CDK12/13-IN-3
Based on 1 Customer Validation
CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6%.
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- Reinheit: 99.14%
- CAS. Nr.: 3029608-57-6
- Formel: C19H22ClN7O2
- Molecular Weight:415.88
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biologische Aktivität
Beschreibung
IC50 & Target
|
CDK13 79.4 nM (IC50) |
CDK12 107.4 nM (IC50) |
Chemical Information
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CAS. Nr. 3029608-57-6
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Appearance Solid
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Molecular Weight 415.88
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Formel C19H22ClN7O2
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Color White to off-white
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SMILES
COC1=NC(N[C@@H]2CCN(C3=NC=NC4=C3CCN(C(C=C)=O)C4)C2)=NC=C1Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 33.33 mg/mL (80.14 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 (sealed storage, away from moisture). 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (273 KB)
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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)
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Handling Instructions (2659 KB)
Verweise
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). 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 | 2.4045 mL | 12.0227 mL | 24.0454 mL | 60.1135 mL |
| 5 mM | 0.4809 mL | 2.4045 mL | 4.8091 mL | 12.0227 mL | |
| 10 mM | 0.2405 mL | 1.2023 mL | 2.4045 mL | 6.0113 mL | |
| 15 mM | 0.1603 mL | 0.8015 mL | 1.6030 mL | 4.0076 mL | |
| 20 mM | 0.1202 mL | 0.6011 mL | 1.2023 mL | 3.0057 mL | |
| 25 mM | 0.0962 mL | 0.4809 mL | 0.9618 mL | 2.4045 mL | |
| 30 mM | 0.0802 mL | 0.4008 mL | 0.8015 mL | 2.0038 mL | |
| 40 mM | 0.0601 mL | 0.3006 mL | 0.6011 mL | 1.5028 mL | |
| 50 mM | 0.0481 mL | 0.2405 mL | 0.4809 mL | 1.2023 mL | |
| 60 mM | 0.0401 mL | 0.2004 mL | 0.4008 mL | 1.0019 mL | |
| 80 mM | 0.0301 mL | 0.1503 mL | 0.3006 mL | 0.7514 mL |