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Cat. No.: HY-183277

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EGFR-IN-209

EGFR-IN-209 (Compound 6g) is an orally active, selective EGFR^{Del19/T790M/C797S} inhibitor with an IC₅₀ of 0.056 μM. EGFR-IN-209 blocks the phosphorylation of EGFR and its downstream effector molecules (pMAPK, pAKT). EGFR-IN-209 induces Apoptosis. EGFR-IN-209 exhibits antitumor activity against Osimertinib (HY-15772)-resistant non-small cell lung cancer. EGFR-IN-209 can be used in research related to non-small cell lung cancer.

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

CAS No.: 3088042-00-3
Formula: C₂₁H₂₅N₅O
Molecular Weight:363.46

Storage:

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

EGFR-IN-209 Chemical Structure

CAS No.: 3088042-00-3

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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
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

EGFR^{del19 T790M C797S}

0.056 μM (IC₅₀)

All EGFR Isoforms :

All p38 MAPK Isoforms :

All Akt Isoforms :

In Vitro

EGFR-IN-209 (30 min) potently inhibits purified EGFR^{Del19/T790M/C797S} kinase, with an IC₅₀ of 0.056 μM^[1].
EGFR-IN-209 (100-300 nM; 24 h) potently inhibits the viability of PC-9^{Del19/T790M/C797S} cells, with an IC₅₀ value of 0.143 μM^[1].
EGFR-IN-209 (100-300 nM; 24-48 h) inhibits the migration of PC-9^{Del19/T790M/C797S} cells in scratch wound healing assays^[1].
EGFR-IN-209 (0.5-1.5 μM) inhibits the activation of EGFR and its downstream AKT/MAPK signaling pathway in PC-9^{Del19/EGFRT790M/C797S} cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

PC-9Del19/T790M/C797S non-small cell lung cancer cells
Concentration:

100, 300 nM
Incubation Time:

24 h
Result:

Inhibited the viability of PC-9Del19/T790M/C797S cells with an IC₅₀ of 0.143 μM.
Was 16-fold more potent than Osimertinib (IC₅₀ = 2.266 μM).

Cell Migration Assay ^[1]

Cell Line:

PC-9Del19/T790M/C797S non-small cell lung cancer cells
Concentration:

100, 300 nM
Incubation Time:

24 h, 48 h
Result:

Inhibited the migration of PC-9^{Del19/T790M/C797S} cells, as evidenced by reduced closure of the scratch wound over time.

Parmacokinetics

Species	Dose	Route	Bioavailability
Rat^[1]	10 mg/kg	p.o.	22.33 %

In Vivo

EGFR-IN-209 (5-10 mg/kg; p.o.; daily) achieves dose-dependent tumor growth inhibition in osimertinib (HY-15772)-resistant NSCLC xenograft models^[1].

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

Animal Model:

NCG mice (male, 6 weeks old)^[1]
Dosage:

5 mg/kg; 10 mg/kg
Administration:

p.o.; daily
Result:

Achieved tumor growth inhibition (TGI) of 47.3%.
Achieved tumor growth inhibition (TGI) of 64.2%.
Showed no significant systemic toxicity.

Chemical Information

CAS No. 3088042-00-3
Molecular Weight 363.46
Formula C₂₁H₂₅N₅O
SMILES

OC1=CC=CC=C1C2=NC(NCCN3CCN(C)CC3)=C4C=CC=CC4=N2
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]. Chang H, et al. Structure-guided discovery of a potent 2-aryl-4-aminoquinazoline-based inhibitor overcoming osimertinib resistance driven by EGFR C797S mutation in NSCLC. Eur J Med Chem. 2026;311:118818. [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
- In Vivo
Chemical Information
Purity & Documentation
References

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EGFR-IN-209

All EGFR Isoforms

All p38 MAPK Isoforms

All Akt Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EGFR-IN-209 Related Classifications

HY-183277 Related Classifications