VVD-442
Based on 1 Customer Validation
VVD-442 is an inhibitor targeting PI3Kα. VVD-442 covalently binds to Cys242 in the RAS-binding domain of PI3K p110α, induces conformational changes, and disrupts the interaction between PI3K p110α and RAS proteins. VVD-442 also blocks RAS-mediated PI3K activation. VVD-442 can be used in research related to RAS-mutant cancers and HER2-overexpressing cancers.
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 3055318-88-9
- Formula: C23H25BrClFN2O5S2
- Molecular Weight:607.94
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
VVD-442 (0.0001-1 μM; 1-4 h) blocks the interaction between KRASG12C and p110α in HEK293T cell lysates[1].
VVD-442 (0.0001-1 μM; 30 min) inhibits the PI3K/AKT signaling pathway in KRASG12C-mutant H358 cells[1].
VVD-442 (1 h) binds to the Cys242 site of PI3Kα in Jurkat cell lysates[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3055318-88-9
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Appearance Solid
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Molecular Weight 607.94
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Formula C23H25BrClFN2O5S2
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Color White to off-white
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SMILES
BrC1=CC(C2=C(Cl)C=CC=C2)=C(S(N3CCC(C(N[C@H](C)/C=C\S(C)(=O)=O)=O)(F)CC3)(=O)=O)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 50 mg/mL (82.24 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 (4.11 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 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 (4.11 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:
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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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
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Data Sheet (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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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 (sealed storage, away from moisture and light). 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 | 1.6449 mL | 8.2245 mL | 16.4490 mL | 41.1225 mL |
| 5 mM | 0.3290 mL | 1.6449 mL | 3.2898 mL | 8.2245 mL | |
| 10 mM | 0.1645 mL | 0.8224 mL | 1.6449 mL | 4.1122 mL | |
| 15 mM | 0.1097 mL | 0.5483 mL | 1.0966 mL | 2.7415 mL | |
| 20 mM | 0.0822 mL | 0.4112 mL | 0.8224 mL | 2.0561 mL | |
| 25 mM | 0.0658 mL | 0.3290 mL | 0.6580 mL | 1.6449 mL | |
| 30 mM | 0.0548 mL | 0.2741 mL | 0.5483 mL | 1.3707 mL | |
| 40 mM | 0.0411 mL | 0.2056 mL | 0.4112 mL | 1.0281 mL | |
| 50 mM | 0.0329 mL | 0.1645 mL | 0.3290 mL | 0.8224 mL | |
| 60 mM | 0.0274 mL | 0.1371 mL | 0.2741 mL | 0.6854 mL | |
| 80 mM | 0.0206 mL | 0.1028 mL | 0.2056 mL | 0.5140 mL |
VVD-442 Related Classifications
HY-176811 Related Classifications
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