NU223612
Based on 1 Customer Validation
NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a Kd of 640 nM. NU223612 potently degrades the IDO1 protein through CRBN-mediated proteasomal degradation. NU223612 is bound to CRBN with an affinity of 290 nM. NU223612 can cross the blood-brain barrier (BBB).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.41%
- CAS No.: 2759420-43-2
- Formule: C49H55FN6O9
- Masse moléculaire:890.99
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
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Activité biologique
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Cereblon |
IDO1 640 nM (Kd) |
NU223612 (0.1-10 μM; 24 h) decreases IDO1 protein levels dose-dependently[1].
A DC50 (the concentration of the NU223612 at which 50% of the IDO1 protein is degraded) of 0.3290 μM and 0.5438 μM in U87 and GBM43 cells is determined, respectively[1].
NU223612 degrades IDO1 protein in multiple cell types, such as CD18 and PANC-1 human pancreatic cancer cells, OVCAR5 and SKOV3 human ovarian cancer cells, PC3 human prostate cancer cells, and the syngeneic GL261 mouse IDO1 cDNA-expressing (IDO1-O/E) glioma cell line[1].
NU223612 equally degrades IDO1 protein levels in both the cytoplasmic and nuclear intracellular compartments in human GBM cells. NU223612 is able to penetrate subcellular compartments[1].
NU223612 dose-dependently inhibits IDO1 enzyme activity resulting in decreased Kyn levels in cultured IFNγ-stimulated GBM cells. NU223612 inhibits both IDO1-mediated tryptophan metabolism as well as IDO1 non-enzyme-mediated NF-κB p65 transcription factor DNA binding activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87 and human GBM43 cells
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Concentration:0 μM, 0.1 μM, 1 μM, and 10 μM
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Incubation Time:24 h
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Result:Decreased IDO1 protein levels dose-dependently.
NU223612 (25 mg/kg; i.p.; 5 days/week; for 3 weeks) leads to an increase in median overall survival as well as longer-term survival for up to 45 days post-tumor cell injection[1].
Mass spectrometry analysis of NU223612 (25 mg/kg; i.p.; once) shows a Cmax of 2 μM and a half-life of 8.3 h in brain tissue. In plasma, Cmax is 365 μM and the half-life is 2.5 h. The binding of NU223612 to mouse brain homogenate using a 6 h equilibrium dialysis shows NU223612 to be 99.8% bound[1].
Half-life, AUC, and Cmax of NU223612 in serum and brain samples[1].
| Plasma | Brain | |
| half-lifr (h) | 2.5 | 8.3 |
| AUC0-24 (μM h) | 582 | 7 |
| Cmax (μM) | 365 | 2 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice bearing GL261 cells[1]
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Dosage:25 mg/kg
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Administration:i.p.; once
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Result:Decreased IDO1 protein by >70% within 2 h post-treatment and remains low for up to 24 h.
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Animal Model:8 week old C57BL/6 wild-type (WT) mice are intracranially engrafted with luciferase-modified GL261 cells (GL261-luc.)[1]
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Dosage:25 mg/kg
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Administration:i.p.; 5 days/week; for 3 weeks
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Result:Led to an increase in median overall survival as well as longer-term survival for up to 45 days post-tumor cell injection.
Chemical Information
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CAS No. 2759420-43-2
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Appearance Solid
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Masse moléculaire 890.99
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Formule C49H55FN6O9
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Color White to yellow
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SMILES
O=C([C@H](C)[C@@]1([H])CC[C@](C2=CC=NC3=CC=C(F)C=C23)([H])CC1)NC4=CC=C(OC5CCN(C(CCOCCOCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)CC5)C=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (112.23 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)
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.
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.
Pureté et documentation
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Fiche technique (274 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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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. 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 | 1.1223 mL | 5.6117 mL | 11.2235 mL | 28.0587 mL |
| 5 mM | 0.2245 mL | 1.1223 mL | 2.2447 mL | 5.6117 mL | |
| 10 mM | 0.1122 mL | 0.5612 mL | 1.1223 mL | 2.8059 mL | |
| 15 mM | 0.0748 mL | 0.3741 mL | 0.7482 mL | 1.8706 mL | |
| 20 mM | 0.0561 mL | 0.2806 mL | 0.5612 mL | 1.4029 mL | |
| 25 mM | 0.0449 mL | 0.2245 mL | 0.4489 mL | 1.1223 mL | |
| 30 mM | 0.0374 mL | 0.1871 mL | 0.3741 mL | 0.9353 mL | |
| 40 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL | 0.7015 mL | |
| 50 mM | 0.0224 mL | 0.1122 mL | 0.2245 mL | 0.5612 mL | |
| 60 mM | 0.0187 mL | 0.0935 mL | 0.1871 mL | 0.4676 mL | |
| 80 mM | 0.0140 mL | 0.0701 mL | 0.1403 mL | 0.3507 mL | |
| 100 mM | 0.0112 mL | 0.0561 mL | 0.1122 mL | 0.2806 mL |
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