CDK12-IN-5
Based on 1 Customer Validation
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1).
For research use only. We do not sell to patients.
- Purity: 98.03%
- CAS No.: 2651200-35-8
- Formula: C18H15F5N8O
- Molecular Weight:454.36
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
CDK12 23.9 nM (IC50) |
CDK2/cyclinE 173 μM (IC50) |
CDK9/cyclinT1 127 μM (IC50) |
CDK12-IN-5 (Example 426) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=3.23 nM) and has no effect on CAL-120 cells[1].
CDK12-IN-5 has antproliferative activity in MDA-MB-231 cells (IC50=4.19 nM) and CAL-120 cells (IC50=3.57 nM)[1].
CDK12-IN-5 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 32[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 2651200-35-8
-
Appearance Solid
-
Molecular Weight 454.36
-
Formula C18H15F5N8O
-
Color White to off-white
-
SMILES
FC(C1=C2N(N=C1)C(NCC3=NC4=CC=C(F)C(F)=C4N3)=NC(N5CCOCC5)=N2)(F)F
-
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 : 125 mg/mL (275.11 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 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (4.58 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 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 (20.8 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.
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 (273 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)
- 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 | 2.2009 mL | 11.0045 mL | 22.0090 mL | 55.0225 mL |
| 5 mM | 0.4402 mL | 2.2009 mL | 4.4018 mL | 11.0045 mL | |
| 10 mM | 0.2201 mL | 1.1004 mL | 2.2009 mL | 5.5022 mL | |
| 15 mM | 0.1467 mL | 0.7336 mL | 1.4673 mL | 3.6682 mL | |
| 20 mM | 0.1100 mL | 0.5502 mL | 1.1004 mL | 2.7511 mL | |
| 25 mM | 0.0880 mL | 0.4402 mL | 0.8804 mL | 2.2009 mL | |
| 30 mM | 0.0734 mL | 0.3668 mL | 0.7336 mL | 1.8341 mL | |
| 40 mM | 0.0550 mL | 0.2751 mL | 0.5502 mL | 1.3756 mL | |
| 50 mM | 0.0440 mL | 0.2201 mL | 0.4402 mL | 1.1004 mL | |
| 60 mM | 0.0367 mL | 0.1834 mL | 0.3668 mL | 0.9170 mL | |
| 80 mM | 0.0275 mL | 0.1376 mL | 0.2751 mL | 0.6878 mL | |
| 100 mM | 0.0220 mL | 0.1100 mL | 0.2201 mL | 0.5502 mL |
Powered by Bioz