PROTAC survivin degrader-1
PROTAC survivin degrader-1 is an orally active, CNS-penetrant survivin-targeting PROTAC. PROTAC survivin degrader-1 induces degradation of survivin via the ubiquitin proteasome system. PROTAC survivin degrader-1 can be used for the research of glioblastoma.
(Pink: Survivin ligand (HY-186213); Blue: Cereblon ligand (HY-W453715); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3079079-69-6
- Formula: C48H43ClFN7O7
- Molecular Weight:884.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
PROTAC survivin degrader-1 (compound 11) (0.03-3 μM; 24 h) reduces survivin protein levels in U87 and CL261 glioblastoma cells[1].
PROTAC survivin degrader-1 (0.01-1.0 μM; 48 h) induces a DNA damage response in GL261 glioblastoma cells and potentiates the DNA damage, cell killing, and apoptotic effects of 2Gy irradiation[1].
PROTAC survivin degrader-1 (0.5 μM; 2 weeks) potentiates the cytotoxic effect of 0Gy, 2Gy, 4Gy, 6Gy, and 8Gy irradiation in GL261 glioblastoma cells[1].
PROTAC survivin degrader-1 (10-100 nM; 24 h) induces proteasome-dependent survivin degradation in U87 glioblastoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GL261 glioblastoma cell line
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Concentration:0.01; 0.1; 0.5; 1.0 μM
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Incubation Time:48 h
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Result:Increased ATM and CHK1 phosphorylation levels, indicating induction of a DNA damage response.
Potentiated the DNA damage response when combined with 2Gy irradiation.
Increased cleaved PARP levels, enhancing cancer cell killing.
Increased levels of cleaved Caspase 3 and Caspase 9, enhancing apoptosis.
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Cell Line:U87 glioblastoma cell line
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Concentration:10; 100 nM
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Incubation Time:24 h
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Result:Reduced survivin protein levels when treated alone.
Prevented the PROTAC-induced reduction of survivin protein levels when co-treated with MG132 (HY-13259).
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUC0-last | AUC0-inf | MRT0-last | MRT0-inf |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 206 mg/kg | p.o. | 125 ng/mL | 6 h | 1.23 h | 680 ng·h/mL | 687 ng·h/mL | 4.74 h | 4.84 h |
Chemical Information
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CAS No. 3079079-69-6
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Molecular Weight 884.35
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Formula C48H43ClFN7O7
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SMILES
N#CC1=C(C2=CC(OCC3=CC=CC=C3)=CC=C2)C=C(C4=C(O)C=C(N5CCC(CC5)CN6CCN(CC6)C7=CC=C8C(N(C9C(NC(CC9)=O)=O)C(C8=C7F)=O)=O)C(Cl)=C4)NC1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC survivin degrader-1 Related Classifications
HY-186212 Related Classifications
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- PROTAC survivin degrader-1
- 3079079-69-6
- PROTAC survivin degrader1
- PROTAC survivin degrader 1
- PROTACs
- Survivin
- PARP
- irradiation
- male C57BL/6J mice
- DNA damage response
- glioblastoma
- survivin
- GL261 glioblastoma cells
- ubiquitin proteasome system
- U87 glioblastoma cells
- male Sprague-Dawley rats
- blood-brain barrier
- Inhibitor
- inhibitor
- inhibit