Epertinib

Name: Epertinib
Brand: TargetMol
SKU: T11213L
Rating: 4.5 (1 reviews)

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Catalog No. T11213LCas No. 908305-13-5

Alias S-22611

Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor activity.

Epertinib

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Catalog No. T11213LAlias S-22611Cas No. 908305-13-5

Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor activity.

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,360	1-2 weeks	1-2 weeks
50 mg	$1,770	1-2 weeks	1-2 weeks
100 mg	$2,500	1-2 weeks	1-2 weeks

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

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Product Introduction

Bioactivity

Description	Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor activity.
Targets&IC50	EGFR:1.48 nM, HER2:2.49 nM, HER4:7.15 nM
In vitro	Epertinib displays inhibitory activity against the growth of cancer cell lines expressing EGFR and/or HER2 (IC50s: 8.3 nM (NCI-N87 (stomach)), 9.9 nM (BT-474 (breast)), and 14 nM (SK-BR-3 (breast))) [1]. Epertinib shows no effect on KDR, IGF1R, SRC, KIT, and PDGFRβ (IC50, >10000 nM). Epertinib inhibits relative phosphorylation of EGFR and HER2 in NCI-N87 cells (IC50s: 4.5 and 1.6 nM) and it also inhibits MDA-MB-361 cell growth (IC50: 26.5 nM) [2].
In vivo	Epertinib displays antitumor activity in nude mice bearing NCI-N87 xenograft via oral administration for 21 days ( ED50:10.2 mg/kg). Epertinib (50 mg/kg, p.o.) is four times more potent activity than GW572016 and completely inhibits the growth of cancer cells in mice [1] and it also obviously decreases the brain tumor volume in the breast cancer intraventricular injection mouse brain metastasis model [2].
Synonyms	S-22611

Chemical Properties

Molecular Weight	560.02
Formula	C₃₀H₂₇ClFN₅O₃
Cas No.	908305-13-5
Smiles	N(C=1C2=C(C=CC(\C(=N\OC[C@H]3COCCN3)\C#CC)=C2)N=CN1)C4=CC(Cl)=C(OCC5=CC(F)=CC=C5)C=C4
Relative Density.	1.31 g/cm3 (Predicted)

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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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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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