Rogocekib
Based on 1 Customer Validation
Rogocekib is an orally effective CLK 2 inhibitor, with an IC50 of 1.4 nM, showing anti-tumor activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.15%
- No. CAS: 2144751-78-8
- Fòrmula: C19H17FN8O2
- Peso molecular:408.39
-
Almacenamiento:
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]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
|
CLK2 1.4 nM (IC50) |
Rogocekib has a strong inhibitory effect on the proliferation of human myeloid K562 and MV-4-11 cells, with an IC50 of 0.15 and 0.036 μM, respectively. For primary acute myeloid leukemia (AML) cells, the IC50 is 0.078 μM, demonstrating its anti-leukemia activity[1].
Rogocekib inhibits the phosphorylation of various serine/arginine (SR) proteins, including SRSF3/4/6, which can interact with SRSF2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Mouse models of myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML). [1]
-
Dosage:6.25, 12.5 mg/kg, two weeks
-
Administration:Oral
-
Result:Showed two cases of SRSF2 mutations, P95H and P95L observed with significant dose-dependent effects. P95H reduced tumor volume and improved survival rates in the SRSF2 P95L model.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 2144751-78-8
-
Appearance Solid
-
Peso molecular 408.39
-
Fòrmula C19H17FN8O2
-
Color White to off-white
-
SMILES
CC1=NC2=NC=C(C3=C4C(OC)=NC=NN4C=C3)C=C2N1CC5=NN=C([C@H](F)C)O5
-
Synonyms
CTX-712
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
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)
Solvente y solubilidad
DMSO : 25 mg/mL (61.22 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 (6.12 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.
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. * 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.
Pureza y Documentación
-
Ficha de datos (275 KB)
-
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)
-
Instrucciones de manejo (2659 KB)
Referencias
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 | 2.4486 mL | 12.2432 mL | 24.4864 mL | 61.2160 mL |
| 5 mM | 0.4897 mL | 2.4486 mL | 4.8973 mL | 12.2432 mL | |
| 10 mM | 0.2449 mL | 1.2243 mL | 2.4486 mL | 6.1216 mL | |
| 15 mM | 0.1632 mL | 0.8162 mL | 1.6324 mL | 4.0811 mL | |
| 20 mM | 0.1224 mL | 0.6122 mL | 1.2243 mL | 3.0608 mL | |
| 25 mM | 0.0979 mL | 0.4897 mL | 0.9795 mL | 2.4486 mL | |
| 30 mM | 0.0816 mL | 0.4081 mL | 0.8162 mL | 2.0405 mL | |
| 40 mM | 0.0612 mL | 0.3061 mL | 0.6122 mL | 1.5304 mL | |
| 50 mM | 0.0490 mL | 0.2449 mL | 0.4897 mL | 1.2243 mL | |
| 60 mM | 0.0408 mL | 0.2041 mL | 0.4081 mL | 1.0203 mL |
Rogocekib Related Classifications
HY-144875 Related Classifications
Powered by Bioz