BT-O2C
Based on 1 Customer Validation
BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC:DUX4 sarcoma (CDS) cell lines (IC50 ranges from 152 to 221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer.
(Pink: p300 ligand (HY-174868); Blue: Cereblon ligand (HY-W023573); Black: linker).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.31%
- CAS. Nr.: 3055107-34-8
- Formel: C48H48F5N9O8
- Molecular Weight:973.94
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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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p300 |
Cereblon |
BT-O2C (0.1-10 μM, 24 h) can significantly degrade p300 and has almost no effect on the degradation of CBP in HAPI cells[1].
BT-O2C (0.25-4 μM, 48-72 h) exhibits significant cytotoxicity in NCC-CDS1-X1 (IC50 = 152 nM) and KITRA (IC50 = 221 nM) cells[1].
BT-O2C (4 μM, 6 h) significantly reduces the expression of CDS target genes in NCC-CDS-X1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HAPI cells
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Concentration:0.1, 1 and 10 μM
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Incubation Time:24 h
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Result:Selectively degraded the protein level of p300, superior to JQAD1 (HY-145765).
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Cell Line:NCC-CDS-X1 cells
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Concentration:4 μM
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Incubation Time:6 h
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Result:Significantly reduced the expression of ETV1, ETV4, ETV5, CCNEE1 and MYC.
Chemical Information
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CAS. Nr. 3055107-34-8
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Appearance Solid
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Molecular Weight 973.94
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Formel C48H48F5N9O8
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Color Light yellow to yellow
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SMILES
O=C(N(CC1=CC=C(F)C=C1)[C@@H](C)C(F)(F)F)CN(C(N[C@]23C[C@@H](F)C4=C3C=CC(C5=CN(CC(NCCCCCCCNC6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7=O)=O)C=C6)=O)N=C5)=C4)=O)C2=O
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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 : 100 mg/mL (102.68 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.
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 (270 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0268 mL | 5.1338 mL | 10.2676 mL | 25.6689 mL |
| 5 mM | 0.2054 mL | 1.0268 mL | 2.0535 mL | 5.1338 mL | |
| 10 mM | 0.1027 mL | 0.5134 mL | 1.0268 mL | 2.5669 mL | |
| 15 mM | 0.0685 mL | 0.3423 mL | 0.6845 mL | 1.7113 mL | |
| 20 mM | 0.0513 mL | 0.2567 mL | 0.5134 mL | 1.2834 mL | |
| 25 mM | 0.0411 mL | 0.2054 mL | 0.4107 mL | 1.0268 mL | |
| 30 mM | 0.0342 mL | 0.1711 mL | 0.3423 mL | 0.8556 mL | |
| 40 mM | 0.0257 mL | 0.1283 mL | 0.2567 mL | 0.6417 mL | |
| 50 mM | 0.0205 mL | 0.1027 mL | 0.2054 mL | 0.5134 mL | |
| 60 mM | 0.0171 mL | 0.0856 mL | 0.1711 mL | 0.4278 mL | |
| 80 mM | 0.0128 mL | 0.0642 mL | 0.1283 mL | 0.3209 mL | |
| 100 mM | 0.0103 mL | 0.0513 mL | 0.1027 mL | 0.2567 mL |