PQR514
Based on 1 Customer Validation
PQR514 is an orally active pan-PI3K inhibitor that targets class I PI3K and mTOR. PQR514 reversibly binds to the ATP site, with a Ki of 2.2 nM for PI3Kα inhibition and a Ki of 32.7 nM for mTOR inhibition. PQR514 inhibits PI3K/mTORC1/mTORC2 signaling, cancer cell proliferation, and xenograft tumor growth. PQR514 is used in research on CIC::DUX4 sarcoma, glucose metabolism disorders, and ovarian cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.92%
- CAS. Nr.: 1927857-55-3
- Formel: C16H20F2N8O2
- Molecular Weight:394.38
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
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PI3Kα 2.2 nM (Ki) |
mTOR 32.7 nM (Ki) |
In Vitro
PQR514 (compound 4) inhibits mTORC2 and mTORC1 signaling in A2058 cells, with an IC50 of 17 nM against pPKB S473 and an IC50 of 61 nM against pS6 S235/236[3].
PQR514 inhibits the proliferation of 66 tumor cell lines, with a mean GI50 of 0.25 µM and a GI50 of 0.24 µM in the matched 44-cell line panel[3].
PQR514 inhibits PI3K signaling in MCF7 cells carrying PIK3CA E545K, with an IC50 of 30.9 nM[5].
PQR514 binds PI3Kα with a Ki of 2.2 nM and mTOR with a Ki of 32.7 nM[3].
PQR514 binds to PI3Kα/β/δ/γ with Kd <7 nM[3].
PQR514 is a high-affinity pan-class I PI3K binder, with a Kd of 2.0 nM for both p110α and p110β, and weaker binding to mTOR (21.5 nM)[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Note | Cmax | Tmax | T1/2 | AUC0-t | CLplasma | CL |
|---|---|---|---|---|---|---|---|---|---|
| Mice[3] | 10 mg/kg | p.o. | Plasma | 3282 ng/mL | 1.0 h | 1.7 h | 10315 ng·h/mL | 934 mL/h/kg | / |
| Mice[3] | 10 mg/kg | p.o. | Brain | 1023 ng/mL | 0.5 h | 1.6 h | 2757 ng·h/mL | / | 3519 mL/h/kg |
| Mice[3] | 10 mg/kg | p.o. | Thigh muscle | 1808 ng/mL | 0.5 h | 1.6 h | 4526 ng·h/mL | / | 2147 mL/h/kg |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male)[3]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Plasma insulin and glucose levels rose rapidly after dosing and reached maximal levels at 2 h after administration.
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Animal Model:BALB/c nude[3]
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Dosage:6.3 mg/kg
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Administration:p.o.; once daily; from day 17 for 28 days
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Result:On day forty-five after tumor inoculation, mean tumor size in mice was 397 mm3.
Tumor weight analysis was consistent with the tumor volume analysis.
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- MTT Cell Proliferation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS. Nr. 1927857-55-3
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Appearance Solid
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Molecular Weight 394.38
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Formel C16H20F2N8O2
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Color White to off-white
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SMILES
FC(C1=NC(N)=NC=C1C2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2)F
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 5 mg/mL (12.68 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
Reinheit & Dokumentation
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Data Sheet (292 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Breunis W, et al. Patient-derived tumoroids from CIC::DUX4 rearranged sarcoma identify MCL1 as a therapeutic target. Nature communications. 2025 Aug 21;16(1):7688. [Content Brief]
[3]. Borsari C, et al. Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl-Pyrimidine Moiety. ACS medicinal chemistry letters. 2019 Oct 10;10(10):1473-1479. [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 | 2.5356 mL | 12.6781 mL | 25.3563 mL | 63.3906 mL |
| 5 mM | 0.5071 mL | 2.5356 mL | 5.0713 mL | 12.6781 mL | |
| 10 mM | 0.2536 mL | 1.2678 mL | 2.5356 mL | 6.3391 mL |
PQR514 Related Classifications
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