PARP/PI3K-IN-1
Based on 1 Customer Validation
PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.40%
- No. CAS: 2337386-47-5
- Fòrmula: C33H28F4N8O3
- Peso molecular:660.62
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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PARP-1 8.22 (pIC50) |
PARP-2 8.44 (pIC50) |
PI3Kα 8.25 (pIC50) |
PI3Kβ 6.54 (pIC50) |
PI3Kδ 8.13 (pIC50) |
PI3Kγ 6.08 (pIC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC1937 | IC50 |
0.504 μM
Compound: 32
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Inhibition of cell proliferation in human HCC1937 cells incubated for 72 hrs by SRB assay
Inhibition of cell proliferation in human HCC1937 cells incubated for 72 hrs by SRB assay
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[PMID: 35051747] |
| HCT-116 | IC50 |
0.775 μM
Compound: 32
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Inhibition of cell proliferation in human HCT-116 cells incubated for 72 hrs by SRB assay
Inhibition of cell proliferation in human HCT-116 cells incubated for 72 hrs by SRB assay
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[PMID: 35051747] |
| MDA-MB-231 | IC50 |
0.155 μM
Compound: 32
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Inhibition of cell proliferation in human MDA-MB-231 cells incubated for 72 hrs by SRB assay
Inhibition of cell proliferation in human MDA-MB-231 cells incubated for 72 hrs by SRB assay
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[PMID: 35051747] |
PARP/PI3K-IN-1 (compound 15; 1 μM; 72 hours) leads to a significant increase in cell apoptosis[1].
PARP/PI3K-IN-1 (1 μM; 72 hours) reduces the autophosphorylation levels of AKT and S6 while increases the autophosphorylation level of ERK after treating cells, indicating that it can inhibit the PI3K pathway and activate the ERK pathway[1].
PARP/PI3K-IN-1 (1 μM) displays a strong capability to downregulate the expression of BRCA1/2 at the mRNA level in MDA-MB-468 cancer cells[1].
PARP/PI3K-IN-1 not only shows significant inhibitory activity against BRCA-deficient cells HCC1937 and HCT116, but also displays potent anti-proliferative activity against BRCA-proficient cells MDA-MB-231 and MDA-MB-468[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-468 cancer cells
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Concentration:1 μM
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Incubation Time:72 hours
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Result:Led to a significant increase in cell apoptosis.
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Cell Line:MDA-MB-468 cancer cells
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Concentration:1 μM
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Incubation Time:72 hours
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Result:Reduced the autophosphorylation levels of AKT and S6 while increased the autophosphorylation level of ERK after treating cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old male BALB/c nude mice with MDA-MB-468 cells[1]
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Dosage:50 mg/kg
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Administration:i.p.; twice daily (BID) for 34 consecutive days
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Result:Significantly suppressed the tumor growth.
Chemical Information
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No. CAS 2337386-47-5
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Appearance Solid
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Peso molecular 660.62
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Fòrmula C33H28F4N8O3
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Color White to off-white
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SMILES
O=C1NN=C(CC2=CC=C(F)C(C(N3CCC4=C(N5CCOCC5)N=C(C6=C(C(F)(F)F)C=C(N)N=C6)N=C4C3)=O)=C2)C7=C1C=CC=C7
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (151.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.78 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (3.78 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5137 mL | 7.5686 mL | 15.1373 mL | 37.8432 mL |
| 5 mM | 0.3027 mL | 1.5137 mL | 3.0275 mL | 7.5686 mL | |
| 10 mM | 0.1514 mL | 0.7569 mL | 1.5137 mL | 3.7843 mL | |
| 15 mM | 0.1009 mL | 0.5046 mL | 1.0092 mL | 2.5229 mL | |
| 20 mM | 0.0757 mL | 0.3784 mL | 0.7569 mL | 1.8922 mL | |
| 25 mM | 0.0605 mL | 0.3027 mL | 0.6055 mL | 1.5137 mL | |
| 30 mM | 0.0505 mL | 0.2523 mL | 0.5046 mL | 1.2614 mL | |
| 40 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9461 mL | |
| 50 mM | 0.0303 mL | 0.1514 mL | 0.3027 mL | 0.7569 mL | |
| 60 mM | 0.0252 mL | 0.1261 mL | 0.2523 mL | 0.6307 mL | |
| 80 mM | 0.0189 mL | 0.0946 mL | 0.1892 mL | 0.4730 mL | |
| 100 mM | 0.0151 mL | 0.0757 mL | 0.1514 mL | 0.3784 mL |
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