PROTAC STAT3 degrader-3
Based on 1 Customer Validation
PROTAC STAT3 degrader-3 is a STAT3 PROTAC degrader. PROTAC STAT3 degrader-3 recruits the E3 ubiquitin ligase CRBN and induces the degradation of STAT3 protein. PROTAC STAT3 degrader-3 inhibits the proliferation of malignant tumor cells. PROTAC STAT3 degrader-3 can be used for the research of non-small cell lung cancer and liver cancer.
(Pink: STAT3 ligand (HY-163526); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W008279)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.75%
- No. CAS: 3033746-17-4
- Fòrmula: C33H29F5N6O9S
- Peso molecular:780.68
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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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
STAT3 |
In Vitro
PROTAC STAT3 degrader-3 (Compound S3D1) (96 h) inhibits the proliferation of H1299 and HepG2 cells, with IC50 values of 10.06 and 14.97 μM[1].
PROTAC STAT3 degrader-3 (1-20 μM; 0-48 h) induces concentration-dependent and time-dependent degradation of STAT3 protein in H1299 and HepG2 liver cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:H1299 non-small cell lung cancer cells and HepG2 hepatocellular carcinoma cells
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Concentration:1, 5, 10, 15 and 20 μM (24 h incubation); 5 μM (time-course incubation)
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Incubation Time:24 h (concentration gradient); 0, 3, 6, 12, 24, 30, 36 and 48 h (time-course)
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Result:Reduced STAT3 protein levels in a concentration-dependent manner after 24 h treatment with 1-20 μM, with higher concentrations causing more pronounced degradation.
Caused gradual reduction of STAT3 protein levels over 48 h of 5 μM treatment, with the degradation effect strengthening as incubation time increased.
Chemical Information
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No. CAS 3033746-17-4
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Appearance Solid
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Peso molecular 780.68
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Fòrmula C33H29F5N6O9S
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Color Light yellow to yellow
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SMILES
CN(S(=O)(C1=C(C(F)=C(C(F)=C1F)F)F)=O)CC(NC2=CC=C(C=C2)C(NCCOCCNC3=C4C(N(C(C4=CC=C3)=O)C5CCC(NC5=O)=O)=O)=O)=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 (128.09 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: ≥ 2.5 mg/mL (3.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Protocolo
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Liver Cancer Modeling
Liver cancer can be classified into primary liver cancer and secondary liver cancer. Secondary liver cancer is the metastatic liver cancer. Primary liver cancer includes hepatocellular carcinoma (HCC), intrahepatic cholangiocarcinoma (ICC) and fibrolamellar HCC, of which HCC is the most common form, accounting for approximately 90% of primary liver cancers[1]. HCC mouse models include chemical agent-induced models, transplanted tumor models, and genetic engineered models.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureza y Documentación
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Ficha de datos (272 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 | 1.2809 mL | 6.4047 mL | 12.8093 mL | 32.0234 mL |
| 5 mM | 0.2562 mL | 1.2809 mL | 2.5619 mL | 6.4047 mL | |
| 10 mM | 0.1281 mL | 0.6405 mL | 1.2809 mL | 3.2023 mL | |
| 15 mM | 0.0854 mL | 0.4270 mL | 0.8540 mL | 2.1349 mL | |
| 20 mM | 0.0640 mL | 0.3202 mL | 0.6405 mL | 1.6012 mL | |
| 25 mM | 0.0512 mL | 0.2562 mL | 0.5124 mL | 1.2809 mL | |
| 30 mM | 0.0427 mL | 0.2135 mL | 0.4270 mL | 1.0674 mL | |
| 40 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8006 mL | |
| 50 mM | 0.0256 mL | 0.1281 mL | 0.2562 mL | 0.6405 mL | |
| 60 mM | 0.0213 mL | 0.1067 mL | 0.2135 mL | 0.5337 mL | |
| 80 mM | 0.0160 mL | 0.0801 mL | 0.1601 mL | 0.4003 mL | |
| 100 mM | 0.0128 mL | 0.0640 mL | 0.1281 mL | 0.3202 mL |
PROTAC STAT3 degrader-3 Related Classifications
HY-163502 Related Classifications
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