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BI-4020

Name: BI-4020
Brand: TargetMol
SKU: T10534
Price: 173 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T10534Cas No. 2664214-60-0

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM), and EGFR wt (IC50=190 nM). BI-4020 also shows high kinome selectivity and good DMPK properties.

BI-4020

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Purity: 99.74%

Catalog No. T10534Cas No. 2664214-60-0

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$173	In Stock	In Stock
5 mg	$418	In Stock	In Stock
10 mg	$598	In Stock	In Stock
25 mg	$893	In Stock	In Stock
50 mg	$1,190	In Stock	In Stock
100 mg	$1,590	In Stock	In Stock
200 mg	$2,170	-	In Stock
1 mL x 10 mM (in DMSO)	$497	In Stock	In 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.

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.

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Purity:99.74%

ee:100%

Appearance:Solid

Color:White to Yellow

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COA HNMR LCMS CSFC

Product Introduction

Bioactivity

Description	BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM), and EGFR wt (IC50=190 nM). BI-4020 also shows high kinome selectivity and good DMPK properties.
Targets&IC50	EGFR (T790M/C797S/del19):0.2 nM, EGFR (del19):1 nM, EGFR (WT):190 nM
In vitro	BI-4020 inhibits p-EGFR del19 T790M C797S (IC50: 0.6 nM) and the triple mutant EGFR (del19/T790M/C797S) variant (IC50=0.2 nM in BaF3 cell lines), as well as the double mutant EGFR (del19/T790M) and primary mutant EGFR del19 (IC50: 1 nM), with activity against EGFR wt (IC50: 190 nM), and exhibits high kinome selectivity and good DMPK properties.
In vivo	In the human PC-9 (EGFR del19/T790M/C797S) triple mutant NSCLC xenograft model in mice, BI-4020 leads to tumor regressions.

Chemical Properties

Molecular Weight	542.68
Formula	C₃₀H₃₈N₈O₂
Cas No.	2664214-60-0
Smiles	C[C@@H]1CCCOc2c(cnn2C)-c2cc(cc(C)n2)C(=O)\N=C2/Nc3ccc(CN4CCN(C)CC4)cc3N2C1
Relative Density.	1.33 g/cm3 (Predicted)

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: 240 mg/mL (442.25 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.21 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	1.8427 mL	9.2135 mL	18.4271 mL	92.1353 mL
5 mM	0.3685 mL	1.8427 mL	3.6854 mL	18.4271 mL
10 mM	0.1843 mL	0.9214 mL	1.8427 mL	9.2135 mL
20 mM	0.0921 mL	0.4607 mL	0.9214 mL	4.6068 mL
50 mM	0.0369 mL	0.1843 mL	0.3685 mL	1.8427 mL
100 mM	0.0184 mL	0.0921 mL	0.1843 mL	0.9214 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:

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