1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. Epertinib hydrochloride

Epertinib hydrochloride  (Synonyms: S-22611 hydrochloride)

Cat. No.: HY-107367A Purity: 98.25%
COA Handling Instructions

Epertinib hydrochloride (S-22611 hydrochloride) est un inhibiteur de la tyrosine kinase EGFR, HER2 et HER4 qui est puissant, oralement actif, réversible et sélectif, avec des IC50s de 1,48 nM, 7,15 nM et 2,49 nM, respectivement. Epertinib hydrochloride présente une activité antitumorale puissante.

Epertinib (S-22611) hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib hydrochloride shows potent antitumor activity. Epertinib (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

Epertinib hydrochloride Chemical Structure

Epertinib hydrochloride Chemical Structure

CAS No. : 2071195-74-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 394 In-stock
Solution
10 mM * 1 mL in DMSO USD 394 In-stock
Solid
5 mg USD 300 In-stock
10 mg USD 490 In-stock
25 mg USD 880 In-stock
50 mg USD 1300 In-stock
100 mg USD 1900 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Epertinib hydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Epertinib (S-22611) hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib hydrochloride shows potent antitumor activity[1][2]. Epertinib (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1]

EGFR

1.48 ± 0.0 nM (IC50)

HER4

2.49 ± 0.1 nM (IC50)

HER2

7.15 nM (IC50)

In Vitro

Epertinib hydrochloride inhibits the phosphorylation of EGFR and HER2 in NCI-N87 cells, with IC50 values of 4.5 and 1.6 nM, respectively[2].
Epertinib hydrochloride shows inhibitory activity against MDA-MB-361 cell, with an IC50 of 26.5 nM[1].
Epertinib hydrochloride (0-10 μM, 72 h) can selectively inhibit the proliferation of a range of cancer cell lines expressing EGFR and/or HER2[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: NCI-N87 (stomach), BT-474 (breast), SK-BR-3 (breast), MDA-MB-453 (breast), MDA-MB-175VII (breast), HT115 (colon), Calu-3 (lung), fR2 (breast), and MRC-5 (lung)
Concentration: 0-10 μM
Incubation Time: 72 h
Result: Inhibited the growth of NCI-N87, BT-474, SK-BR-3, MDA-MB-453, MDA-MB-175VII, HT115, Calu-3, fR2, and MRC-5, with IC50 values of 8.3 ± 2.6, 9.9 ± 0.8, 14.0 ± 3.6, 48.6 ± 3.1, 21.6 ± 4.3, 53.3 ± 8.6, 241.5 ± 29.2, 5366.7 ± 65.2, and 4964.6 ± 340.3.
In Vivo

Epertinib hydrochloride (0-100 mg/kg, Orally, once daily for 28 days) shows antitumor activity[1].
Epertinib hydrochloride (50 mg/kg, Orally, once daily for 30 days) significantly reduces the brain tumor volume[1].
Epertinib hydrochloride (0-50 mg/kg, Orally, once daily for 10-28 days) significantly inhibits the tumor growth in a dose-dependent manner[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)[1]
Dosage: 12.5, 25, 50, 100  mg/kg
Administration: Orally, once daily for 28 days
Result: Showed antitumor activity in the mammary fat pad implantation model using both cell lines and the ED50 values were comparable (24.1 mg/kg and 26.5 mg/kg for MDA-MB-361 and BR2 (MDA-MB-361-luc-BR2), respectively).
Animal Model: Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)[1]
Dosage: 50 mg/kg
Administration: Orally, once daily for 30 days
Result: Significantly reduced the brain tumor volume, indicating that epertinib could have potent antitumor activity in brain metastasis even in the presence of an intact BTB (blood-tumor barrier).
Animal Model: Nude mice (BALB/cAJcl-nu/nu, prepared by subcutaneous implantation of human gastric cancer cells, NCI-N87 into the back of nude mice)[2]
Dosage: 0, 6.25, 12.5, 25, and 50 mg/kg
Administration: Oral gavage, daily for 10-28 days
Result: Significantly inhibited the tumor growth in a dose-dependent manner.
Molecular Weight

596.48

Formula

C30H28Cl2FN5O3

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC#C/C(C1=CC2=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)N=CN=C2C=C1)=N\OC[C@@H]5NCCOC5.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (209.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 33.33 mg/mL (55.88 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6765 mL 8.3825 mL 16.7650 mL
5 mM 0.3353 mL 1.6765 mL 3.3530 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (3.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.6765 mL 8.3825 mL 16.7650 mL 41.9126 mL
5 mM 0.3353 mL 1.6765 mL 3.3530 mL 8.3825 mL
10 mM 0.1677 mL 0.8383 mL 1.6765 mL 4.1913 mL
15 mM 0.1118 mL 0.5588 mL 1.1177 mL 2.7942 mL
20 mM 0.0838 mL 0.4191 mL 0.8383 mL 2.0956 mL
25 mM 0.0671 mL 0.3353 mL 0.6706 mL 1.6765 mL
30 mM 0.0559 mL 0.2794 mL 0.5588 mL 1.3971 mL
40 mM 0.0419 mL 0.2096 mL 0.4191 mL 1.0478 mL
50 mM 0.0335 mL 0.1677 mL 0.3353 mL 0.8383 mL
DMSO 60 mM 0.0279 mL 0.1397 mL 0.2794 mL 0.6985 mL
80 mM 0.0210 mL 0.1048 mL 0.2096 mL 0.5239 mL
100 mM 0.0168 mL 0.0838 mL 0.1677 mL 0.4191 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Epertinib hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Epertinib hydrochloride
Cat. No.:
HY-107367A
Quantity:
MCE Japan Authorized Agent: