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

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PARP1/c-Met-IN-3

PARP1/c-Met-IN-3 Chemical Structure

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PARP1/c-Met-IN-3 Related Antibodies

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Description

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[1].

IC50 & Target[1]

c-Met

5.4 nM (IC50)

PARP1

3.7 nM (IC50)

PARP2

4.52 nM (IC50)

In Vitro

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.

PARP1/c-Met-IN-3 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MDA-MB-231
Concentration: 0.1-4 μM
Incubation Time: 72 h
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.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231
Concentration: 0.5-4 μM
Incubation Time: 72 h
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.
Parmacokinetics
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 % / /
In Vivo

PARP1/c-Met-IN-3 (10 mg/kg, i.p., once every other day for 30 consecutive days) exhibits antitumor activity in Balb/c nude mice bearing MDA-MB-231 xenografts[1].
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.

Animal Model: Balb/c nude (female, 6−7 weeks old)[1]
Dosage: 10 mg/kg
Administration: i.p.; every other day; 30 days
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.
Molecular Weight

661.69

Formula

C38H28FN9O2
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
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-3 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-3c-Met/HGFRPARPApoptosispoly ADP ribose polymerase BT-549MDA-MB-453HCC1937BRCA wild-type triple-negative breast cancer cellsPARP1c-MetMDA-MB-231 xenograft modelsPARP2MDA-MB-231MDA-MB-468Inhibitorinhibitorinhibit

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