PKI-179
Based on 1 publication(s) in Google Scholar
PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.0%
- No. CAS: 1197160-28-3
- Fòrmula: C25H28N8O3
- Peso molecular:488.54
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 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
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Publications Citing Use of MedChemExpress (MCE) PKI-179
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
mTOR 0.42 nM (IC50) |
PI3Kα 8 nM (IC50) |
PI3Kβ 24 nM (IC50) |
PI3Kγ 74 nM (IC50) |
PI3Kδ 77 nM (IC50) |
E545K 14 nM (IC50) |
H1047R 11 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-361 | IC50 |
22 nM
Compound: 8m
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Antiproliferative activity against human MDA-MB-361 cells
Antiproliferative activity against human MDA-MB-361 cells
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[PMID: 20797855] |
| PC-3 | IC50 |
29 nM
Compound: 8m
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Antiproliferative activity against human PC3 cells
Antiproliferative activity against human PC3 cells
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[PMID: 20797855] |
In Vitro
PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1].
PKI-179 shows inhibitory activity against a panel of 361 other kinases, hERG and cytochrome P450 (CYP) isoforms at concentrations up to >30 μM, but does have activity for CYP2C8 (IC50=3 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
PKI-179 (50 mg/kg; p.o.) results in good inhibition of PI3K signaling in nude mice bearing MDA361 tumor xenografts[1].
PKI-179 exhibits good oral bioavailability (98% in nude mouse, 46% in rat, 38% in monkey, and 61% in dog) and a high half-life (>60 min) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice bearing MDA-361 human breast cancer tumors[1]
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Dosage:5, 10, 25, 50 mg/kg
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Administration:I.p. every 3 days for 4 weeks
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Result:Exhibited pronounced tumor growth arrest when dosed above 10 mg/kg.
No significant weight loss of tested animals was observed for all different dosages.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1197160-28-3
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Appearance Solid
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Peso molecular 488.54
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Fòrmula C25H28N8O3
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Color Off-white to yellow
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SMILES
O=C(NC1=CC=NC=C1)NC2=CC=C(C3=NC(N4C5CCC4COC5)=NC(N6CCOCC6)=N3)C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Antiviral Res
Large-scale deep learning identifies the antiviral potential of PKI-179 and MTI-31 against coronaviruses. [Abstract]2024 Nov:231:106012. PMID: 39332537
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (204.69 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)
In Vivo:
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.12 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 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.
In Vivo Dissolution Calculator
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 (278 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
[1]. Venkatesan AM, et, al. PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5869-73. [Content Brief]
[2]. Rehan M. A structural insight into the inhibitory mechanism of an orally active PI3K/mTOR dual inhibitor, PKI-179 using computational approaches. J Mol Graph Model. 2015 Nov;62:226-234. [Content Brief]
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 | 2.0469 mL | 10.2346 mL | 20.4692 mL | 51.1729 mL |
| 5 mM | 0.4094 mL | 2.0469 mL | 4.0938 mL | 10.2346 mL | |
| 10 mM | 0.2047 mL | 1.0235 mL | 2.0469 mL | 5.1173 mL | |
| 15 mM | 0.1365 mL | 0.6823 mL | 1.3646 mL | 3.4115 mL | |
| 20 mM | 0.1023 mL | 0.5117 mL | 1.0235 mL | 2.5586 mL | |
| 25 mM | 0.0819 mL | 0.4094 mL | 0.8188 mL | 2.0469 mL | |
| 30 mM | 0.0682 mL | 0.3412 mL | 0.6823 mL | 1.7058 mL | |
| 40 mM | 0.0512 mL | 0.2559 mL | 0.5117 mL | 1.2793 mL | |
| 50 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0235 mL | |
| 60 mM | 0.0341 mL | 0.1706 mL | 0.3412 mL | 0.8529 mL | |
| 80 mM | 0.0256 mL | 0.1279 mL | 0.2559 mL | 0.6397 mL | |
| 100 mM | 0.0205 mL | 0.1023 mL | 0.2047 mL | 0.5117 mL |
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