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Cat. No.: HY-189464

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EGFR/Akt/STAT3-IN-1

EGFR/Akt/STAT3-IN-1 is an EGFR/Akt/STAT3 inhibitor (IC₅₀ values of 9.79 μM, 17.80 μM, and 8.30 μM, respectively) that induces apoptosis and G0/G1 cell cycle arrest by inhibiting EGFR tyrosine kinase, Akt kinase, and STAT3 transcriptional activity, and exhibits selective cytotoxicity against cancer cells. EGFR/Akt/STAT3-IN-1 can be used for research on non-small cell lung cancer.

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

Formula: C₁₇H₁₁Br₂N₃O₂S
Molecular Weight:481.16

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

EGFR/Akt/STAT3-IN-1 Chemical Structure

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

EGFR

9.79 μM (IC₅₀)

Akt

17.80 μM (IC₅₀)

STAT3

8.30 μM (IC₅₀)

All EGFR Isoforms :

All Akt Isoforms :

All STAT Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC50	24.11 μM	Cytotoxicity against human A549 lung adenocarcinoma cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay. Cytotoxicity against human A549 lung adenocarcinoma cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.	42612271
L929	IC50	> 500 μM	Cytotoxicity against mouse L929 embryonic fibroblast cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay. Cytotoxicity against mouse L929 embryonic fibroblast cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.	42612271
A549	IC50	9.79 μM	Inhibition of EGFR in human A549 cells incubated for 24 hrs by in-cell ELISA. Inhibition of EGFR in human A549 cells incubated for 24 hrs by in-cell ELISA.	42612271
A549	IC50	17.80 μM	Inhibition of Akt in human A549 cells incubated for 24 hrs by in-cell ELISA. Inhibition of Akt in human A549 cells incubated for 24 hrs by in-cell ELISA.	42612271
A549	IC50	8.30 μM	Inhibition of STAT3 in human A549 cells incubated for 24 hrs by in-cell ELISA. Inhibition of STAT3 in human A549 cells incubated for 24 hrs by in-cell ELISA.	42612271
A549	IC50	13.14 μM	Cytotoxic activity against human A549 non-small cell lung cancer cells. Cytotoxic activity against human A549 non-small cell lung cancer cells.	42612271

In Vitro

Compound 2f (3.9-500 μM; 24 h) exhibits cytotoxic activity against A549 human lung adenocarcinoma cells with an IC₅₀ of 24.11 μM^[1].
Compound 2f (IC₅₀ concentration; 24 h) concurrently inhibits EGFR (IC₅₀ = 9.79 μM), Akt (IC₅₀ = 17.80 μM), and STAT3 (IC₅₀ = 8.30 μM) in A549 cells^[1].
Compound 2f (3.9-500 μM; 24 h) shows selective cytotoxicity, with no detectable toxicity against L929 normal mouse embryonic fibroblasts at concentrations up to 500 μM^[1].
Compound 2f (IC₅₀ concentration; 24 h) strongly induces early and late apoptosis in A549 cells, with 28.71% early and 3.47% late apoptotic cells at its IC₅₀ concentration^[1].
Compound 2f (IC₅₀ concentration; 24 h) induces G0/G1 cell cycle arrest in A549 cells, with 62.84% of cells accumulating in the G0/G1 phase^[1].

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

Apoptosis Analysis^[1]

Cell Line:

A549
Concentration:

24.11 μM
Incubation Time:

24 h
Result:

Induced 28.71% early apoptosis and 3.47% late apoptosis, with total apoptosis of 32.18%.

Cell Cycle Analysis^[1]

Cell Line:

A549
Concentration:

24.11 μM
Incubation Time:

24 h
Result:

Induced cell cycle arrest at G0/G1 phase with 62.84% of cells in G0/G1, 19.60% in S phase, and 6.87% in G2/M phase.

ELISA Assay^[1]

Cell Line:

A549
Concentration:

24.11 μM
Incubation Time:

24 h
Result:

Inhibited EGFR with an IC₅₀ of 9.79 μM, Akt with an IC₅₀ of 17.80 μM, and STAT3 with an IC₅₀ of 8.30 μM.

Chemical Information

Molecular Weight 481.16
Formula C₁₇H₁₁Br₂N₃O₂S
SMILES

BrC1=CC=C(C2=CSC(N/N=C/C3=C(Br)C=C(OCO4)C4=C3)=N2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Altıntop MD, et al. Development of thiazole-hydrazone hybrids for targeted therapy of non-small cell lung cancer. Bioorganic chemistry. 2026 Oct 05;181:110369.

Calculators

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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.

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100 mg

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