CDK12-IN-6
Based on 1 Customer Validation
CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1).
For research use only. We do not sell to patients.
- Purity: 99.15%
- CAS No.: 2651196-71-1
- Formula: C20H21F2N9
- Molecular Weight:425.44
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Kinase Inhibitor Library
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Anti-Cancer Compound Library
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Biological Activity
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CDK12 1.19 μM (IC50) |
CDK2/cyclinE >20 μM (IC50) |
CDK9/cyclinT1 >20 μM (IC50) |
CDK12-IN-6 (Example 174) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=0.872 nM) and has no effect on CAL-120 cells[1].
CDK12-IN-6 has antproliferative activity in MDA-MB-231 cells (IC50=2.19 nM) and CAL-120 cells (IC50=1 nM)[1].
CDK12-IN-6 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 1851[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. 2651196-71-1
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Appearance Solid
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Molecular Weight 425.44
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Formula C20H21F2N9
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Color White to off-white
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SMILES
FC1=C2C(N=C(CNC3=NC(N4CCNCC4)=NC5=C(C6CC6)C=NN53)N2)=CC=C1F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (235.05 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: ≥ 2.5 mg/mL (5.88 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 (5.88 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.
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 (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)
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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. 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 | 2.3505 mL | 11.7525 mL | 23.5051 mL | 58.7627 mL |
| 5 mM | 0.4701 mL | 2.3505 mL | 4.7010 mL | 11.7525 mL | |
| 10 mM | 0.2351 mL | 1.1753 mL | 2.3505 mL | 5.8763 mL | |
| 15 mM | 0.1567 mL | 0.7835 mL | 1.5670 mL | 3.9175 mL | |
| 20 mM | 0.1175 mL | 0.5876 mL | 1.1753 mL | 2.9381 mL | |
| 25 mM | 0.0940 mL | 0.4701 mL | 0.9402 mL | 2.3505 mL | |
| 30 mM | 0.0784 mL | 0.3918 mL | 0.7835 mL | 1.9588 mL | |
| 40 mM | 0.0588 mL | 0.2938 mL | 0.5876 mL | 1.4691 mL | |
| 50 mM | 0.0470 mL | 0.2351 mL | 0.4701 mL | 1.1753 mL | |
| 60 mM | 0.0392 mL | 0.1959 mL | 0.3918 mL | 0.9794 mL | |
| 80 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7345 mL | |
| 100 mM | 0.0235 mL | 0.1175 mL | 0.2351 mL | 0.5876 mL |
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