Shopping Cart

Your shopping cart is currently empty

WHI-P258

Name: WHI-P258
Brand: TargetMol
SKU: T2035
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

Copy Product Info

😃Good

Catalog No. T2035Cas No. 21561-09-1

WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of new therapeutics.

WHI-P258

Copy Product Info

😃Good

Purity: 99.92%

Catalog No. T2035Cas No. 21561-09-1

WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of new therapeutics.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$29	In Stock	In Stock
10 mg	$48	In Stock	In Stock
25 mg	$93	In Stock	In Stock
50 mg	$147	In Stock	In Stock
100 mg	$251	In Stock	In Stock
200 mg	$367	-	In Stock
1 mL x 10 mM (in DMSO)	$34	In Stock	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Batch Information

Select Batch

Purity:99.92%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

WHI-P258 AI Summary

WHI-P258 exhibits multiple bioactivities targeting various protein kinases and receptors. It notably inhibits Epidermal Growth Factor Receptor (EGFR) with an IC50 value of approximately 29.5 nM, showing significant inhibition (96.0%) at a concentration of 10 µM in ELISA assays. Additionally, WHI-P258 inhibits the phosphorylation of a 14-residue fragment of phospholipase C gamma 1 by EGFR from A431 cell vesicles with an IC50 of 29.0 nM. It also inhibits VEGFR2, displaying 19.0% inhibition at 10 µM in the presence of 20 µM ATP. This compound shows bioactivity against the JAK2V617F mutant with IC50 values of 5.924 µM in HEL cells and cytotoxicity in the Ba/F3 cell line at greater than 40 µM. In extended assays, WHI-P258 demonstrated weaker inhibition of other kinases such as CLK1, DYRK1A, CK1 delta/epsilon, GSK3 alpha/beta, and CDK5/p25, with IC50 values exceeding 10,000 nM. It also shows selectivity and provides a greater than 5.0 selectivity ratio for N-terminal GST fused human RET over KDR, with an IC50 of 1700.0 nM for inhibiting RET. The compound exhibits good solubility in pH7.4 buffer (117500.0 nM) and a LogD7.4 of 3.04. Additionally, it shows cytotoxicity in human MV4-11 cells with IC50 values greater than 1.0 nM and irreversible inhibition of both wild type FLT3 and FLT3 D835Y mutant at 1 µM concentrations..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of new therapeutics.
Targets&IC50	JAK3:72 μM(Ki)

Chemical Properties

Molecular Weight	281.31
Formula	C₁₆H₁₅N₃O₂
Cas No.	21561-09-1
Smiles	COC1=CC2=NC=NC(NC3=CC=CC=C3)=C2C=C1OC
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 6 mg/mL (21.33 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (3.55 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.5548 mL	17.7740 mL	35.5480 mL	177.7399 mL
5 mM	0.7110 mL	3.5548 mL	7.1096 mL	35.5480 mL
10 mM	0.3555 mL	1.7774 mL	3.5548 mL	17.7740 mL
20 mM	0.1777 mL	0.8887 mL	1.7774 mL	8.8870 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc