PROTAC IDO1 Degrader-1
Based on 1 Customer Validation
PROTAC IDO1 Degrader-1 is a potent IDO1 (Indoleamine 2,3-dioxygenase 1) PROTAC degrader with a DC50 of 2.84 μM. PROTAC IDO1 Degrader-1 forms a ternary complex with IDO1 and the CRBN E3 ligase, and induces polyubiquitination of IDO1 followed by proteasomal degradation via the ubiquitin-proteasome system. PROTAC IDO1 Degrader-1 is applicable for related research on cancer immunity.
(Pink: IDO-1 ligand (HY-16987); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W050087)).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.00%
- CAS No.: 2488851-89-2
- Formule: C40H53BrFN9O13
- Masse moléculaire:966.80
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
IDO1 2.84 μM (DC50) |
IDO1 1.07 μM (IC50) |
Cereblon |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HeLa | IC50 |
37.43 μM
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Cytotoxicity against human HeLa cells assessed by MTT assay following 48 h incubation with the reagent.
Cytotoxicity against human HeLa cells assessed by MTT assay following 48 h incubation with the reagent.
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33163345 |
| HeLa | IC50 |
1.07 μM
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Cell-based IDO1 inhibitory activity against human HeLa cells assessed via kynurenine analysis.
Cell-based IDO1 inhibitory activity against human HeLa cells assessed via kynurenine analysis.
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33163345 |
| HeLa | DC50 |
2.84 μM
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Degradation of IFN-γ-upregulated IDO1 protein in human HeLa cells measured via Western blot following 24 h incubation with the reagent.
Degradation of IFN-γ-upregulated IDO1 protein in human HeLa cells measured via Western blot following 24 h incubation with the reagent.
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33163345 |
In Vitro
PROTAC IDO1 Degrader-1 (Compound 2c) exhibits weak cytotoxicity in HeLa cells at concentrations up to 40 μM after 48 h, with an IC50 of 37.43 μM; it can inhibit IDO1 activity in HeLa cells, with an IC50 of 1.07 μM[1].
PROTAC IDO1 Degrader-1 (5 μM; pretreatment for 24 h) moderately enhances the cytotoxic activity of HER-2 CAR-T cells against HeLa cells[1].
PROTAC IDO1 Degrader-1 (0.5-10 μM; 4-48 h) continuously degrades IDO1 upregulated by IFN-γ (HY-P7025) induction in HeLa cells in a dose-dependent manner via the ubiquitin-proteasome system, and significantly reduces the intracellular IDO1 fluorescent signal, with a DC50 of 2.84 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:0.5, 1, 2.5, 5, 10 μM
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Incubation Time:4, 8, 12, 24, 48 h
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Result:Significantly induced IDO1 protein degradation in a dose-dependent manner, with a maximum degradation (Dmax) of 93% and a half-maximal degradation concentration (DC50) of 2.84 μM.
Significantly decreased the IDO1 protein level induced by IFN-γ (5 ng/mL).
Caused persistent and almost complete IDO1 degradation that lasted up to 48 hours.
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Cell Line:IFN-γ-stimulated HeLa cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Dramatically reduced the intracellular IDO1 fluorescence signal, restoring it to the control group level.
Chemical Information
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CAS No. 2488851-89-2
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Appearance Solid
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Masse moléculaire 966.80
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Formule C40H53BrFN9O13
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Color Yellow to brown
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SMILES
O=C1C2=C(NCCOCCOCCOCCOCCOCCOCCOCCNCCNC3=NON=C3/C(NC4=CC(Br)=C(C=C4)F)=N/O)C=CC=C2C(N1C5C(NC(CC5)=O)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (103.43 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (2.59 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 (2.59 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Pureté et documentation
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Fiche technique (271 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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Instruction de manipulation (2659 KB)
Références
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 (sealed storage, away from moisture). 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 | 1.0343 mL | 5.1717 mL | 10.3434 mL | 25.8585 mL |
| 5 mM | 0.2069 mL | 1.0343 mL | 2.0687 mL | 5.1717 mL | |
| 10 mM | 0.1034 mL | 0.5172 mL | 1.0343 mL | 2.5859 mL | |
| 15 mM | 0.0690 mL | 0.3448 mL | 0.6896 mL | 1.7239 mL | |
| 20 mM | 0.0517 mL | 0.2586 mL | 0.5172 mL | 1.2929 mL | |
| 25 mM | 0.0414 mL | 0.2069 mL | 0.4137 mL | 1.0343 mL | |
| 30 mM | 0.0345 mL | 0.1724 mL | 0.3448 mL | 0.8620 mL | |
| 40 mM | 0.0259 mL | 0.1293 mL | 0.2586 mL | 0.6465 mL | |
| 50 mM | 0.0207 mL | 0.1034 mL | 0.2069 mL | 0.5172 mL | |
| 60 mM | 0.0172 mL | 0.0862 mL | 0.1724 mL | 0.4310 mL | |
| 80 mM | 0.0129 mL | 0.0646 mL | 0.1293 mL | 0.3232 mL | |
| 100 mM | 0.0103 mL | 0.0517 mL | 0.1034 mL | 0.2586 mL |
PROTAC IDO1 Degrader-1 Related Classifications
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