SR-5037
Based on 1 Customer Validation
SR-5037 is an orally active CDK12 (IC50 = 31 nM)/CDK13 inhibitor and CycK (DC50 = 30 nM; Dmax > 98%) molecular glue degrader. SR-5037 inhibits the enzymatic activity of CDK12/CycK and CDK13/CycK complexes. SR-5037 promotes the recruitment of DDB1 to the CDK12/CycK complex, thereby triggering proteasome-mediated CycK degradation. SR-5037 degrades active CycK in mouse models of triple-negative breast cancer. SR-5037 can be used in the research of cancers such as triple-negative breast cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.58%
- No. CAS: 2387704-74-5
- Fòrmula: C21H18Cl2F2N10O
- Peso molecular:535.34
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Almacenamiento:Powder -20°C, 3 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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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CDK12 31 nM (IC50) |
CDK13 |
CDK12/Cyclin K 58.7 nM (IC50) |
CDK13/Cyclin K 234.6 nM (IC50) |
CDK12/Cyclin K 139 nM (Kd) |
SR-5037 (1 μM) degrades CycK (DC50 = 30 nM;
Dmax > 98%) and inhibits the kinase activities of WEE1 (59.8%), mTOR (50.6%) and CDK15 (49.2%)[1].
SR-5037 (0.000001-10 μM; 2 h (room temperature)) inhibits the enzymatic activity of purified human CDK12/CycK (IC50 = 58.7 nM, Kd = 139 nM) and CDK13/CycK (IC50 = 134.6 nM) complexes, and promotes the formation of a stable ternary complex between CDK12/CycK and DDB1 (Kd = 2.81 nM)[1].
SR-5037 (100 nM, 1-4 h) potently and rapidly induces the degradation of CycK in MDA-MB-231 cells[1].
SR-5037 (2 h) degrades cyclin K in HiBiT-CycK knock-in A549 cells, with a DC50 of 30 nM and a Dmax > 95%[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 human triple-negative breast cancer cells
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Concentration:0.000000037-10 μM
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Incubation Time:72 h
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Result:Inhibited MDA-MB-231 cell proliferation with a half-maximal growth inhibition concentration (GI50) of 9 nM.
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Cell Line:MDA-MB-231 cells
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Concentration:100 nM
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Incubation Time:4 h
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Result:Weakened the anticyclin K antibody
(red) signal，degraded CycK
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Cell Line:MDA-MB-231 cells
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Concentration:100 nM
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Incubation Time:1, 2, 4 h
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Result:Gradually reduced her CycK protein intake.
| Species | Dose | Route | Cmax | AUC0-t | T1/2 | F |
|---|---|---|---|---|---|---|
| Mice[1] | 20 mg/kg | p.o. | 6.52 μM | 30.2 μM·h | 6.52 h | 13 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice (female, nonirradiated, orthotopic triple-negative breast cancer model)[1]
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Dosage:2, 6, 18 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently reduced CycK protein.
Chemical Information
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No. CAS 2387704-74-5
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Appearance Solid
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Peso molecular 535.34
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Fòrmula C21H18Cl2F2N10O
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Color White to off-white
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SMILES
ClC1=C(C=C(N2)C(N=C2CNC3=C4C(N(C=N4)C(C=N5)=CN5C(F)F)=NC(N6CCOCC6)=N3)=C1)Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 4.17 mg/mL (7.79 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. 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)
Pureza y Documentación
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Ficha de datos (279 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. 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 | 1.8680 mL | 9.3399 mL | 18.6797 mL | 46.6993 mL |
| 5 mM | 0.3736 mL | 1.8680 mL | 3.7359 mL | 9.3399 mL |
SR-5037 Related Classifications
HY-181405 Related Classifications
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