2. Protein Tyrosine Kinase/RTK Apoptosis
  3. c-Met/HGFR Apoptosis
  4. c-Met-IN-29

c-Met-IN-29 is an orally active c-Met inhibitor with an IC50 of 1.6 nM. c-Met-IN-29 binds to and functionally modulates c-Met protein, inhibiting tumor cell proliferation, migration and apoptosis. c-Met-IN-29 exhibits anti-tumor activity both in vitro and in vivo. c-Met-IN-29 can be used for the research of non-small cell lung cancer.

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

c-Met-IN-29

c-Met-IN-29 Chemical Structure

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c-Met-IN-29 Related Antibodies

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Description

c-Met-IN-29 is an orally active c-Met inhibitor with an IC50 of 1.6 nM. c-Met-IN-29 binds to and functionally modulates c-Met protein, inhibiting tumor cell proliferation, migration and apoptosis. c-Met-IN-29 exhibits anti-tumor activity both in vitro and in vivo. c-Met-IN-29 can be used for the research of non-small cell lung cancer[1].

In Vitro

c-Met-IN-29 (11g) potently inhibits proliferation of MHCC97H liver cancer cells (IC50 = 4.01 nM) and EBC-1 lung cancer cells (IC50 = 3.50 nM) in vitro[1].
c-Met-IN-29 (5-50 nM) potently suppresses colony formation of MHCC97H liver cancer cells and EBC-1 lung cancer cells, with slightly stronger activity against EBC-1 cells[1].
c-Met-IN-29 inhibits proliferation of EBC-1 lung cancer cell spheroids (IC50 = 12.63 nM) and MHCC97H liver cancer cell spheroids (IC50 = 20.9 nM) in a concentration-dependent manner[1].
c-Met-IN-29 (5-50 nM; 24-48 h) inhibits MET phosphorylation in MHCC97H liver cancer cells and EBC-1 lung cancer cells in a time-dependent manner, with no effect on total MET protein levels[1].
c-Met-IN-29 (5-10 nM; 24 h for adherent cells) induces apoptosis in MHCC97H liver cancer cells and EBC-1 lung cancer cells (and their 3D spheroids) in a concentration-dependent manner, with EC50 values of 32.2 nM and 26.9 nM for MHCC97H and EBC-1 spheroids, respectively[1].
c-Met-IN-29 (5 nM, 0-24h) potently inhibits migration and invasion of MHCC97H liver cancer cells and EBC-1 lung cancer cells[1].
c-Met-IN-29 potently inhibits c-Met kinase in a cell-free assay with an IC50 of 1.6 nM[1].
c-Met-IN-29 shows excellent selectivity for c-Met kinase over 75 other tested tyrosine kinases[1].

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

c-Met-IN-29 Related Antibodies

Western Blot Analysis[1]

Cell Line: MHCC97H liver cancer cells, EBC-1 lung cancer cells
Concentration: 5, 10, 50 nM
Incubation Time: 24 h (WB)
48 h (WB, Immunofluorescence)
Result: Reduced p-MET levels obviously in two cell lines at 24 h and 48 h without altering total MET protein.
Produced a stronger decline of p-MET in EBC-1 cells at 24 h and robust p-MET suppression in both cell lines at 48 h.
Verified the downregulation of p-MET by immunofluorescence at 48 h.

Apoptosis Analysis[1]

Cell Line: MHCC97H liver cancer cells, EBC-1 lung cancer cells
Concentration: 5, 10 nM
Incubation Time: 24 h
Result: Induced apoptosis in MHCC97H liver cancer cells and EBC-1 lung cancer cells (and their 3D spheroids) in a concentration-dependent manner.

Cell Invasion Assay[1]

Cell Line: MHCC97H liver cancer cells, EBC-1 lung cancer cells
Concentration: 5 nM
Incubation Time: 0, 24h
Result: Inhibited migration and invasion of MHCC97H liver cancer cells and EBC-1 lung cancer cells.
Parmacokinetics
Species Dose Route AUC0-∞ CL Vz T1/2 Cmax Tmax F
Mice[1] 8 mg/kg i.v. 2872.907 h·μg/L 2.785 L/h/kg 16.038 L/kg 3.991 h / / /
Mice[1] 8 mg/kg p.o. 1728.598 h·μg/L / / / 131.04 μg/L 0.25 h 60.17 %
In Vivo

c-Met-IN-29 (11g) (4 mg/kg; p.o.; daily; 16 days) exhibits potent in vivo anti-tumor activity in EBC-1 xenograft mice, achieving a 64.9% tumor growth inhibition rate[1].

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

478.55

Formula

C28H26N6O2
SMILES

CN1CCC[C@H]1COC2=CN=C(N=C2)C3=CC(CN4N=C(C=CC4=O)C5=CC(C#N)=CC=C5)=CC=C3
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
References
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c-Met-IN-29 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:

c-Met-IN-29c-Met/HGFRApoptosisEBC-1 lung cancer cellsnon-small cell lung cancerMET phosphorylationBALB/c-nu micec-Mettumor cell apoptosistumor cell migrationrat liver microsomestumor cell proliferationMHCC97H liver cancer cellsInhibitorinhibitorinhibit

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