CVM-05-002
Based on 1 Customer Validation
CVM-05-002 is a selective pan-phosphatidylinositol 5-phosphate 4-kinase (PI5P4K) inhibitor, with IC50 values of 0.27 μM and 1.69 μM against PI5P4Kα and PI5P4Kβ, respectively. CVM-05-002 binds non-covalently to the ATP-binding pocket of PI5P4Kα, forming hydrophobic interactions and hydrogen bonds with pocket residues. CVM-05-002 can be used in tumor-related research.
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- Pureté : 98.83%
- CAS No.: 2428738-43-4
- Formule: C16H14N4O3S2
- Masse moléculaire:374.44
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Stockage:
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)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
PI5P4Kα 0.27 μM (IC50) |
PI5P4Kβ 1.69 μM (IC50) |
In Vitro
CVM-05-002 potently inhibits recombinant PI5P4Kα with an IC50 of 0.27 μM in an ADP-Glo biochemical assay[1].
CVM-05-002 inhibits recombinant PI5P4Kβ with an IC50 of 1.69 μM in a biochemical assay[1].
CVM-05-002 (2-fold excess inhibitor) binds noncovalently to the ATP-binding pocket of recombinant PI5P4Kα, forming key hydrophobic and hydrogen-bonding interactions, as visualized in a 1.7 Å resolution cocrystal structure[1].
CVM-05-002 (1 μM) exhibits high kinome-wide selectivity, with a selectivity score S35 of 0.02, and strongly binds PI5P4Kγ in addition to its target PI5P4Kα and PI5P4Kβ[1].
CVM-05-002 (2 h) exhibits minimal to no covalent reactivity with recombinant PI5P4Kα and PI5P4Kβ enzymes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 2428738-43-4
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Appearance Solid
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Masse moléculaire 374.44
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Formule C16H14N4O3S2
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Color Off-white to light yellow
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SMILES
CS(NC(C=C1)=CC=C1C2=CN=CC(/C=C3SC(NC\3=O)=N)=C2)(=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (267.07 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)
In Vivo:
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 (6.68 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 (6.68 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.
In Vivo Dissolution Calculator
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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
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 (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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6707 mL | 13.3533 mL | 26.7065 mL | 66.7664 mL |
| 5 mM | 0.5341 mL | 2.6707 mL | 5.3413 mL | 13.3533 mL | |
| 10 mM | 0.2671 mL | 1.3353 mL | 2.6707 mL | 6.6766 mL | |
| 15 mM | 0.1780 mL | 0.8902 mL | 1.7804 mL | 4.4511 mL | |
| 20 mM | 0.1335 mL | 0.6677 mL | 1.3353 mL | 3.3383 mL | |
| 25 mM | 0.1068 mL | 0.5341 mL | 1.0683 mL | 2.6707 mL | |
| 30 mM | 0.0890 mL | 0.4451 mL | 0.8902 mL | 2.2255 mL | |
| 40 mM | 0.0668 mL | 0.3338 mL | 0.6677 mL | 1.6692 mL | |
| 50 mM | 0.0534 mL | 0.2671 mL | 0.5341 mL | 1.3353 mL | |
| 60 mM | 0.0445 mL | 0.2226 mL | 0.4451 mL | 1.1128 mL | |
| 80 mM | 0.0334 mL | 0.1669 mL | 0.3338 mL | 0.8346 mL | |
| 100 mM | 0.0267 mL | 0.1335 mL | 0.2671 mL | 0.6677 mL |
CVM-05-002 Related Classifications
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