PROTAC survivin degrader-1
Based on 1 Customer Validation
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.
- Purity : 98.84%
- CAS No.: 3079079-69-6
- Formula: C48H43ClFN7O7
- Molecular Weight:884.35
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Storage:Powder -20°C, 3 years , 4°C, 2 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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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
Description
In Vitro
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).
Parmacokinetics
| 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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Appearance Solid
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Molecular Weight 884.35
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Formula C48H43ClFN7O7
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Color Light yellow to yellow
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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
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (113.08 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. 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (5.65 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (5.65 mM); Suspended solution
This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (270 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. 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 |
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| DMSO | 1 mM | 1.1308 mL | 5.6539 mL | 11.3077 mL | 28.2694 mL |
| 5 mM | 0.2262 mL | 1.1308 mL | 2.2615 mL | 5.6539 mL | |
| 10 mM | 0.1131 mL | 0.5654 mL | 1.1308 mL | 2.8269 mL | |
| 15 mM | 0.0754 mL | 0.3769 mL | 0.7538 mL | 1.8846 mL | |
| 20 mM | 0.0565 mL | 0.2827 mL | 0.5654 mL | 1.4135 mL | |
| 25 mM | 0.0452 mL | 0.2262 mL | 0.4523 mL | 1.1308 mL | |
| 30 mM | 0.0377 mL | 0.1885 mL | 0.3769 mL | 0.9423 mL | |
| 40 mM | 0.0283 mL | 0.1413 mL | 0.2827 mL | 0.7067 mL | |
| 50 mM | 0.0226 mL | 0.1131 mL | 0.2262 mL | 0.5654 mL | |
| 60 mM | 0.0188 mL | 0.0942 mL | 0.1885 mL | 0.4712 mL | |
| 80 mM | 0.0141 mL | 0.0707 mL | 0.1413 mL | 0.3534 mL | |
| 100 mM | 0.0113 mL | 0.0565 mL | 0.1131 mL | 0.2827 mL |
PROTAC survivin degrader-1 Related Classifications
HY-186212 Related Classifications
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Keywords
- 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