Tersolisib
Based on 1 publication(s) in Google Scholar
STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.77%
- No. CAS: 2883540-92-7
- Fòrmula: C16H12F5N5O2
- Peso molecular:401.29
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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) Tersolisib
More
Actividad biológica
Descripciòn
IC50 & Target
PI3Kα[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| T47D | IC50 |
116 nM
Compound: 6; STX-478
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Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 38477582] |
In Vitro
STX-478 (0-10,000 nM; 1 h) demonstrates selectivity for MCF10A cells harboring the H1047R kinase-domain mutation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:MCF10A cells
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Concentration:0-10,000 nM
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Incubation Time:1 h
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Result:Targeted the MCF10A cells (with the H1047R kinase domain mutation).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice (CAL-33 xenograft model)[1].
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Dosage:30, 100 mg/kg
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Administration:Oral administration
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Result:Showed a dose-dependent reduction in tumor volume.
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 2883540-92-7
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Appearance Solid
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Peso molecular 401.29
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Fòrmula C16H12F5N5O2
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Color White to off-white
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SMILES
NC1=NC=C(C=N1)NC(N[C@H](C2=C(C3=CC(F)=CC(F)=C3O2)C)C(F)(F)F)=O
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Synonyms
STX-478; STX-478-101; LY4064809
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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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Br J Cancer
Multi-node inhibition targeting mTORC1, mTORC2 and PI3Kα potently inhibits the PI3K/AKT/mTOR pathway in endometrial and breast cancer models. [Abstract]2025 Aug;133(2):144-154. PMID: 40360883
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (249.20 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 6.25 mg/mL (15.57 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
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 (273 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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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 |
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| DMSO | 1 mM | 2.4920 mL | 12.4598 mL | 24.9196 mL | 62.2991 mL |
| 5 mM | 0.4984 mL | 2.4920 mL | 4.9839 mL | 12.4598 mL | |
| 10 mM | 0.2492 mL | 1.2460 mL | 2.4920 mL | 6.2299 mL | |
| 15 mM | 0.1661 mL | 0.8307 mL | 1.6613 mL | 4.1533 mL | |
| 20 mM | 0.1246 mL | 0.6230 mL | 1.2460 mL | 3.1150 mL | |
| 25 mM | 0.0997 mL | 0.4984 mL | 0.9968 mL | 2.4920 mL | |
| 30 mM | 0.0831 mL | 0.4153 mL | 0.8307 mL | 2.0766 mL | |
| 40 mM | 0.0623 mL | 0.3115 mL | 0.6230 mL | 1.5575 mL | |
| 50 mM | 0.0498 mL | 0.2492 mL | 0.4984 mL | 1.2460 mL | |
| 60 mM | 0.0415 mL | 0.2077 mL | 0.4153 mL | 1.0383 mL | |
| 80 mM | 0.0311 mL | 0.1557 mL | 0.3115 mL | 0.7787 mL | |
| 100 mM | 0.0249 mL | 0.1246 mL | 0.2492 mL | 0.6230 mL |
Tersolisib Related Classifications
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