VVD-699
Based on 1 Customer Validation
VVD-699 is a covalent blocker of the RAS-p110α interaction with oral activity. VVD-699 inhibits activation of PI3Kα (IC50: 104 nM in H358 cells) . VVD-699 inhibits phosphorylated AKT. VVD-699 can be used for the research of KRAS mutant/amplified cancer.
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 3055319-82-6
- Formula: C25H30ClFN2O6S2
- Molecular Weight:573.10
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
|
PI3Kα 104 nM (IC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Immunodeficient mice[1]
-
Dosage:30 mg/kg; 100 mg/kg
-
Administration:p.o.; twice daily (BID); 3 days
-
Result:Induced no significant changes in blood glucose levels or plasma insulin levels with 30 mg/kg or 100 mg/kg dosing.
Achieved near-maximal p110α-C242 target engagement in liver and spleen tissue with both doses.
Chemical Information
-
CAS No. 3055319-82-6
-
Appearance Solid
-
Molecular Weight 573.10
-
Formula C25H30ClFN2O6S2
-
Color White to off-white
-
SMILES
COC1=CC(C2=C(Cl)C=CC=C2)=C(S(N3CC[C@](C(N[C@@H](/C=C\S(C)(=O)=O)C)=O)(F)C[C@H]3C)(=O)=O)C=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (174.49 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.36 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 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Purity & Documentation
-
Data Sheet (275 KB)
-
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)
-
Handling Instructions (2659 KB)
References
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 | 1.7449 mL | 8.7245 mL | 17.4490 mL | 43.6224 mL |
| 5 mM | 0.3490 mL | 1.7449 mL | 3.4898 mL | 8.7245 mL | |
| 10 mM | 0.1745 mL | 0.8724 mL | 1.7449 mL | 4.3622 mL | |
| 15 mM | 0.1163 mL | 0.5816 mL | 1.1633 mL | 2.9082 mL | |
| 20 mM | 0.0872 mL | 0.4362 mL | 0.8724 mL | 2.1811 mL | |
| 25 mM | 0.0698 mL | 0.3490 mL | 0.6980 mL | 1.7449 mL | |
| 30 mM | 0.0582 mL | 0.2908 mL | 0.5816 mL | 1.4541 mL | |
| 40 mM | 0.0436 mL | 0.2181 mL | 0.4362 mL | 1.0906 mL | |
| 50 mM | 0.0349 mL | 0.1745 mL | 0.3490 mL | 0.8724 mL | |
| 60 mM | 0.0291 mL | 0.1454 mL | 0.2908 mL | 0.7270 mL | |
| 80 mM | 0.0218 mL | 0.1091 mL | 0.2181 mL | 0.5453 mL | |
| 100 mM | 0.0174 mL | 0.0872 mL | 0.1745 mL | 0.4362 mL |