EGFR T790M/FAK-IN-2
EGFR T790M/FAK-IN-2 is an orally active dual FAK and EGFRT790M kinase inhibitor, with an IC50 of 1.03 nM against FAK and an IC50 of 3.89 nM against EGFRT790M. EGFR T790M/FAK-IN-2 exerts antiproliferative effects in drug-resistant cancer cells overexpressing FAK, inducing apoptosis and cell cycle arrest. EGFR T790M/FAK-IN-2 exhibits antitumor activity in a pancreatic cancer xenograft mouse model. EGFR T790M/FAK-IN-2 can be used for the research of pancreatic cancer, breast cancer and non-small cell lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 2143104-11-2
- Formula: C25H28ClN7O3
- Molecular Weight:510.00
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1975 | IC50 |
0.333 μM
Compound: 8
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
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[PMID: 34218082] |
EGFR T790M/FAK-IN-2 (Compound 9a) (1.25-40 μM; 72 h) inhibits the proliferation of AsPC-1, BxPC-3, Panc-1, Hpde6-c7, MCF-7/adr and H1975 cells, with IC50 values ranging from 0.333 μM to 1.347 μM[1].
EGFR T790M/FAK-IN-2 (0.5-8 μM; 24-72 h) reduces the viability of AsPC-1 and Panc-1 cells in a dose- and time-dependent manner[1].
EGFR T790M/FAK-IN-2 (0-1 μM; 72 h) induces apoptosis in AsPC-1 cells in a dose-dependent manner in vitro[1].
EGFR T790M/FAK-IN-2 (0.25-1.0 μM; 72 h) dose-dependently arrests AsPC-1 cells at the G2/M phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AsPC-1, BxPC-3, Panc-1, Hpde6-c7, MCF-7/adr, H1975 human cancer cell lines
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Concentration:1.25-40 μM
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Incubation Time:72 h
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Result:Inhibited proliferation of AsPC-1 cells with an IC50 of 0.909 μM.
Inhibited proliferation of BxPC-3 cells with an IC50 of 0.761 μM.
Inhibited proliferation of Panc-1 cells with an IC50 of 1.218 μM.
Inhibited proliferation of Hpde6-c7 cells with an IC50 of 1.347 μM.
Inhibited proliferation of MCF-7/adr cells with an IC50 of 0.892 μM.
Inhibited proliferation of H1975 cells with an IC50 of 0.333 μM.
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Cell Line:AsPC-1, Panc-1 human cancer cell lines
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Concentration:0.5 μM, 4 μM, 8 μM (AsPC-1); 0.5 μM, 2 μM, 8 μM (Panc-1)
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Incubation Time:24 h, 48 h, 72 h
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Result:Decreased cell viability of AsPC-1 cells in a dose- and time-dependent manner: 0.5 μM reduced viability to 62.6% (24 h), 58.3% (48 h), 44.5% (72 h); 4 μM reduced viability to 10.1% (24 h), 5.1% (48 h), 0% (72 h); 8 μM reduced viability to 3.4% (24 h), 38.6% (48 h), 2.4% (72 h).
Decreased cell viability of Panc-1 cells in a dose- and time-dependent manner: 0.5 μM reduced viability to 88.7% (24 h), 82.6% (48 h), 33.2% (72 h); 2 μM reduced viability to 60% (24 h), 9.8% (48 h), 9.5% (72 h); 8 μM reduced viability to 3.7% (24 h), 36.5% (48 h), 0.71% (72 h).
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Cell Line:AsPC-1 human cancer cell line
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Concentration:0, 0.25, 0.5, 1 μM
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Incubation Time:72 h
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Result:Induced apoptosis in a dose-dependent manner, with the percentage of apoptotic cells increasing from 52.9% to 90.4% with higher inhibitor concentrations after 72 h treatment, compared to the control group.
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Cell Line:AsPC-1 human cancer cell line
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Concentration:0, 0.25, 0.5, 1 μM
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Incubation Time:72 h
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Result:Arrested cells in the G2/M phase in a dose-dependent manner: 0.25 μM increased G2/M phase cells to 5.72% and decreased G0/G1 phase cells to 63.89%; 0.5 μM increased G2/M phase cells to 15.42% and decreased G0/G1 phase cells to 57.38%; 1.0 μM increased G2/M phase cells to 27.19% and decreased G0/G1 phase cells to 39.90%.
Showed minor changes in the percentage of cells in S phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/cJNju-Foxn1nu/Nju (nude) (female, 5-6 weeks old, 20-25 g, subcutaneous xenograft with human AsPC-1 cells)[1]
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Dosage:30 mg/kg; 60 mg/kg
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Administration:p.o.; daily; 10 days
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Result:Achieved tumor growth inhibition (TGI) rate of 24.45% at 30 mg/kg dose.
Achieved tumor growth inhibition (TGI) rate of 36.6% at 60 mg/kg dose.
Exhibited dose-dependent reduction in tumor weight and volume relative to controls.
Chemical Information
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CAS No. 2143104-11-2
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Molecular Weight 510.00
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Formula C25H28ClN7O3
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SMILES
O=C(NC)C=1C=CC=CC1NC2=NC(=NC=C2Cl)NC3=CC=C(NC(=O)CN4CCOCC4)C(=C3)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR T790M/FAK-IN-2 Related Classifications
HY-183120 Related Classifications
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