XL-418 |
Katalog-Nr.GC80870
One-Click Copy Product Info
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XL-418 is an orally active dual Akt and p70S6K inhibitor with IC50 s of 1 nM for Akt1 and 2 nM for p70S6K.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 871343-09-8
Sample solution is provided at 25 µL, 10mM.
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In Vivo, XL-418 (compound 11b; 100 mg/kg; p.o.;twice a day; total five doses) inhibits the phosphorylation of ribosomal protein S6 and GSK3β in the PC-3 prostate carcinoma model[1]. 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].
In Vitro, 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].
References:
[1]. Rice KD, et al. Pyrazolopyrimidines as dual Akt/p70S6K inhibitors. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2693-7.
| Cas No. | 871343-09-8 | SDF | |
| Formula | C26H32BrF3N8O | M.Wt | 609.48 |
| Löslichkeit | DMSO: 50 mg/mL (82.04 mM; Need ultrasonic) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6407 mL | 8.2037 mL | 16.4074 mL |
| 5 mM | 328.1 μL | 1.6407 mL | 3.2815 mL |
| 10 mM | 164.1 μL | 820.4 μL | 1.6407 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)