PROTAC CDK12/13 Degrader-1
Based on 1 Customer Validation
PROTAC CDK12/13 Degrader-1 (7f) 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 has anti-proliferative activity and can be used in breast cancer research.
For research use only. We do not sell to patients.
- Purity: 98.01%
- CAS No.: 3025994-75-3
- Formula: C45H46N10O6
- Molecular Weight:822.91
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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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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Biological Activity
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CDK12 2.2 nM (DC50) |
CDK13 2.1 nM (DC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF-10A | IC50 |
>5 nM
Compound: 7f
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Antiproliferative activity against human MCF-10A cells assessed as inhibition of cell growth measured after 5 days by cell titer glo-based luminescence assay
Antiproliferative activity against human MCF-10A cells assessed as inhibition of cell growth measured after 5 days by cell titer glo-based luminescence assay
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[PMID: 35938508] |
| MCF7 | IC50 |
4.4 nM
Compound: 7f
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 5 days by cell titer glo-based luminescence assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 5 days by cell titer glo-based luminescence assay
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[PMID: 35938508] |
| MDA-MB-231 | IC50 |
3.3 nM
Compound: 7f
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 5 days by cell titer glo-based luminescence assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 5 days by cell titer glo-based luminescence assay
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[PMID: 35938508] |
| MDA-MB-436 | IC50 |
197.9 nM
Compound: 7f
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Antiproliferative activity against human MDA-MB-436 cells assessed as inhibition of cell growth measured after 5 days by cell titer glo-based luminescence assay
Antiproliferative activity against human MDA-MB-436 cells assessed as inhibition of cell growth measured after 5 days by cell titer glo-based luminescence assay
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[PMID: 35938508] |
| MFM-223 | IC50 |
47 nM
Compound: 7f
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Antiproliferative activity against human MFM-223 cells assessed as inhibition of cell growth measured after 5 days by cell titer glo-based luminescence assay
Antiproliferative activity against human MFM-223 cells assessed as inhibition of cell growth measured after 5 days by cell titer glo-based luminescence assay
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[PMID: 35938508] |
PROTAC CDK12/13 Degrader-1 (7f) (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) (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.
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Cell Line:MDA-MB-231 cell lines
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Concentration:1.0 μM
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Incubation Time:15 hours
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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
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CAS No. 3025994-75-3
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Appearance Solid
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Molecular Weight 822.91
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Formula C45H46N10O6
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Color Light yellow to yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 110 mg/mL (133.67 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 (protect from 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 (protect from 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
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Data Sheet (272 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)
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 (protect from 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 | 1.2152 mL | 6.0760 mL | 12.1520 mL | 30.3800 mL |
| 5 mM | 0.2430 mL | 1.2152 mL | 2.4304 mL | 6.0760 mL | |
| 10 mM | 0.1215 mL | 0.6076 mL | 1.2152 mL | 3.0380 mL | |
| 15 mM | 0.0810 mL | 0.4051 mL | 0.8101 mL | 2.0253 mL | |
| 20 mM | 0.0608 mL | 0.3038 mL | 0.6076 mL | 1.5190 mL | |
| 25 mM | 0.0486 mL | 0.2430 mL | 0.4861 mL | 1.2152 mL | |
| 30 mM | 0.0405 mL | 0.2025 mL | 0.4051 mL | 1.0127 mL | |
| 40 mM | 0.0304 mL | 0.1519 mL | 0.3038 mL | 0.7595 mL | |
| 50 mM | 0.0243 mL | 0.1215 mL | 0.2430 mL | 0.6076 mL | |
| 60 mM | 0.0203 mL | 0.1013 mL | 0.2025 mL | 0.5063 mL | |
| 80 mM | 0.0152 mL | 0.0759 mL | 0.1519 mL | 0.3797 mL | |
| 100 mM | 0.0122 mL | 0.0608 mL | 0.1215 mL | 0.3038 mL |
PROTAC CDK12/13 Degrader-1 Related Classifications
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