PARP1/c-Met-IN-2
PARP1/c-Met-IN-2 is a highly potent, orally active, PARP1 (IC50 = 21.8 nM) and c-Met (IC50 = 30.2 nM) dual inhibitor. PARP1/c-Met-IN-2 can elevate the expression level of γH2AX, cause DNA damage. PARP1/c-Met-IN-2 exhibits remarkable anti-tumor efficacy in the Olaparib (HY-10162)-resistant HCT116 (HCT116OR) xenograft models. PARP1/c-Met-IN-2 can be used for the study of Colon Cancer.
For research use only. We do not sell to patients.
- Formula: C36H30ClN7O5
- Molecular Weight:676.12
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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- References
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Biological Activity
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PARP1 21.8 nM (IC50) |
c-Met 30.2 nM (IC50) |
PARP1/c-Met-IN-2 (Compound S12) exhibits significant anti-proliferative activity against HCT116OR cells in vitro (IC50 = 4.05), and shows a high level of safety in NRK cells (IC50 = 17.16)[1].
PARP1/c-Met-IN-2 (1 μM, 72 h) significantly enhances the thermal stability of c-Met when the temperature exceeded 43 °C in MDA-MB-231 cells, indicating that compound PARP1/c-Met-IN-2 can directly interact with both PARP1 and c-Met[1].
PARP1/c-Met-IN-2 (5 μM, 72 h) significantly suppresses c-Met phosphorylation without altering the total expression level of c-Met protein in HCT116OR cells[1].
PARP1/c-Met-IN-2 (5 μM, 72 h) not only markedly elevates the expression level of γH2AX, suggesting the induction of more DNA damage, and inhibits c-Met activity, thereby weakening the activation of PARP1 and ultimately leading to a decrease in the PAR level, but also decreases the protein expression level of PARP1 in HCT116OR cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:1 μM
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Incubation Time:72 h
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Result:Significantly enhanced the thermal stability of c-Met.
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Cell Line:H2O2-Induced HCT116OR cells
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Concentration:5 μM
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Incubation Time:72 h
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Result:Significantly suppressed c-Met phosphorylation without altering the total expression level of c-Met protein.
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Cell Line:HCT116OR cells
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Concentration:5 μM
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Incubation Time:72 h
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Result:Markedly elevates the expression level of γH2AX.
Inhibited c-Met activity weakened the activation of PARP1.
Led to a decrease in the PAR level.
Decrease the protein expression level of PARP1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Each 6 to 8-week-old female Balb/c nude mouse was subcutaneously inoculated with 200 μL of HCT116OR cells at a concentration of 1 × 107 under the right axillary tissue[1].
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Dosage:25 mg/kg, 50 mg/kg
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Administration:I.p., once daily for 21 days
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Result:Exhibited dose-dependent anti-tumor effects and could reverse the acquired resistance in HCT116OR cells, with tumor growth inhibition (TGI) values of 67 % and 72 %, respectively.
Did not cause any decrease in body weight in mice at either dosage, demonstrating a favorable safety profile in vivo.
Chemical Information
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Molecular Weight 676.12
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Formula C36H30ClN7O5
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SMILES
N#CC1=CC(C2=NN(C(C=C2)=O)CCOC3=C4C=CC(N5CCN(CC5)C(C6=CC7=C(C(C(N)=O)=CC=C7)O6)=O)=CC4=NC=C3)=CC=C1.Cl
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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)
PARP1/c-Met-IN-2 Related Classifications
HY-178348 Related Classifications
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