CDK-TCIP2
Based on 1 Customer Validation
CDK-TCIP2 is an inhibitor targeting CDK9 and BCL6. CDK-TCIP2 recruits CDK9 to BCL6 binding sites and regulatory regions, phosphorylates RNA Pol II, and activates or silences gene transcription, thereby altering the function of BCL6 in germinal center B cells and reducing germinal center B cells. CDK-TCIP2 kills diffuse large B-cell lymphoma cells and can be used in research on diffuse large B-cell lymphoma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.94%
- Formel: C52H67ClN12O8S2
- Molecular Weight:1087.75
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
BCL6 |
CDK9 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| SU-DHL-5 | EC50 |
0.9 nM
|
Killing of human SUDHL5 DLBCL cells measured by cell viability/cell-killing assay.
Killing of human SUDHL5 DLBCL cells measured by cell viability/cell-killing assay.
|
37961702 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CDK-TCIP2 (i.p.; once or twice daily; for 8 days) produces a dose-dependent decrease in the percentage of GC B cells in immunized mice, indicating altered BCL6 function in vivo[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57Bl/6[1]
-
Dosage:5 mg/kg (once daily); 10 mg/kg (once daily); 5 mg/kg (twice daily)
-
Administration:i.p.; once daily; twice daily; 8 days beginning 2 days after SRBC immunization
-
Result:Reduced the percentage of splenic germinal center B cells (B220+Fas+GL7+) in a dose-dependent manner, with the greatest reduction at 5 mg/kg twice daily.
The total frequency of B220+ B cells was only modestly reduced.
Memory B cells showed a modest increase.
No changes in body weight or other adverse effects were observed over the 8-day dosing period.
Chemical Information
-
Appearance Solid
-
Molecular Weight 1087.75
-
Formel C52H67ClN12O8S2
-
Color White to off-white
-
SMILES
O=C1C(OCC(NC)=O)=CC2=C(N1C)C(OC)=CC(NC3=NC(N4CCC(CC4)C(N5CCC6(CCN(C(CN7CCC(CC7)C(NC8=NC=C(SCC9=NC=C(C(C)(C)C)O9)S8)=O)=O)CC6)CC5)=O)=NC=C3Cl)=C2
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (91.93 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
In Vivo Dissolution Calculator
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.
Reinheit & Dokumentation
-
Data Sheet (271 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)
Verweise
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 | 0.9193 mL | 4.5966 mL | 9.1933 mL | 22.9832 mL |
| 5 mM | 0.1839 mL | 0.9193 mL | 1.8387 mL | 4.5966 mL | |
| 10 mM | 0.0919 mL | 0.4597 mL | 0.9193 mL | 2.2983 mL | |
| 15 mM | 0.0613 mL | 0.3064 mL | 0.6129 mL | 1.5322 mL | |
| 20 mM | 0.0460 mL | 0.2298 mL | 0.4597 mL | 1.1492 mL | |
| 25 mM | 0.0368 mL | 0.1839 mL | 0.3677 mL | 0.9193 mL | |
| 30 mM | 0.0306 mL | 0.1532 mL | 0.3064 mL | 0.7661 mL | |
| 40 mM | 0.0230 mL | 0.1149 mL | 0.2298 mL | 0.5746 mL | |
| 50 mM | 0.0184 mL | 0.0919 mL | 0.1839 mL | 0.4597 mL | |
| 60 mM | 0.0153 mL | 0.0766 mL | 0.1532 mL | 0.3831 mL | |
| 80 mM | 0.0115 mL | 0.0575 mL | 0.1149 mL | 0.2873 mL |