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PKI-166

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Catalog No. T16549Cas No. 187724-61-4

PKI-166 is an oral inhibitor of EGF-R tyrosine kinase (IC50:0.7 nM) that is both effective and selective. PKI-166 can effectively inhibit the growth and metastasis of various human cancer cells including pancreatic cancer.

PKI-166

PKI-166

😃Good
Purity: 99.2%
Catalog No. T16549Cas No. 187724-61-4
PKI-166 is an oral inhibitor of EGF-R tyrosine kinase (IC50:0.7 nM) that is both effective and selective. PKI-166 can effectively inhibit the growth and metastasis of various human cancer cells including pancreatic cancer.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$35In StockIn Stock
5 mg$73In StockIn Stock
10 mg$119In StockIn Stock
25 mg$238In StockIn Stock
50 mg$397In StockIn Stock
100 mg$636-In Stock
200 mg$852-In Stock
1 mL x 10 mM (in DMSO)$80In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Batch Information

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Purity:99.2%
ee:100%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
PKI-166 is an oral inhibitor of EGF-R tyrosine kinase (IC50:0.7 nM) that is both effective and selective. PKI-166 can effectively inhibit the growth and metastasis of various human cancer cells including pancreatic cancer.
Targets&IC50
EGFR tyrosine kinase:0.7 nM
In vitro
PKI-166 (0–0.5 μM; 1 hour) pretreatment suppresses EGFR autophosphorylation in human pancreatic cancer cells. PKI-166 (0.03μ M; 6 days) increased the cytotoxicity mediated by gemcitabine.[1]
In vivo
PKI-166 (100 mg/kg; p.o.; daily; day 7-day 35 after xenograft) suppresses pancreatic cancer growth.
Chemical Properties
Molecular Weight330.38
FormulaC20H18N4O
Cas No.187724-61-4
SmilesC[C@@H](Nc1ncnc2[nH]c(cc12)-c1ccc(O)cc1)c1ccccc1
Relative Density.1.324 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 27.5 mg/mL (83.24 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.0268 mL15.1341 mL30.2682 mL151.3409 mL
5 mM0.6054 mL3.0268 mL6.0536 mL30.2682 mL
10 mM0.3027 mL1.5134 mL3.0268 mL15.1341 mL
20 mM0.1513 mL0.7567 mL1.5134 mL7.5670 mL
50 mM0.0605 mL0.3027 mL0.6054 mL3.0268 mL

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

Keywords

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