Cat. No.: HY-161927

EGFR-TK-IN-4

Customer Review

Based on 1 Customer Validation

EGFR-TK-IN-4 (compound 10k) is a potent and selective EGFR-TK inhibitor. EGFR-TK-IN-4 can induce apoptosis . EGFR-TK-IN-4 has antitumor activity.

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

Purity: 99.90%
CAS No.: 3053485-72-3
Formula: C₂₃H₁₆F₂N₆O₂S₂
Molecular Weight:510.54

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

EGFR-TK-IN-4 Chemical Structure

CAS No.: 3053485-72-3

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Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- Cellular Effect
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

EGFR-TK-IN-4 (compound 10k) is a potent and selective EGFR-TK inhibitor. EGFR-TK-IN-4 can induce apoptosis . EGFR-TK-IN-4 has antitumor activity^[1].

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.82 μM Compound: 10k	Anticancer activity against human A549 cells incubated for 72 hrs by MTT assay Anticancer activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 39094428]
BEAS-2B	IC₅₀	38.41 μM Compound: 10k	Cytotoxicity against human BEAS-2B cells Cytotoxicity against human BEAS-2B cells	[PMID: 39094428]
HCC827	IC₅₀	0.01 μM Compound: 10k	Anticancer activity against human HCC827 cells incubated for 72 hrs by MTT assay Anticancer activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 39094428]
NCI-H1975	IC₅₀	0.08 μM Compound: 10k	Anticancer activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay Anticancer activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay	[PMID: 39094428]

Chemical Information

CAS No. 3053485-72-3
Appearance Solid
Molecular Weight 510.54
Formula C₂₃H₁₆F₂N₆O₂S₂
Color White to off-white
SMILES

NC1=NC=C(C2=CN=C(SC(C3=CC=CC(NS(C4=CC(F)=CC=C4F)(=O)=O)=C3C)=N5)C5=C2)C=N1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (195.87 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.9587 mL

9.7936 mL

19.5871 mL

5 mM

0.3917 mL

1.9587 mL

3.9174 mL

10 mM

0.1959 mL

0.9794 mL

1.9587 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, 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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

References

[1]. T Borude AS, et al. Design and synthesis of novel Thiazolo[5,4-b]pyridine derivatives as potent and selective EGFR-TK inhibitors targeting resistance Mutations in non-small cell lung cancer. Eur J Med Chem. 2024 Oct 5;276:116727. [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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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
DMSO	1 mM	1.9587 mL	9.7936 mL	19.5871 mL	48.9678 mL
	5 mM	0.3917 mL	1.9587 mL	3.9174 mL	9.7936 mL
	10 mM	0.1959 mL	0.9794 mL	1.9587 mL	4.8968 mL
	15 mM	0.1306 mL	0.6529 mL	1.3058 mL	3.2645 mL
	20 mM	0.0979 mL	0.4897 mL	0.9794 mL	2.4484 mL
	25 mM	0.0783 mL	0.3917 mL	0.7835 mL	1.9587 mL
	30 mM	0.0653 mL	0.3265 mL	0.6529 mL	1.6323 mL
	40 mM	0.0490 mL	0.2448 mL	0.4897 mL	1.2242 mL
	50 mM	0.0392 mL	0.1959 mL	0.3917 mL	0.9794 mL
	60 mM	0.0326 mL	0.1632 mL	0.3265 mL	0.8161 mL
	80 mM	0.0245 mL	0.1224 mL	0.2448 mL	0.6121 mL
	100 mM	0.0196 mL	0.0979 mL	0.1959 mL	0.4897 mL

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EGFR-TK-IN-4

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All EGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

EGFR-TK-IN-4 Related Classifications

Cat. No.: HY-161927