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Cat. No.: HY-182742

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EGFR-IN-208

EGFR-IN-208 is an allosteric mutant EGFR^L858R/T790M and EGFR^{L858R/T790M/C797S} inhibitor, with IC₅₀ values of 3.06 μM and 1.08 μM, respectively. EGFR-IN-208 binds to the allosteric site of EGFR and inhibits EGFR phosphorylation. EGFR-IN-208 induces apoptosis and exhibits antiproliferative effects in cancer cells. EGFR-IN-208 can be used in research related to non-small cell lung cancer.

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

CAS No.: 3087298-90-3
Formula: C₃₂H₃₀FN₅O
Molecular Weight:519.61

Storage:

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

EGFR-IN-208 Chemical Structure

CAS No.: 3087298-90-3

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Antibody-Drug Conjugates

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
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Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

EGFR^L858R/T790M

1.08 μM (IC₅₀)

EGFR^{L858R/T790M/C797S}

3.06 μM (IC₅₀)

All EGFR Isoforms :

In Vitro

EGFR-IN-208 (Compound 2b) potently inhibits the proliferation of A549 (EGFR^WT), H3255 (EGFR^L858R), PC-9 (EGFR^Del19), H1975 (EGFR^L858R/T790M) and Ba/F3 (EGFR^{L858R/T790M/C797S}) cells, with IC₅₀ values ranging from 1.08 μM to 4.33 μM, and exhibits the strongest inhibitory activity against Ba/F3 cells^[1].
EGFR-IN-208 (0.1-3 μM) inhibits EGFR phosphorylation in a concentration-dependent manner in H1975 cells and Ba/F3-EGFR^{L858R/T790M/C797S} cells without altering the total EGFR protein level^[1].
EGFR-IN-208 (0.5-5 μM; 48 h) induces apoptosis in H1975 cells and Ba/F3-EGFR^{L858R/T790M/C797S} cells in a dose-dependent manner within 48 hours, with apoptosis rates ranging from 12.98% to 51.8% across the tested concentration range^[1].

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

Apoptosis Analysis^[1]

Cell Line:

H1975 (EGFRL858R/T790M), Ba/F3-EGFRL858R/T790M/C797S
Concentration:

1, 3 and 5 μM (H1975 cells); 0.5, 1 and 1.5 μM (Ba/F3-EGFRL858R/T790M/C797S cells)
Incubation Time:

48 h
Result:

Induced dose-dependent apoptosis in both cell lines.
Increased apoptotic rates of H1975 cells to 12.98%, 22.64%, and 36.8% at 1, 3, and 5 μM respectively, with statistically significant increases relative to DMSO control.
Increased apoptotic rates of Ba/F3-EGFRL858R/T790M/C797S cells to 20.41%, 40.1%, and 51.8% at 0.5, 1.0, and 1.5 μM respectively, with statistically significant increases relative to DMSO control.

Chemical Information

CAS No. 3087298-90-3
Molecular Weight 519.61
Formula C₃₂H₃₀FN₅O
SMILES

CC1=CC(NC(C2=CC=C3C=CC(C4=CC=C(C=C4)N5CCNCC5)=NC3=C2O)C6=CC(F)=CC=C6)=NC=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]. Xu X, et al. Discovering potent EGFR inhibitors through the structural optimization of the Betti-base scaffold. Bioorg Med Chem Lett. Published online March 25, 2026. [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
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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EGFR-IN-208

All EGFR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EGFR-IN-208 Related Classifications

HY-182742 Related Classifications