1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK MAPK/ERK Pathway PI3K/Akt/mTOR Apoptosis
  2. EGFR p38 MAPK Akt Apoptosis
  3. EGFR-IN-209

EGFR-IN-209 (Compound 6g) is an orally active, selective EGFRDel19/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.

EGFR-IN-209

EGFR-IN-209 Chemical Structure

CAS No. : 3088042-00-3

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Description

EGFR-IN-209 (Compound 6g) is an orally active, selective EGFRDel19/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[1].

IC50 & Target[1]

EGFRdel19 T790M C797S

0.056 μM (IC50)

In Vitro

EGFR-IN-209 (30 min) potently inhibits purified EGFRDel19/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-9Del19/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-9Del19/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-9Del19/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-9Del19/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.
Molecular Weight

363.46

Formula

C21H25N5O

CAS No.
SMILES

OC1=CC=CC=C1C2=NC(NCCN3CCN(C)CC3)=C4C=CC=CC4=N2

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Room temperature in continental US; may vary elsewhere.

Storage

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

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References
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EGFR-IN-209
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HY-183277
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