BT-O2C
Based on 1 Customer Validation
BT-O2C is a p300 PROTAC degrader. BT-O2C induces p300 degradation via proteasome- and ubiquitin-like modification-dependent pathways, downregulates the expression of CIC::DUX4 sarcoma target genes, and exerts cytotoxicity against such sarcoma cells. BT-O2C can be used in CIC::DUX4 sarcoma-related studies.
(Pink: p300 ligand (HY-174868); Blue: Cereblon ligand (HY-W023573); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.31%
- No. CAS: 3055107-34-8
- Fòrmula: C48H48F5N9O8
- Peso molecular:973.94
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
p300 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCC | IC50 |
152 nM
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Cytotoxic activity against human NCC-CDS-X1 CIC::DUX4 sarcoma cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay measuring ATP levels.
Cytotoxic activity against human NCC-CDS-X1 CIC::DUX4 sarcoma cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay measuring ATP levels.
|
40093518 |
In Vitro
BT-O2C (72 h) exhibits cytotoxicity against the CIC::DUX4 sarcoma cell lines NCC-CDS-X1 and KITRA, with IC50 values of 152 nM and 221 nM respectively after 72 hours of treatment[1].
BT-O2C (0.1-10 μM; 24-48 h) potently and selectively induces the degradation of p300 in HAP1 cells, and exhibits higher selectivity for p300 degradation over CBP[1].
BT-O2C (4 μM; 6 h) reduces the expression of CIC::DUX4 target genes ETV1, ETV4 and ETV5 in NCC-CDS-X1 cells, with no statistically significant difference compared with its negative control BT-O2C-N[1].
BT-O2C (4 μM; 24 h) slightly reduces the acetylation level of H3K27 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:CIC::DUX4 sarcoma (CDS) cell lines NCC-CDS-X1 and KITRA
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Concentration:0.25, 1.0, 4.0 μM
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Incubation Time:72 h
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Result:Exhibited cytotoxic activity in both CDS cell lines.
Achieved an IC50 of 152 nM in NCC-CDS-X1 cells after 72-hour incubation.
Achieved an IC50 of 221 nM in KITRA cells after 72-hour incubation.
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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:Reduced expression of CDS target genes ETV1, ETV4, and ETV5.
Showed no statistically significant difference in gene expression reduction compared to its negative control BT-O2C-N.
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Cell Line:NCC-CDS-X1 cells
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Concentration:4 μM
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Incubation Time:24 h
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Result:Caused a slight decrease in H3K27 acetylation.
Showed no clear effect on H3K18 acetylation.
Chemical Information
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No. CAS 3055107-34-8
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Appearance Solid
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Peso molecular 973.94
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
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.
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.
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.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
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 |
BT-O2C Related Classifications
HY-174866 Related Classifications
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