Home JAK/STAT JAK inhibitor WHI-P97

research use only

WHI-P97 JAK inhibitor

Cat.No.S5904

WHI-P97 is a potent inhibitor of JAK-3 with an estimated Ki value of 0.09 μM in modeling studies and a measured IC50 value of 2.5 μM in EGFR kinase inhibition assays.
WHI-P97 JAK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 455.10

Jump to

Quality Control

Batch: S590401 DMSO]8 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.83%
99.83

Solubility

In vitro
Batch:

DMSO : 8 mg/mL (17.57 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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

mg/kg
g
μL

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 455.10 Formula

C16H13Br2N3O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 211555-05-4 -- Storage of Stock Solutions

Synonyms N/A Smiles COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C(=C3)Br)O)Br)OC

Mechanism of Action

Targets/IC50/Ki
JAK3
In vitro
Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcεRI crosslinking by >90% at low micromolar concentrations. This compound does not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal.
In vivo
WHI-P97 was very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 μg/kg to 50 mg/kg, and LD10was not reached at a 50 mg/kg dose level when administered as a single i.p. or i.v. bolus dose. Therapeutic concentrations of this compound, which inhibit mast cell leukotriene synthesis in vitro, could easily be achieved in vivo after the i.v. or i.p. administration of a single nontoxic 40 mg/kg bolus dose. It showed promising biological activity in a mouse model of allergic asthma at nontoxic dose levels. Treatment of ovalbumin-sensitized mice with this chemical prevented the development of airway hyper-responsiveness to methacholine in a dose-dependent fashion. It inhibited the eosinophil recruitment to the airway lumen after the ovalbumin challenge in a dose-dependent fashion. This compound had an elimination half-life (t1/2) of 58.9 min and systemic clearance (CL) of 891 ml/h/kg in CD-1 mice and a t1/2 of 84.2 min and CL of 1513 ml/h/kg in BALB/c mice. The values for AUC and Cmaxwere 107.3 μM·h and 296.7 μM, respectively, in CD-1 mice, and 58.4 μM·h and 212.7 μM, respectively, in BALB/c mice. The large volume of distribution [322 ml/kg in CD-1 mice and 415 ml/kg in BALB/c mice; ∼6-fold greater than the plasma volume (50 ml/kg)] suggests that it may be extensively partitioned into extravascular compartments.
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map