 Completed
Healthy
Pfizer
 September 8 2017 Phase 1
NCT02609139 Completed
Healthy
Pfizer
 November 2015 Phase 1
NCT02485769 Completed
Healthy
Pfizer
 June 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 361.37 Formula

C18H20FN3O4
CAS No. 1817626-54-2 SDF --
Smiles CCC1C(NC(=O)C1F)COC2=NC=CC3=CC(=C(C=C32)OC)C(=O)N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 72 mg/mL ( (199.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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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.

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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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