Pomalidomide-C3-adavosertib
Based on 1 Customer Validation
Pomalidomide-C3-adavosertib is a rapid and selective PROTAC Wee1 degrader (IC50=3.58 nM). Pomalidomide-C3-adavosertib shows anti-cancer cell proliferation activity, and induces apoptosis.
(Pink: Wee1 ligand (HY-10993); Blue: Cereblon ligand (HY-41547); Black: linker (HY-W011561)).
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- Reinheit: 99.84%
- CAS. Nr.: 2414418-49-6
- Formel: C42H45N11O6
- Molecular Weight:799.88
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
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| MOLT-4 | IC50 |
390 nM
Compound: 12
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Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo Luminescent assay
Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo Luminescent assay
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[PMID: 38663873] |
Pomalidomide-C3-adavosertib (1 nM-10 μM; 24-72 h) induces CRBN-dependent anti-proliferative effects and synergized with Olaparib (HY-10162)[1].
Pomalidomide-C3-adavosertib (100 nM; 24 h) induces DNA damage, apoptosis, and deregulation of the G2/M checkpoint[1].
Pomalidomide-C3-adavosertib (1 nM-10 μM; 6 h) degrades Wee1 in MOLT4 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OVCAR8, COV362, and Kuramochi cells
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Concentration:1 nM-10 μM
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Incubation Time:24, 48, and 72 hours
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Result:Degraded Wee1 in OVCAR8 cells, with maximal degradation observed at a 100 nM treatment.
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Cell Line:MOLT4 cells
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Concentration:100 nM
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Incubation Time:24 hours
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Result:Led to reduced pCDKl Y15, increased apoptosis, and increased unrepaired DNA.
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Cell Line:MOLT4 cells
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Concentration:1 nM-10 μM
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Incubation Time:6 hours
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Result:Degraded Wee1 after a 6-hour treatment in MOLT4 cells, and induced the downstream changes expected from Wee1 loss-including a decrease in phosphorylated cyclin-dependent kinase 1 (pCDK1) and an increase in pH 3.
Chemical Information
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CAS. Nr. 2414418-49-6
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Appearance Solid
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Molecular Weight 799.88
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Formel C42H45N11O6
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Color Light yellow to yellow
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SMILES
O=C1N(CC=C)N(C2=NC(C(O)(C)C)=CC=C2)C3=NC(NC4=CC=C(N5CCN(CCCNC6=CC=CC(C(N7C8CCC(NC8=O)=O)=O)=C6C7=O)CC5)C=C4)=NC=C31
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (62.51 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 1.25 mg/mL (1.56 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 1.2502 mL | 6.2509 mL | 12.5019 mL | 31.2547 mL |
| 5 mM | 0.2500 mL | 1.2502 mL | 2.5004 mL | 6.2509 mL | |
| 10 mM | 0.1250 mL | 0.6251 mL | 1.2502 mL | 3.1255 mL | |
| 15 mM | 0.0833 mL | 0.4167 mL | 0.8335 mL | 2.0836 mL | |
| 20 mM | 0.0625 mL | 0.3125 mL | 0.6251 mL | 1.5627 mL | |
| 25 mM | 0.0500 mL | 0.2500 mL | 0.5001 mL | 1.2502 mL | |
| 30 mM | 0.0417 mL | 0.2084 mL | 0.4167 mL | 1.0418 mL | |
| 40 mM | 0.0313 mL | 0.1563 mL | 0.3125 mL | 0.7814 mL | |
| 50 mM | 0.0250 mL | 0.1250 mL | 0.2500 mL | 0.6251 mL | |
| 60 mM | 0.0208 mL | 0.1042 mL | 0.2084 mL | 0.5209 mL |
Pomalidomide-C3-adavosertib Related Classifications
HY-133618 Related Classifications
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