Art. -Nr.: HY-107367A

Epertinib hydrochloride

(Synonyms: S-22611 hydrochloride)

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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.

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Reinheit: 98.15%
CAS. Nr.: 2071195-74-7
Formel: C₃₀H₂₈Cl₂FN₅O₃
Molecular Weight:596.48

Speicherung:

4°C, sealed storage, away from moisture

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

Epertinib hydrochloride Chemical Structure

CAS. Nr.: 2071195-74-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle EGFR Isoform-spezifische Produkte anzeigen :

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.

Chemical Information

CAS. Nr. 2071195-74-7
Appearance Solid
Molecular Weight 596.48
Formel C₃₀H₂₈Cl₂FN₅O₃
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
Synonyms

S-22611 hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6765 mL

8.3825 mL

16.7650 mL

5 mM

0.3353 mL

1.6765 mL

3.3530 mL

10 mM

0.1677 mL

0.8383 mL

1.6765 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Tanaka Y, et al. Distribution analysis of epertinib in brain metastasis of HER2-positive breast cancer by imaging mass spectrometry and prospect for antitumor activity. Sci Rep. 2018 Jan 10;8(1):343. [Content Brief]

[2]. Tanaka H, et al. Preclinical antitumor activity of S-222611, an oral reversible tyrosine kinase inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor 2. Cancer Sci. 2014 Aug;105(8):1040-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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Epertinib hydrochloride

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Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alkyne Compound Library

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Epertinib hydrochloride Related Classifications

HY-107367A Related Classifications