Cat. No.: HY-181928

PARP1/c-Met-IN-3

Name: PARP1/c-Met-IN-3
Brand: MedChemExpress
SKU: HY-181928
Price: 450.00 USD
Availability: InStock
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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

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PARP1/c-Met-IN-3 Chemical Structure

CAS No.: 3123529-62-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

c-Met

5.4 nM (IC₅₀)

PARP1

3.7 nM (IC₅₀)

PARP2

4.52 nM (IC₅₀)

All PARP Isoforms :

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.

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	T_1/2	C_max	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	Bioavailability	V_z	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.

Chemical Information

CAS No. 3123529-62-1
Appearance Solid
Molecular Weight 661.69
Formula C₃₈H₂₈FN₉O₂
Color White to off-white
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

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (151.13 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5113 mL

7.5564 mL

15.1128 mL

5 mM

0.3023 mL

1.5113 mL

3.0226 mL

10 mM

0.1511 mL

0.7556 mL

1.5113 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (7.56 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Liu F, et al. Design and synthesis of c-Met/PARP dual-target inhibitors for the treatment of BRCA wild-type TNBC. Eur J Med Chem. 2026;308:118722. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5113 mL	7.5564 mL	15.1128 mL	37.7820 mL
	5 mM	0.3023 mL	1.5113 mL	3.0226 mL	7.5564 mL
	10 mM	0.1511 mL	0.7556 mL	1.5113 mL	3.7782 mL
	15 mM	0.1008 mL	0.5038 mL	1.0075 mL	2.5188 mL
	20 mM	0.0756 mL	0.3778 mL	0.7556 mL	1.8891 mL
	25 mM	0.0605 mL	0.3023 mL	0.6045 mL	1.5113 mL
	30 mM	0.0504 mL	0.2519 mL	0.5038 mL	1.2594 mL
	40 mM	0.0378 mL	0.1889 mL	0.3778 mL	0.9446 mL
	50 mM	0.0302 mL	0.1511 mL	0.3023 mL	0.7556 mL
	60 mM	0.0252 mL	0.1259 mL	0.2519 mL	0.6297 mL
	80 mM	0.0189 mL	0.0945 mL	0.1889 mL	0.4723 mL
	100 mM	0.0151 mL	0.0756 mL	0.1511 mL	0.3778 mL

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PARP1/c-Met-IN-3

All PARP Isoforms