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Cat. No.: HY-184274

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EGFR/c-SRC-IN-1

EGFR/c-SRC-IN-1 is a blood-brain barrier-impermeable, ATP-competitive dual-target inhibitor of EGFR/c-SRC, with an IC₅₀ of 0.05 μM against EGFR and an IC₅₀ of 0.07 μM against c-SRC. EGFR/c-SRC-IN-1 shows selectivity toward ABL-2 and VEGFR-2 kinases. EGFR/c-SRC-IN-1 triggers endogenous apoptosis by upregulating p53 and Bax, downregulating Bcl-2, and altering the Bax/Bcl-2 ratio. EGFR/c-SRC-IN-1 can be used in the research of non-small cell lung cancer, hepatocellular carcinoma, and triple-negative breast cancer.

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

Formula: C₂₃H₁₇F₃N₄O₂
Molecular Weight:438.40

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

EGFR/c-SRC-IN-1 Chemical Structure

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Antibody-Drug Conjugates

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

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- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
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Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

SRC-3

0.05 μM (IC₅₀)

All EGFR Isoforms :

All Src Isoforms :

In Vitro

EGFR/c-SRC-IN-1 (compound 9b) (0.04-100 μM; 24 h) potently inhibits the proliferation of A549, HepG2, and MDA-MB-468 cancer cells with IC₅₀ values of 0.61 μM, 1.47 μM, and 9.14 μM, respectively^[1].
EGFR/c-SRC-IN-1 induces G₀/G₁ cell cycle arrest in A549 cells, reducing progression to S and G₂/M phases^[1].
EGFR/c-SRC-IN-1 potently induces apoptosis in A549 cells, increasing total apoptotic populations by approximately 10-fold while leaving necrotic cell levels largely unchanged^[1].
EGFR/c-SRC-IN-1 modulates apoptotic gene expression in A549 cells, upregulating pro-apoptotic p53 and Bax while downregulating anti-apoptotic Bcl-2^[1].

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

Chemical Information

Molecular Weight 438.40
Formula C₂₃H₁₇F₃N₄O₂
SMILES

O=C(NC1=CC=C(C(F)(F)F)C=C1)NN2C(C)=NC3=C(C=C(C4=CC=CC=C4)C=C3)C2=O
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]. Radwan MA, et al. Discovery of new quinazolin-4-ones as dual EGFR/c-SRC inhibitors with potential to overcome bypass-mediated resistance in cancer. European journal of medicinal chemistry. 2026 Oct 05;315:118985. [Content Brief]

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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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Biological Activity
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- In Vitro
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EGFR/c-SRC-IN-1

All EGFR Isoforms

All Src Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EGFR/c-SRC-IN-1 Related Classifications

HY-184274 Related Classifications