FIZ1 degrader 1
Based on 1 Customer Validation
FIZ1 degrader 1 is an IMiD-based molecular glue degrader. FIZ1 degrader 1 induces CRBN-dependent FIZ1 ubiquitination and proteasomal degradation; inhibition of the proteasome, ubiquitination or ubiquitination-like processes blocks this degradation. FIZ1 degrader 1 also induces the degradation of IKZF1, IKZF3 and ZFP91. FIZ1 degrader 1 is applicable to molecular glue-related research.
For research use only. We do not sell to patients.
- Purity : 99.50%
- CAS No.: 1957235-62-9
- Formula: C16H15N3O4
- Molecular Weight:313.31
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
IKZF1 |
IKZF3 |
In Vitro
FIZ1 degrader 1 (compound 1) (5 μM; 13 h) induces the degradation of FIZ1, IKZF1, IKZF3 and ZFP91 in Jurkat cells[1].
FIZ1 degrader 1 (10 μM; 15 h) induces degradation of FLAG-tagged FIZ1 and endogenous IKZF3 in Jurkat cells[1].
FIZ1 degrader 1 (10 μM; 16 h) induces degradation of FLAG-tagged FIZ1 in HEK293T cells[1].
FIZ1 degrader 1 (5-20 μM; 0-24 h) induces dose- and time-dependent degradation of FLAG-tagged FIZ1 in HEK293T cells[1].
FIZ1 degrader 1 (20 μM; 13 h) induces degradation of FLAG-tagged FIZ1 in HEK293T cells; this degradation is blocked when the compound is administered at 20 μM for 13 h in combination with a neddylation inhibitor, proteasome inhibitor, or ubiquitination inhibitor[1].
FIZ1 degrader 1 (10 μM; 24 h) induces CRBN-dependent degradation of FLAG-tagged FIZ1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human Jurkat cells stably expressing FIZ1-nluc-FLAG
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Concentration:10 μM
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Incubation Time:15 h
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Result:Reduced levels of FLAG-tagged FIZ1 and endogenous IKZF3 compared to DMSO-treated controls.
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Cell Line:human HEK293T cells stably expressing FIZ1-nluc-FLAG
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Concentration:10 μM
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Incubation Time:16 h
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Result:Reduced levels of FLAG-tagged FIZ1 compared to DMSO-treated controls.
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Cell Line:human HEK293T cells stably expressing FIZ1-nluc-FLAG
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Concentration:20 μM (FIZ1 degrader 1)
1 μM neddylation inhibitor, 1 μM proteasome inhibitor, 10 μM ubiquitination inhibitor (inhibitor co-treatments) -
Incubation Time:13 h
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Result:Blocked degradation of FLAG-tagged FIZ1 induced by FIZ1 degrader 1 when co-treated with inhibitors of neddylation, proteasome, or ubiquitination pathways.
Indicated the degradation is CRBN-dependent and requires functional ubiquitin-proteasome system machinery.
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Cell Line:CRBN-knockout and CRBN-reconstituted human RKO cells stably expressing FIZ1-nluc-FLAG
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Concentration:10 μM
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Incubation Time:24 h
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Result:Induced degradation of FLAG-tagged FIZ1 in CRBN-reconstituted cells.
Did not induce degradation of FLAG-tagged FIZ1 in CRBN-knockout cells.
Confirmed CRBN-dependent degradation.
Chemical Information
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CAS No. 1957235-62-9
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Appearance Solid
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Molecular Weight 313.31
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Formula C16H15N3O4
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Color Light yellow to yellow
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SMILES
O=C1CCC(C(N1)=O)N2C(C3=CC=CC(NC4CC4)=C3C2=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
In Vitro:
DMSO : 33.33 mg/mL (106.38 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: ≥ 2.5 mg/mL (7.98 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 (7.98 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 (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.
Purity & Documentation
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Data Sheet (289 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 |
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| DMSO | 1 mM | 3.1917 mL | 15.9586 mL | 31.9173 mL | 79.7932 mL |
| 5 mM | 0.6383 mL | 3.1917 mL | 6.3835 mL | 15.9586 mL | |
| 10 mM | 0.3192 mL | 1.5959 mL | 3.1917 mL | 7.9793 mL | |
| 15 mM | 0.2128 mL | 1.0639 mL | 2.1278 mL | 5.3195 mL | |
| 20 mM | 0.1596 mL | 0.7979 mL | 1.5959 mL | 3.9897 mL | |
| 25 mM | 0.1277 mL | 0.6383 mL | 1.2767 mL | 3.1917 mL | |
| 30 mM | 0.1064 mL | 0.5320 mL | 1.0639 mL | 2.6598 mL | |
| 40 mM | 0.0798 mL | 0.3990 mL | 0.7979 mL | 1.9948 mL | |
| 50 mM | 0.0638 mL | 0.3192 mL | 0.6383 mL | 1.5959 mL | |
| 60 mM | 0.0532 mL | 0.2660 mL | 0.5320 mL | 1.3299 mL | |
| 80 mM | 0.0399 mL | 0.1995 mL | 0.3990 mL | 0.9974 mL | |
| 100 mM | 0.0319 mL | 0.1596 mL | 0.3192 mL | 0.7979 mL |
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