CDK2 degrader 6
Based on 1 Customer Validation
CDK2 degrader 6 is an orally active and potent CDK2 molecular glue degrader with a DC50 of 46.5 nM. CDK2 degrader 6 binds to cereblon and CDK2 to induce ubiquitination and subsequent proteasomal degradation of CDK2. CDK2 degrader 6 modulates cell cycle in breast cancer cells. CDK2 degrader 6 reduces proliferation of breast cancer cells. CDK2 degrader 6 exhibits in vivo antitumor activity in gastric cancer mouse models. CDK2 degrader 6 can be used for the research of breast cancer, gastric cancer.
For research use only. We do not sell to patients.
- Purity: 99.81%
- CAS No.: 3036606-92-2
- Formula: C23H22F5N5O3
- Molecular Weight:511.44
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Storage:
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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
Biological Activity
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CDK2 46.5 nM (DC50) |
CDK2 degrader 6 (compound 6) (24 h) potently induces degradation of CDK2 in CDK2 HiBiT-tagged HEK293 cells, with a 62.0% maximal reduction in CDK2 protein levels and a DC50 of 46.5 nM after 24 hours of treatment[1].
CDK2 degrader 6 (24 h) shows minimal activity in degrading GSPT1 in GSPT1 HiBiT-tagged HEK293 cells, with only a 9.9% maximal reduction in GSPT1 protein levels after 24 hours of treatment[1].
CDK2 degrader 6 (0.316-1000 nM; 7 days) potently inhibits proliferation of MDA-MB-157 breast cancer cells, with a 90% maximal reduction in cell proliferation and an EC50 of 10 nM after 7 days of treatment[1].
CDK2 degrader 6 (152 nM-1000 nM; 24 h) potently induces degradation of CDK2 protein in MDA-MB-157 breast cancer cells, with an 84% maximal reduction in CDK2 levels and a DC50 of 4 nM after 24 hours of treatment[1].
CDK2 degrader 6 (10-1000 nM; 24 h) disrupts the cell cycle of MDA-MB-157 breast cancer cells, causing dose-dependent G1 phase arrest and reduction in S phase cells after 24 hours of treatment at concentrations from 10 nM to 1000 nM[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-157 breast cancer cells
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Concentration:0.316 nM, 1 nM, 3.16 nM, 10 nM, 31.6 nM, 100 nM, 316 nM, 1000 nM
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Incubation Time:7 days
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Result:Reduced cell proliferation by 90% relative to DMSO controls, with an EC50 of 10 nM.
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Cell Line:MDA-MB-157 breast cancer cells
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Concentration:0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM
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Incubation Time:24 h
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Result:Induced a maximal 84% reduction in CDK2 protein levels, with a DC50 of 4 nM.
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Cell Line:MDA-MB-157 breast cancer cells
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Concentration:10 nM, 100 nM, 1000 nM
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Incubation Time:24 h
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Result:Caused a dose-dependent accumulation of cells in the G1 phase (56.3% in DMSO controls vs 65.4% at 1000 nM) and a reduction in cells in the S phase (35.8% in DMSO controls vs 3.1% at 1000 nM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice injected with MKN1[1]
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Dosage:30 mg/kg; 100 mg/kg
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Administration:p.o.; twice daily; 21 days
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Result:Achieved 45% tumor growth inhibition (TGI) on day 21, with a statistically significant difference compared to vehicle.
Achieved 47% tumor growth inhibition (TGI) on day 21, with a statistically significant difference compared to vehicle.
Chemical Information
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CAS No. 3036606-92-2
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Appearance Solid
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Molecular Weight 511.44
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Formula C23H22F5N5O3
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Color Off-white to light yellow
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SMILES
O=C(C(CC1)C2=C(F)C=C(N3C[C@H](NC4=NN=C(C56CC(C6)(C(F)(F)F)C5)O4)[C@H]3C)C=C2F)NC1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Solvent & Solubility
DMSO : 15 mg/mL (29.33 mM; Need ultrasonic and warming; 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 (stored under nitrogen, 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 (stored under nitrogen, 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 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 (stored under nitrogen, 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 | 1.9553 mL | 9.7763 mL | 19.5526 mL | 48.8816 mL |
| 5 mM | 0.3911 mL | 1.9553 mL | 3.9105 mL | 9.7763 mL | |
| 10 mM | 0.1955 mL | 0.9776 mL | 1.9553 mL | 4.8882 mL | |
| 15 mM | 0.1304 mL | 0.6518 mL | 1.3035 mL | 3.2588 mL | |
| 20 mM | 0.0978 mL | 0.4888 mL | 0.9776 mL | 2.4441 mL | |
| 25 mM | 0.0782 mL | 0.3911 mL | 0.7821 mL | 1.9553 mL |
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