EGFR-IN-186

Name: EGFR-IN-186
Brand: TargetMol
SKU: T214432
Rating: 4.5 (1 reviews)

Catalog No. T214432 Copy Product Info

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EGFR-IN-186 is a potent EGFR inhibitor with an IC50 value of 0.065 µM. It also exhibits inhibitory activity against EGFRL858R (IC50= 0.528 µM) and EGFRT790M (IC50= 0.465 µM). EGFR-IN-186 induces apoptosis by increasing levels of Bax and caspase-3, while decreasing the expression of Bcl-2. This compound can be utilized in non-small cell lung cancer (NSCLC) research.

EGFR-IN-186

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Catalog No. T214432

EGFR-IN-186

Pack Size	Price	USA Stock	Global Stock	Quantity
10 mg	Inquiry	Inquiry	Inquiry
50 mg	Inquiry	Inquiry	Inquiry

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	EGFR-IN-186 is a potent EGFR inhibitor with an IC50 value of 0.065 µM. It also exhibits inhibitory activity against EGFRL858R (IC50= 0.528 µM) and EGFRT790M (IC50= 0.465 µM). EGFR-IN-186 induces apoptosis by increasing levels of Bax and caspase-3, while decreasing the expression of Bcl-2. This compound can be utilized in non-small cell lung cancer (NSCLC) research.
Targets&IC50	EGFR:0.065 μM
In vitro	EGFR-IN-186 (compound 6) demonstrates potent cytotoxicity against A549, NCI-H460, and HOP-62 cancer cell lines, with IC50 values of 4.55, 26.09, and 10.72 μM, respectively, while exhibiting significantly lower toxicity to normal human lung fibroblast WI-38 cells (IC50 = 44.64 μM). It also shows enhanced cytotoxicity to A-549 cells post-radiation, with an IC50 of 2.38 μM, indicating notable radiosensitizing properties. Additionally, EGFR-IN-186 (4.55 μM; 48 hours) induces apoptosis in A549 cells by increasing Bax and caspase-3 levels and downregulating Bcl-2 expression.

Chemical Properties

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.

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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.

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

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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