2. Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. FAK EGFR Apoptosis
  4. 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.

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EGFR T790M/FAK-IN-2

EGFR T790M/FAK-IN-2 Chemical Structure

CAS No. : 2143104-11-2

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EGFR T790M/FAK-IN-2 Related Antibodies

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Description

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[1].

In Vitro

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.

EGFR T790M/FAK-IN-2 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: AsPC-1, BxPC-3, Panc-1, Hpde6-c7, MCF-7/adr, H1975 human cancer cell lines
Concentration: 1.25-40 μM
Incubation Time: 72 h
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.

Cell Viability Assay[1]

Cell Line: AsPC-1, Panc-1 human cancer cell lines
Concentration: 0.5 μM, 4 μM, 8 μM (AsPC-1); 0.5 μM, 2 μM, 8 μM (Panc-1)
Incubation Time: 24 h, 48 h, 72 h
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).

Apoptosis Analysis[1]

Cell Line: AsPC-1 human cancer cell line
Concentration: 0, 0.25, 0.5, 1 μM
Incubation Time: 72 h
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.

Cell Cycle Analysis[1]

Cell Line: AsPC-1 human cancer cell line
Concentration: 0, 0.25, 0.5, 1 μM
Incubation Time: 72 h
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.
In Vivo

EGFR T790M/FAK-IN-2 (30-60 mg/kg; p.o.; once daily; 10 days) inhibits the growth of pancreatic cancer tumors in BALB/c nude mice in a dose-dependent manner[1].

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

Animal Model: BALB/cJNju-Foxn1nu/Nju (nude) (female, 5-6 weeks old, 20-25 g, subcutaneous xenograft with human AsPC-1 cells)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; daily; 10 days
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.
Molecular Weight

510.00

Formula

C25H28ClN7O3
CAS No.
SMILES

O=C(NC)C=1C=CC=CC1NC2=NC(=NC=C2Cl)NC3=CC=C(NC(=O)CN4CCOCC4)C(=C3)C
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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EGFR T790M/FAK-IN-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EGFR T790M/FAK-IN-22143104-11-2FAKEGFRApoptosisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseEpidermal growth factor receptorErbB-1HER1EGFR T790MPanc-1pancreatic cancerdrug-resistant breast cancerBxPC-3drug-resistant non-small-cell lung cancerMCF-7/adrH1975AsPC-1BALB/cJNju-Foxn1nu/Nju (nude) miceInhibitorinhibitorinhibit

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