PARP1/c-Met-IN-3
PARP1/c-Met-IN-3 (Compound L19) is a selective c-Met and PARP1 inhibitor, with an IC50 of 5.4 nM against c-Met and an IC50 of 3.7 nM against PARP1. PARP1/c-Met-IN-3 inhibits PARP2 enzymatic activity with an IC50 of 4.52 nM, and shows no specificity for PARP1 and PARP2. PARP1/c-Met-IN-3 induces cell cycle arrest and apoptosis. PARP1/c-Met-IN-3 exhibits anti-tumor activity against triple-negative breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 3123529-62-1
- Formula: C38H28FN9O2
- Molecular Weight:661.69
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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c-Met 5.4 nM (IC50) |
PARP1 3.7 nM (IC50) |
PARP2 4.52 nM (IC50) |
PARP1/c-Met-IN-3 (L19) potently inhibits c-Met enzymatic activity with an IC50 of 5.4 ± 0.4 nM[1].
PARP1/c-Met-IN-3 (L19) potently inhibits the enzymatic activity of PARP1, with an IC50 of 3.7 ± 0.3 nM[1].
PARP1/c-Met-IN-3 (L19) inhibits the enzymatic activity of PARP2 with an IC50 of 4.52 ± 0.52 nM, and lacks specificity for PARP1 and PARP2[1].
PARP1/c-Met-IN-3 (L19) (72 h) potently inhibits the proliferation of BRCA wild-type triple-negative breast cancer cell lines (MDA-MB-231, MDA-MB-453, MDA-MB-468, BT-549), with IC50 values ranging from 0.19 ± 0.07 μM to 1.61 ± 0.02 μM; it shows weak activity against BRCA1-mutant HCC1937 cells (IC50 = 8.95 ± 0.85 μM)[1].
PARP1/c-Met-IN-3 (L19) (0.05-1 μM; 72 h) inhibits the invasion of MDA-MB-231 cells in a concentration-dependent manner[1].
PARP1/c-Met-IN-3 (L19) (0.1-4 μM; 72 h) induces apoptosis and activates apoptotic signaling pathways in MDA-MB-231 cells in a concentration-dependent manner in vitro[1].
PARP1/c-Met-IN-3 (L19) (0.5-4 μM; 72 h) arrests MDA-MB-231 cells at the S phase in a concentration-dependent manner[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
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Concentration:0.1-4 μM
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Incubation Time:72 h
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Result:Induced apoptosis in a concentration-dependent manner, with an apoptotic rate of 47.85% at 4 μM compared to 7.74% for DMSO.
Enhanced PARP cleavage and caspase 3, 7, 8 cleavage in a concentration-dependent manner.
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Cell Line:MDA-MB-231
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Concentration:0.5-4 μM
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Incubation Time:72 h
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Result:Arrested cells in the S phase in a concentration-dependent manner; 23.12% (0.5 μM), 26.27% (1 μM), 28.78% (2 μM), and 30.59% (4 μM) of cells were in S phase.
| Species | Dose | Route | T1/2 | Cmax | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | Bioavailability | Vz | CL |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 0.89 ± 0.04 h | 13600 ± 1836 ng/mL | 10348 ± 1890 ng·h/mL | 10369 ± 1889 ng·h/mL | 0.94 ± 0.02 h | 0.96 ± 0.01 h | / | 254 ± 57.5 mL/kg | 197 ± 35.8 mL/h/kg |
| Rat[1] | 10 mg/kg | p.o. | 1.71 ± 0.53 h | 1241 ± 546 ng/mL | 2465 ± 578 ng·h/mL | 2542 ± 601 ng·h/mL | 1.81 ± 0.37 h | 2.08 ± 0.35 h | 4.90 ± 0.01 % | / | / |
PARP1/c-Met-IN-3 (10 mg/kg; i.p.; administered once every other day for 28 consecutive days) achieves a 56% tumor growth inhibition rate in NCG mice bearing MDA-MB-231 xenografts, with low observed toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c nude (female, 6−7 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every other day; 30 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 32%.
Showed no significant body weight loss compared to the vehicle control group.
Detected no observable adverse effects in major organs including heart, liver, spleen, lung, and kidney.
Reduced tumor cell proliferation via IHC Ki67 staining.
Upregulated cleaved caspase 3 expression in tumor tissue.
Increased γH2AX expression in tumor tissue.
Showed stronger inhibition of PARP1 expression in tumor tissue compared to a combination treatment group.
Chemical Information
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CAS No. 3123529-62-1
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Molecular Weight 661.69
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Formula C38H28FN9O2
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SMILES
FC1=CC=C(CC2=NNC(C3=C2C=CC=C3)=O)C=C1C(NCC4=CC=C(C5=NC(N(C(C)C6=CC(C=CC=N7)=C7C=C6)N=N8)=C8N=C5)C=C4)=O
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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-3 Related Classifications
HY-181928 Related Classifications
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