2. Cell Cycle/DNA Damage Epigenetics Protein Tyrosine Kinase/RTK
  3. PARP c-Met/HGFR DNA/RNA Synthesis
  4. 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.

PARP1/c-Met-IN-2

PARP1/c-Met-IN-2 Chemical Structure

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PARP1/c-Met-IN-2 Related Antibodies

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Description

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[1].

IC50 & Target

PARP1

21.8 nM (IC50)

c-Met

30.2 nM (IC50)

In Vitro

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 ℃ 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.

PARP1/c-Met-IN-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1 μM
Incubation Time: 72 h
Result: Significantly enhanced the thermal stability of c-Met.

Western Blot Analysis[1]

Cell Line: H2O2-Induced HCT116OR cells
Concentration: 5 μM
Incubation Time: 72 h
Result: Significantly suppressed c-Met phosphorylation without altering the total expression level of c-Met protein.

Western Blot Analysis[1]

Cell Line: HCT116OR cells
Concentration: 5 μM
Incubation Time: 72 h
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.
In Vivo

PARP1/c-Met-IN-2 (Compound S12) (25 mg/kg, 50 mg/kg, i.p., once daily for 21 days) effectively inhibits the growth of Olaparib-resistant HCT116OR tumors in mice without showing significant toxicity at the tested doses[1].

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

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].
Dosage: 25 mg/kg, 50 mg/kg
Administration: I.p., once daily for 21 days
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.
Molecular Weight

676.12

Formula

C36H30ClN7O5
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
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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PARP1/c-Met-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:

PARP1/c-Met-IN-2PARPc-Met/HGFRDNA/RNA Synthesispoly ADP ribose polymerasePARP1c-MetAcquired drug-resistanceDual target inhibitorInhibitorinhibitorinhibit

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