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EGFR-IN-5

Name: EGFR-IN-5
Brand: TargetMol
SKU: T11160
Price: 86 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11160Cas No. 2225887-26-1

EGFR-IN-5 is a selective inhibitor of EGFR. The IC50s for EGFR, EGFR(L858R), EGFR(L858R/T790M), and EGFR(L858R/T790M/C797S) are 10.4, 1.1, 34, 7.2 nM, respectively.

EGFR-IN-5

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Purity: 98.17%

Catalog No. T11160Cas No. 2225887-26-1

EGFR-IN-5 is a selective inhibitor of EGFR. The IC50s for EGFR, EGFR(L858R), EGFR(L858R/T790M), and EGFR(L858R/T790M/C797S) are 10.4, 1.1, 34, 7.2 nM, respectively.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$86	-	In Stock
5 mg	$208	-	In Stock
10 mg	$338	-	In Stock
25 mg	$648	-	In Stock
1 mL x 10 mM (in DMSO)	$263	-	In Stock

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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.

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Batch Information

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Purity:98.17%

Appearance:Solid

Color:Yellow

Resource Download

COA HPLC HNMR

Product Introduction

EGFR-IN-5 AI Summary

EGFR-IN-5 exhibits potent antiproliferative activity against various cancer cell lines with different EGFR mutations, including HCC827 cells (EGFR E746-A750 deletion mutant), NCI-H1975 cells (EGFR L858R/T790M double mutant), and A549 cells (wild type EGFR). It significantly inhibits wild type EGFR and its mutants (L858R, L858R/T790M, L858R/T790M/C797S) using Poly (Glu, Tyr) as a substrate in kinase-Glo luminescence assays. The compound induces apoptosis in HCC827 cells at various stages, including early and late apoptosis, as determined by Annexin V-FITC/propidium iodide staining flow cytometry. It also affects cell cycle progression, inducing arrest in G1, G2, and S phases at different concentrations. The inhibitory potency of EGFR-IN-5 on EGFR mutations is reflected in low IC50 values, such as 7.2 nM for the L858R/T790M/C797S triple mutant and 1.1 nM for the L858R mutant. It has an antiproliferative IC50 of 40.0 nM against HCC827 cells and 400.0 nM against NCI-H1975 cells..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	EGFR-IN-5 is a selective inhibitor of EGFR. The IC50s for EGFR, EGFR(L858R), EGFR(L858R/T790M), and EGFR(L858R/T790M/C797S) are 10.4, 1.1, 34, 7.2 nM, respectively.
Targets&IC50	EGFR:10.4 nM, EGFR (L858R/T790M):34 nM, EGFR (L858R):1.1 nM, EGFR (L858R/T790M/C797S):7.2 nM

Chemical Properties

Molecular Weight	571.69
Formula	C₃₁H₃₈FN₉O
Cas No.	2225887-26-1
Smiles	N(C=1N=C(C2=C(N1)C=NC(NC3=CC=C(C=N3)N4CCC(N(C)C)CC4)=C2)N5CCC(CO)CC5)C6=CC=C(F)C=C6
Relative Density.	1.35 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: 120 mg/mL (209.9 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (7 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	1.7492 mL	8.7460 mL	17.4920 mL	87.4600 mL
5 mM	0.3498 mL	1.7492 mL	3.4984 mL	17.4920 mL
10 mM	0.1749 mL	0.8746 mL	1.7492 mL	8.7460 mL
20 mM	0.0875 mL	0.4373 mL	0.8746 mL	4.3730 mL
50 mM	0.0350 mL	0.1749 mL	0.3498 mL	1.7492 mL
100 mM	0.0175 mL	0.0875 mL	0.1749 mL	0.8746 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