Name: Zimlovisertib (PF-06650833)
Brand: Selleck Chemicals
SKU: S8531
Availability: InStock
Rating: 5 (6 reviews)

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Quality Control

Batch: Purity: 99.88%

99.88

Related Targets	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Other IRAK Products	IRAK4-IN-1 IRAK-1-4 Inhibitor I Emavusertib (CA-4948) KT-474 (SAR444656) Zabedosertib KT-413 JH-X-119-01 HS-243 IRAK inhibitor 6 IRAK-4 protein kinase inhibitor 2

Solubility

In vitro
Batch:

DMSO : 72 mg/mL (199.24 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.600mg/ml (9.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 72 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.900mg/ml (2.49mM)	Taking the 1 mL working solution as an example, add 50 μL of 18 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	361.37	Formula	C₁₈H₂₀FN₃O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1817626-54-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCC1C(NC(=O)C1F)COC2=NC=CC3=CC(=C(C=C32)OC)C(=O)N

Mechanism of Action

Targets/IC₅₀/Ki	IRAK4 (Cell-free assay) 0.2 nM
In vitro	Zimlovisertib (PF-06650833) was assessed in a panel of 278 kinases (Invitrogen) at 200 nM inhibitor concentration using the ATP Km for each kinase, revealing its kinome selectivity profile. Approximately 100% inhibition was observed for IRAK4, while greater than 70% inhibition was seen for the following kinases, in order of potency: IRAK1, MNK2, LRRK2, CLK4, and CK1γ1. This compound was subsequently evaluated in a whole cell functional VEGF2R assay (PAE-KDR cell line), where no activity was observed at concentrations up to and including 30 μM. .
In vivo	Zimlovisertib (PF-06650833) significantly inhibits LPS-induced TNF in a dose dependent manner. Mean exposures of this compound in plasma are 2.1 nM, 7.7 nM, 19 nM and 150 nM free, respectively, at 2.5 hours after oral administration 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/28498658-discovery-of-clinical-candidate-1-2s3s4s-3-ethyl-4-fluoro-5-oxopyrrolidin-2-ylmethoxy-7-methoxyisoquinoline-6-carboxamide-pf-06650833-a-potent-selective-inhibitor-of-interleukin-1-receptor-associated-kinase-4-irak4-by-fragment-based-drug-design/?from_single_result=Discovery+of+Clinical+Candidate+1-%7B%5B%282S%2C3S%2C4S%29-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl%5Dmethoxy%7D-7-methoxyisoquinoline-6-carboxamide+%28PF-06650833%29%2C+a+Potent%2C+Selective+Inhibitor+of+Interleukin-1+Receptor+Associated+Kinase+4+%28IRAK4%29%2C+by+Fragment-Based+Drug+Design.

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Zimlovisertib (PF-06650833) IRAK inhibitor

Chemical Structure

Molecular Weight: 361.37