TMX-2138
Based on 1 Customer Validation
TMX-2138 is a CDK PROTAC degrader, with IC50 values against different targets as follows: CDK1 (IC50 = 8.7 nM), CDK2 (IC50 = 10.9 nM), CDK5 (IC50 = 7.0 nM), CDK4 (IC50 = 901.0 nM), CDK6 (IC50 = 465.0 nM), CDK7 (IC50 = 286.0 nM), and CDK9 (IC50 = 25.7 nM). TMX-2138 promotes the ubiquitination of CDK and induces its degradation via the proteasomal pathway. TMX-2138 can be used in ovarian cancer research.
(Pink: CDK ligand (HY-151071); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W008352)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.99%
- No. CAS: 2488892-07-3
- Fòrmula: C40H43BrFN9O11S
- Peso molecular:956.79
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Ver todos los productos específicos de isoformas PROTACs
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Actividad biológica
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CDK1/cyclinB 8.7 nM (IC50) |
CDK2/cyclinA 10.9 nM (IC50) |
Cdk5/p25 7.0 nM (IC50) |
CDK9/cyclinT1 25.7 nM (IC50) |
CDK4/cyclinD1 901 nM (IC50) |
CDK6/cyclinD1 465 nM (IC50) |
CDK7/cyclin H 286 nM (IC50) |
TMX-2138 (10-point dose response) potently inhibits purified human CDK1/cyclin B (IC50 = 8.7 nM), CDK2/cyclin A (IC50 = 10.9 nM), CDK5/p25 (IC50 = 7.0 nM), and CDK9/cyclin T1 (IC50 = 25.7 nM), while showing much weaker activity against CDK4/cyclin D1, CDK6/cyclin D1, and CDK7/cyclin H/MNAT1[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 2488892-07-3
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Appearance Solid
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Peso molecular 956.79
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Fòrmula C40H43BrFN9O11S
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Color White to light yellow
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SMILES
O=C(C1=C(NC2=NC(NC3=CC=C(S(=O)(NCCOCCOCCOCCOCCNC4=CC=CC(C(N5C6C(NC(CC6)=O)=O)=O)=C4C5=O)=O)C=C3)=NC=C2Br)C=CC=C1F)N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 100 mg/mL (104.52 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)
Pureza y Documentación
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Ficha de datos (269 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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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 (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 | 1.0452 mL | 5.2258 mL | 10.4516 mL | 26.1290 mL |
| 5 mM | 0.2090 mL | 1.0452 mL | 2.0903 mL | 5.2258 mL | |
| 10 mM | 0.1045 mL | 0.5226 mL | 1.0452 mL | 2.6129 mL | |
| 15 mM | 0.0697 mL | 0.3484 mL | 0.6968 mL | 1.7419 mL | |
| 20 mM | 0.0523 mL | 0.2613 mL | 0.5226 mL | 1.3065 mL | |
| 25 mM | 0.0418 mL | 0.2090 mL | 0.4181 mL | 1.0452 mL | |
| 30 mM | 0.0348 mL | 0.1742 mL | 0.3484 mL | 0.8710 mL | |
| 40 mM | 0.0261 mL | 0.1306 mL | 0.2613 mL | 0.6532 mL | |
| 50 mM | 0.0209 mL | 0.1045 mL | 0.2090 mL | 0.5226 mL | |
| 60 mM | 0.0174 mL | 0.0871 mL | 0.1742 mL | 0.4355 mL | |
| 80 mM | 0.0131 mL | 0.0653 mL | 0.1306 mL | 0.3266 mL | |
| 100 mM | 0.0105 mL | 0.0523 mL | 0.1045 mL | 0.2613 mL |