CDK12-IN-2
Based on 1 publication(s) in Google Scholar
CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12.
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- Pureza: 99.36%
- No. CAS: 2244987-03-7
- Fòrmula: C32H32N6O2
- Peso molecular:532.64
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) CDK12-IN-2
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Actividad biológica
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CDK12 52 nM (IC50) |
CDK2 >100 μM (IC50) |
CDK7 >10 μM (IC50) |
CDK9 16 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| SK-BR-3 | GI50 |
0.8 μM
Compound: 2
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Growth inhibition of human SK-BR-3 cells incubated for 72 hrs by cell-titer-Glo luminescent cell viability assay
Growth inhibition of human SK-BR-3 cells incubated for 72 hrs by cell-titer-Glo luminescent cell viability assay
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[PMID: 30067358] |
CDK12-IN-2 inhibits the phosphorylation of the CTD Ser2 in SK-BR-3 cells at low submicromolar concentrations, it inhibits C-terminal domain ser2 phosphorylation with an IC50 of 185 nM. And CDK12-IN-2 exhibits a growth inhibition with an IC50 of 0.8 μM in SK-BR-3 cells[1].CDK12-IN-2 exhibits time dependency for CDK12 inhibition, the IC50 value for CDK12-IN-2 are 0.0078 μM, 0.042 μM, 0.057 μM,and 0.059 μM, for 0h, 1h, 2h and 5h respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2244987-03-7
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Appearance Solid
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Peso molecular 532.64
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Fòrmula C32H32N6O2
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Color White to off-white
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SMILES
O=C(NCC1=CC=CC=C1)N([C@H]2CC[C@@H](CC2)NC3=CC=C(C=N3)C#N)C4=CC=C(C5=CN(C(C=C5)=O)C)C=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
2025 Nov 3:2025.11.02.685764. PMID: 41279360
Solvente y solubilidad
DMSO : 50 mg/mL (93.87 mM; ultrasonic and warming and heat to 60°C; 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 (4.69 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 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 (4.69 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.
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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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. 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 | 1.8774 mL | 9.3872 mL | 18.7744 mL | 46.9360 mL |
| 5 mM | 0.3755 mL | 1.8774 mL | 3.7549 mL | 9.3872 mL | |
| 10 mM | 0.1877 mL | 0.9387 mL | 1.8774 mL | 4.6936 mL | |
| 15 mM | 0.1252 mL | 0.6258 mL | 1.2516 mL | 3.1291 mL | |
| 20 mM | 0.0939 mL | 0.4694 mL | 0.9387 mL | 2.3468 mL | |
| 25 mM | 0.0751 mL | 0.3755 mL | 0.7510 mL | 1.8774 mL | |
| 30 mM | 0.0626 mL | 0.3129 mL | 0.6258 mL | 1.5645 mL | |
| 40 mM | 0.0469 mL | 0.2347 mL | 0.4694 mL | 1.1734 mL | |
| 50 mM | 0.0375 mL | 0.1877 mL | 0.3755 mL | 0.9387 mL | |
| 60 mM | 0.0313 mL | 0.1565 mL | 0.3129 mL | 0.7823 mL | |
| 80 mM | 0.0235 mL | 0.1173 mL | 0.2347 mL | 0.5867 mL |
CDK12-IN-2 Related Classifications
HY-112626 Related Classifications
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