PROTAC-O4I2
Based on 1 Customer Validation
PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells.
(Pink: SF3B1 ligand (HY-18772); Blue: Cereblon ligand (HY-41547); Black: linker (HY-W008296)).
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- Pureza: 99.56%
- No. CAS: 2785323-62-6
- Fòrmula: C29H29ClN6O5S
- Peso molecular:609.10
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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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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]|
Cereblon |
In Vitro
PROTAC-O4I2 introduces Thalidomide to ubiquitin E3 ligase cereblon (CRBN), which selectively degrades SF3B1 and inhibits tumor growth in cells[1].
PROTAC-O4I2 degrades and inhibits SF3B1 in K562 cells. PROTAC-O4I2 exhibits anti-proliferation effects on SF3B1 WT, SF3B1 OE, and SF3B1 K700E cells with IC50s of 228, 63, and 90 nM, respectively[1].
PROTAC-O4I2 induces FLAG-SF3B1 degradation in a concentration-dependent manner with a half maximal inhibitory concentration (IC50) value of 0.244 μM in K562 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 control cells (WT), cells overexpressing SF3B1 (OE), and cells expressing SF3B1K700E (K700E)
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Concentration:1 pM, 0.1 nM, 10 nM, 1 μM, 100 μM
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Incubation Time:72 hours
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Result:In K562 WT cells, the parental compound O4I2 exhibited a marginal anti-proliferation effect (IC50 >10 μM). In contrast, PROTAC-O4I2 showed significantly higher toxicity with an IC50 of 228 nM, nearly 3-fold less potent than pladienolide B (IC50, 76 nM). Cells overexpressing SF3B1 WT was slightly resistant to pladienolide B (IC50, 134 nM), but more sensitive to PROTAC-O4I2 (an IC50 value of 63 nM).
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Cell Line:K562 cell
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Concentration:1 μM
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Incubation Time:48 h
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Result:Induced cellular apoptosis s in cells expressing SF3B1WT or SF3B1K700E.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Drosophila melanogaster[1]
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Dosage:10 μM
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Administration:Flies were fed on a round filter paper loaded with PROTAC-O4I2 in a 5% sucrose solution, maintained at 18℃ and flipped into a freshly prepared vial every 2 days
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Result:Decreased stem cell activity, blocked the initiation and growth of tumor, and improved the survival of the Drosophila ISC tumor model.
Chemical Information
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No. CAS 2785323-62-6
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Appearance Solid
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Peso molecular 609.10
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Fòrmula C29H29ClN6O5S
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Color White to yellow
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SMILES
O=C(NCCCCCCNC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O)C4=CSC(NC5=CC=C(C=C5)Cl)=N4
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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 : 250 mg/mL (410.44 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: ≥ 2.08 mg/mL (3.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 (275 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 |
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| DMSO | 1 mM | 1.6418 mL | 8.2088 mL | 16.4177 mL | 41.0442 mL |
| 5 mM | 0.3284 mL | 1.6418 mL | 3.2835 mL | 8.2088 mL | |
| 10 mM | 0.1642 mL | 0.8209 mL | 1.6418 mL | 4.1044 mL | |
| 15 mM | 0.1095 mL | 0.5473 mL | 1.0945 mL | 2.7363 mL | |
| 20 mM | 0.0821 mL | 0.4104 mL | 0.8209 mL | 2.0522 mL | |
| 25 mM | 0.0657 mL | 0.3284 mL | 0.6567 mL | 1.6418 mL | |
| 30 mM | 0.0547 mL | 0.2736 mL | 0.5473 mL | 1.3681 mL | |
| 40 mM | 0.0410 mL | 0.2052 mL | 0.4104 mL | 1.0261 mL | |
| 50 mM | 0.0328 mL | 0.1642 mL | 0.3284 mL | 0.8209 mL | |
| 60 mM | 0.0274 mL | 0.1368 mL | 0.2736 mL | 0.6841 mL | |
| 80 mM | 0.0205 mL | 0.1026 mL | 0.2052 mL | 0.5131 mL | |
| 100 mM | 0.0164 mL | 0.0821 mL | 0.1642 mL | 0.4104 mL |
PROTAC-O4I2 Related Classifications
HY-141881 Related Classifications
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