PROTAC CDK12/13 Degrader-1 TFA
Based on 1 Customer Validation
PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research.
For research use only. We do not sell to patients.
- Purity: 99.12%
- Formula: C47H47F3N10O8
- Molecular Weight:936.93
-
Storage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
All PROTACs Isoforms
More
Biological Activity
|
CDK12 2.2 nM (DC50) |
CDK13 2.1 nM (DC50) |
PROTAC CDK12/13 Degrader-1 (7f) TFA (0.02-10 μM, 150 h) significantly inhibits the proliferation of MFM223 and MDA-MB-231 cells in a dose-dependent manner[1].
PROTAC CDK12/13 Degrader-1 (7f) TFA (500 nM, 4 h) can significantly degrade CDK12 and CDK13 of MFM223 and MDA-MB-231 cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MDA-MB-231 cell lines
-
Concentration:1.0 μM
-
Incubation Time:15 hours
-
Result:Showed 88% degradation for CDK12 and 74% for CDK13.
Acted on CDK12 with the DC50 value of 2.2 nM, and acted on CDK13 with the DC50 value of 2.1 nM.
| Parameters | oral (20 mg/kg) | iv (10 mg/kg) | ip (20 mg/kg) | iv (2.5 mg/kg) |
| t1/2 (h) | - | 5.28 | 10.85 | 5.8 |
| Tmax (h) | 5.33 | 0.08 | 2.17 | 0.08 |
| Cmax (ng/mL) | 7.73 | 19892.4 | 24.79 | 1498.5 |
| Cmax (ng/mL) | 7.73 | 19892.4 | 24.79 | 1498.5 |
| AUC0-t(h*ng/mL) | 21.83 | 7193.3 | 284.8 | 383.9 |
| AUC0-∞(h*ng/mL) | - | 7242.7 | 318.5 | 391.55 |
| CL (mL/h/kg) | - | 1406.5 | - | 6495.4 |
| F (%) | 0.15 | - | 10.63 | - |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
Appearance Solid
-
Molecular Weight 936.93
-
Formula C47H47F3N10O8
-
Color Light yellow to yellow
-
SMILES
O=C(NCC1=CC=CC=C1)N([C@H]2CC[C@H](NC3=NC=C(C#N)C=C3)CC2)C4=CC=C(N5CCN(C(CNC6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7=O)=O)C=C6)=O)CC5)C=C4.O=C(O)C(F)(F)F
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 25 mg/mL (26.68 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 and light). 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 and light). 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)
Purity & Documentation
-
Data Sheet (273 KB)
-
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)
-
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 (sealed storage, away from moisture and light). 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 | 1.0673 mL | 5.3366 mL | 10.6732 mL | 26.6829 mL |
| 5 mM | 0.2135 mL | 1.0673 mL | 2.1346 mL | 5.3366 mL | |
| 10 mM | 0.1067 mL | 0.5337 mL | 1.0673 mL | 2.6683 mL | |
| 15 mM | 0.0712 mL | 0.3558 mL | 0.7115 mL | 1.7789 mL | |
| 20 mM | 0.0534 mL | 0.2668 mL | 0.5337 mL | 1.3341 mL | |
| 25 mM | 0.0427 mL | 0.2135 mL | 0.4269 mL | 1.0673 mL |
PROTAC CDK12/13 Degrader-1 TFA Related Classifications
HY-151110A Related Classifications
Powered by Bioz