XL-418
Based on 1 Customer Validation
XL-418 is an orally active dual Akt and p70S6K inhibitor with IC50s of 1 nM for Akt1 and 2 nM for p70S6K. XL-418 inhibits the phosphorylation of ribosomal protein S6 and GSK3β. XL-418 can be used for the study of prostate carcinoma and breast cancer.
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- Pureté: 95.19%
- CAS No.: 871343-09-8
- Formule: C26H32BrF3N8O
- Masse moléculaire:609.48
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Akt1 1 nM (IC50) |
p70S6K 2 nM (IC50) |
GSK-3β |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
30 nM
Compound: 11b
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Inhibition of p70S6K-mediated ribosomal protein S6 phosphorylation in human A549 cells after 3 hrs by chemiluminescence assay
Inhibition of p70S6K-mediated ribosomal protein S6 phosphorylation in human A549 cells after 3 hrs by chemiluminescence assay
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[PMID: 22450127] |
| PC-3 | IC50 |
194 nM
Compound: 11b
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Inhibition of AKT1-mediated GSK3beta phosphorylation in human PC3 cells after 3 hrs by chemiluminescence assay
Inhibition of AKT1-mediated GSK3beta phosphorylation in human PC3 cells after 3 hrs by chemiluminescence assay
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[PMID: 22450127] |
| PC-3 | IC50 |
55 nM
Compound: 11b
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Inhibition of p70S6K-mediated ribosomal protein S6 phosphorylation in human PC3 cells after 3 hrs by chemiluminescence assay
Inhibition of p70S6K-mediated ribosomal protein S6 phosphorylation in human PC3 cells after 3 hrs by chemiluminescence assay
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[PMID: 22450127] |
XL-418 inhibits the phosphorylation of ribosomal protein S6 with IC50 values of 30 nM and 55 nM in A549 and PC-3 cells. XL-418 inhibits the phosphorylation of GSK3β with an IC50 value of 194 nM in PC-3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
XL-418 (50 mg/kg; p.o.; once a day; for 15 days) inhibits tumor growth in the PC-3 prostate carcinoma model[1].
XL-418 (50-100 mg/kg; p.o.; two days every 4 days) shows highly active in this study with 71% tumor growth inhibition for the 50 mg/kg dose and 96% tumor growth inhibition (TGI) for the 100 mg/kg alternate dosing schedule as a single agent[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 871343-09-8
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Appearance Solid
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Masse moléculaire 609.48
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Formule C26H32BrF3N8O
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Color Off-white to light yellow
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SMILES
O=C(C1=CC(NCCN2CCCC2)=C(C)C(N3CCN(C4=C5C(NN=C5Br)=NC=N4)CC3)=C1)CCC(F)(F)F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 50 mg/mL (82.04 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 (4.10 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 (4.10 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.
Pureté et documentation
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Fiche technique (275 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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Instruction de manipulation (2659 KB)
Références
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 | 1.6407 mL | 8.2037 mL | 16.4074 mL | 41.0186 mL |
| 5 mM | 0.3281 mL | 1.6407 mL | 3.2815 mL | 8.2037 mL | |
| 10 mM | 0.1641 mL | 0.8204 mL | 1.6407 mL | 4.1019 mL | |
| 15 mM | 0.1094 mL | 0.5469 mL | 1.0938 mL | 2.7346 mL | |
| 20 mM | 0.0820 mL | 0.4102 mL | 0.8204 mL | 2.0509 mL | |
| 25 mM | 0.0656 mL | 0.3281 mL | 0.6563 mL | 1.6407 mL | |
| 30 mM | 0.0547 mL | 0.2735 mL | 0.5469 mL | 1.3673 mL | |
| 40 mM | 0.0410 mL | 0.2051 mL | 0.4102 mL | 1.0255 mL | |
| 50 mM | 0.0328 mL | 0.1641 mL | 0.3281 mL | 0.8204 mL | |
| 60 mM | 0.0273 mL | 0.1367 mL | 0.2735 mL | 0.6836 mL | |
| 80 mM | 0.0205 mL | 0.1025 mL | 0.2051 mL | 0.5127 mL |
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