CDK12-IN-E9
Based on 2 publication(s) in Google Scholar
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM.
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- Pureté : 99.71%
- CAS No.: 2020052-55-3
- Formule: C24H30N6O2
- Masse moléculaire:434.53
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) CDK12-IN-E9
More
Activité biologique
Description
IC50 & Target
[1]|
CDK12 |
CDK9/cyclinT1 23.9 nM (IC50) |
cdk2/cyclin A 932 nM (IC50) |
CDK7/Cyclin H/MNAT1 1210 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| BT-474 | IC50 |
490 nM
Compound: CICAMPA-01
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Cytotoxicity against human BT-474 cells incubated for 48 hrs by CCK-8 reagent microplate reader assay
Cytotoxicity against human BT-474 cells incubated for 48 hrs by CCK-8 reagent microplate reader assay
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[PMID: 36827953] |
In Vitro
CDK12-IN-E9 (E9; 10 nM-10 μM; 72 hours; Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells) treatment shows potent antiproliferative activity in THZ1R NB and lung cancer cells, with IC50 values ranging from 8 to 40 nM[1].
CDK12-IN-E9 (E9; 0-3000 nM; 6 hours; Kelly, PC-9, and NCI-H82 cells) treatment leads to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1r NB and lung cancer models, accompanied by decreased MYC and MCL1 expression[1].
CDK12-IN-E9 also results in increased PARP cleavage, and an increase in the subGI population in THZ1r lung cancer cells, while in NB cells, more of a G2/M arrest is seen after a 24-hr exposure to CDK12-IN-E9[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells
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Concentration:10 nM-10 μM
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Incubation Time:72 hours
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Result:Showed potent antiproliferative activity in THZ1R NB and lung cancer cells, with IC50 values ranging from 8 to 40 nM.
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Cell Line:Kelly, PC-9, and NCI-H82 cells
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Concentration:0 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 nM
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Incubation Time:6 hours
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Result:Led to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1r NB and lung cancer models.
Chemical Information
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CAS No. 2020052-55-3
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Appearance Solid
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Masse moléculaire 434.53
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Formule C24H30N6O2
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Color White to off-white
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SMILES
C=CC(NC1=CC=CC(NC2=CC(N3[C@H](CCO)CCCC3)=NC4=C(CC)C=NN24)=C1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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NPJ Precis Oncol
High-throughput screening identifies NT-1 that synergizes with MRTX1133 against acquired resistant KRASG12D colorectal cancer. [Abstract]2026 Apr 8;10(1):211. PMID: 41951768 -
Biomed Pharmacother
Antitumoral activity of a CDK12 inhibitor in colorectal cancer through a liposomal formulation. [Abstract]2024 Sep:178:117165. PMID: 39059354
Solvant et solubilité
In Vitro:
DMSO : 125 mg/mL (287.67 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
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.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (278 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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Instruction de manipulation (2659 KB)
Références
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 | 2.3013 mL | 11.5067 mL | 23.0134 mL | 57.5334 mL |
| 5 mM | 0.4603 mL | 2.3013 mL | 4.6027 mL | 11.5067 mL | |
| 10 mM | 0.2301 mL | 1.1507 mL | 2.3013 mL | 5.7533 mL | |
| 15 mM | 0.1534 mL | 0.7671 mL | 1.5342 mL | 3.8356 mL | |
| 20 mM | 0.1151 mL | 0.5753 mL | 1.1507 mL | 2.8767 mL | |
| 25 mM | 0.0921 mL | 0.4603 mL | 0.9205 mL | 2.3013 mL | |
| 30 mM | 0.0767 mL | 0.3836 mL | 0.7671 mL | 1.9178 mL | |
| 40 mM | 0.0575 mL | 0.2877 mL | 0.5753 mL | 1.4383 mL | |
| 50 mM | 0.0460 mL | 0.2301 mL | 0.4603 mL | 1.1507 mL | |
| 60 mM | 0.0384 mL | 0.1918 mL | 0.3836 mL | 0.9589 mL | |
| 80 mM | 0.0288 mL | 0.1438 mL | 0.2877 mL | 0.7192 mL | |
| 100 mM | 0.0230 mL | 0.1151 mL | 0.2301 mL | 0.5753 mL |
CDK12-IN-E9 Related Classifications
HY-117203A Related Classifications
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