SB1-G-187
Based on 1 Customer Validation
SB1-G-187 is a multi-target kinase PROTAC degrader with activity against various kinases including GCK, YES1, IRAK1 and LYN. SB1-G-187 induces degradation of target kinases via a p97-dependent pathway, and forms ternary complexes with CRBN and specific functional kinases. SB1-G-187 can be used in tumor-related research.
(Pink: Lyn and Yes and IRAK1 ligand (HY-125142); Blue: Cereblon ligand (HY-A0003); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.70%
- No. CAS: 2769753-18-4
- Fòrmula: C52H54F3N9O10
- Peso molecular:1022.03
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Almacenamiento:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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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
Ver todos los productos específicos de isoformas PROTACs
MoreVer todos los productos específicos de isoformas MAP4K
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Cereblon |
Lyn |
CDK5 |
CDK14/Cyclin Y |
MAP4K2 |
IRAK1 |
In Vitro
SB1-G-187 (1 μM; 5 h) significantly degrades FER, BLK, IRAK1, MAP4K2, RIPK1, GAK, CDK5, CDK14, and LYN kinases in MOLT-4 cells[1].
SB1-G-187 (1 μM; 5 h) forms stable ternary complexes with YES1, IRAK1, and LYN kinases and CRBN in transiently transfected HEK293T cells[1].
SB1-G-187 (1 μM; 5 h) significantly degrades GAK, RIPK1, LYN, FER, and IRAK1 kinases in HEK293T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Chemical Information
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No. CAS 2769753-18-4
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Appearance Solid
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Peso molecular 1022.03
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Fòrmula C52H54F3N9O10
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Color White to light yellow
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SMILES
O=C1N(C2CCC(NC2=O)=O)C(C3=C1C=CC=C3OCC(NCCOCCOCCOCCCN4CCN(CC5=C(C(F)(F)F)C=C(NC(C6=CC(C#CC7=CN=C8N7N=CC=C8)=C(C)C=C6)=O)C=C5)CC4)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (97.84 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 (stored under nitrogen). 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 (stored under nitrogen). 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 (4.89 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. 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 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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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 (269 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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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 (stored under nitrogen). 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 | 0.9784 mL | 4.8922 mL | 9.7844 mL | 24.4611 mL |
| 5 mM | 0.1957 mL | 0.9784 mL | 1.9569 mL | 4.8922 mL | |
| 10 mM | 0.0978 mL | 0.4892 mL | 0.9784 mL | 2.4461 mL | |
| 15 mM | 0.0652 mL | 0.3261 mL | 0.6523 mL | 1.6307 mL | |
| 20 mM | 0.0489 mL | 0.2446 mL | 0.4892 mL | 1.2231 mL | |
| 25 mM | 0.0391 mL | 0.1957 mL | 0.3914 mL | 0.9784 mL | |
| 30 mM | 0.0326 mL | 0.1631 mL | 0.3261 mL | 0.8154 mL | |
| 40 mM | 0.0245 mL | 0.1223 mL | 0.2446 mL | 0.6115 mL | |
| 50 mM | 0.0196 mL | 0.0978 mL | 0.1957 mL | 0.4892 mL | |
| 60 mM | 0.0163 mL | 0.0815 mL | 0.1631 mL | 0.4077 mL | |
| 80 mM | 0.0122 mL | 0.0612 mL | 0.1223 mL | 0.3058 mL |
SB1-G-187 Related Classifications
HY-137342 Related Classifications
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