DS-7423
Based on 1 Customer Validation
DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM, 34.9 nM for PI3Kα and mTOR, respectively. DS-7423 possesses anti-tumor activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.83%
- CAS. Nr.: 1222104-37-1
- Formel: C22H27F3N10O2
- Molecular Weight:520.51
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biologische Aktivität
DS-7423 increases TP53 expression, the level of p-TP53 on Ser-46, and induced apoptosisrelated TP53 target genes (TP53AIP1 and PUMA) in OCCC cells[1].
DS-7423 also inhibits other isoforms of class I PI3K (IC50 values: PI3Kβ = 1,143 nM; PI3Kγ = 249 nM; PI3Kδ = 262 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1222104-37-1
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Appearance Solid
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Molecular Weight 520.51
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Formel C22H27F3N10O2
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Color White to off-white
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SMILES
CC(N1[C@H](C)CN(C2=NC3=C(N4CCOCC4)N=C(C5=CN=C(N)N=C5)N=C3N2CC(F)(F)F)CC1)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (192.12 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)
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 (4.80 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.
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 (273 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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Handling Instructions (2659 KB)
Verweise
[1]. Katsutoshi Oda, et al. Characterization of TP53 and PI3K signaling pathways as molecular targets in gynecologic malignancies. J Obstet Gynaecol Res. 2016 Jul;42(7):757-62. [Content Brief]
[2]. Tomoko Kashiyama, et al. Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220. [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 | 1.9212 mL | 9.6060 mL | 19.2119 mL | 48.0298 mL |
| 5 mM | 0.3842 mL | 1.9212 mL | 3.8424 mL | 9.6060 mL | |
| 10 mM | 0.1921 mL | 0.9606 mL | 1.9212 mL | 4.8030 mL | |
| 15 mM | 0.1281 mL | 0.6404 mL | 1.2808 mL | 3.2020 mL | |
| 20 mM | 0.0961 mL | 0.4803 mL | 0.9606 mL | 2.4015 mL | |
| 25 mM | 0.0768 mL | 0.3842 mL | 0.7685 mL | 1.9212 mL | |
| 30 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6010 mL | |
| 40 mM | 0.0480 mL | 0.2401 mL | 0.4803 mL | 1.2007 mL | |
| 50 mM | 0.0384 mL | 0.1921 mL | 0.3842 mL | 0.9606 mL | |
| 60 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8005 mL | |
| 80 mM | 0.0240 mL | 0.1201 mL | 0.2401 mL | 0.6004 mL | |
| 100 mM | 0.0192 mL | 0.0961 mL | 0.1921 mL | 0.4803 mL |