ZXH-4-130 TFA
Based on 2 publication(s) in Google Scholar
ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC). ZXH-4-130 TFA induces ~80% CRBN degradation at 10 nM in MM1.S cells.
(Pink: Cereblon ligand (HY-14658); Blue: VHL ligand (HY-125845); Black: linker (HY-W142804)).
For research use only. We do not sell to patients.
- Purity: 99.71%
- CAS No.: 2711006-67-4
- Formula: C48H59F3N6O11S
- Molecular Weight:985.08
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Storage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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
Publications Citing Use of MedChemExpress (MCE) ZXH-4-130 TFA
MoreAll PROTACs Isoforms
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Biological Activity
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VHL |
ZXH-4-130 (100 nM; 2 h pre-treatment; followed by 96-hour treatment with 1 μM of Pomalidomide) TFA prevents Pomalidomide (1 μM) cytotoxicity to a significant extent, ZXH-4-130 TFA has statistically significant amounts of prevention[1].
ZXH-4-130 TFA (pretreatment with 50 nM) rescues GSPT1 degradation induced by CC-885 in MM1.S cells[1].
ZXH-4-130 (100 nM; 2 h pre-treatment; followed by 6 h treatment with THAL-SNS-032)TFA induces nearly complete CRBN degradation, but THAL-SNS-032's activity against CDK9 is only partially prevented[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2711006-67-4
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Appearance Solid
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Molecular Weight 985.08
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Formula C48H59F3N6O11S
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Color Off-white to gray
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SMILES
O=C([C@H]1N(C([C@@H](NC(CCCCCCCCCCOC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5.OC(C(F)(F)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (2)
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Journal Impact Factor
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Most Recent
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J Med Chem
Discovery and Characterization of a First-In-Class HCK/BTK PROTAC DFCI-002-06 for the Treatment of MYD88 Mutated B Cell Malignancies. [Abstract]2026 Jan 22;69(2):1119-1134. PMID: 41482966 -
bioRxiv
Cholesterol Dysregulation Drives Seed-Dependent Tau Aggregation in Patient Stem Cell-Derived Models of Tauopathy. [Abstract]2023 Dec 12:2023.12.11.571147. PMID: 38168389
Solvent & Solubility
DMSO : 170 mg/mL (172.57 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 and light). 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 and light). 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 (274 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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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 (sealed storage, away from moisture and light). 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 | 1.0151 mL | 5.0757 mL | 10.1515 mL | 25.3786 mL |
| 5 mM | 0.2030 mL | 1.0151 mL | 2.0303 mL | 5.0757 mL | |
| 10 mM | 0.1015 mL | 0.5076 mL | 1.0151 mL | 2.5379 mL | |
| 15 mM | 0.0677 mL | 0.3384 mL | 0.6768 mL | 1.6919 mL | |
| 20 mM | 0.0508 mL | 0.2538 mL | 0.5076 mL | 1.2689 mL | |
| 25 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0151 mL | |
| 30 mM | 0.0338 mL | 0.1692 mL | 0.3384 mL | 0.8460 mL | |
| 40 mM | 0.0254 mL | 0.1269 mL | 0.2538 mL | 0.6345 mL | |
| 50 mM | 0.0203 mL | 0.1015 mL | 0.2030 mL | 0.5076 mL | |
| 60 mM | 0.0169 mL | 0.0846 mL | 0.1692 mL | 0.4230 mL | |
| 80 mM | 0.0127 mL | 0.0634 mL | 0.1269 mL | 0.3172 mL | |
| 100 mM | 0.0102 mL | 0.0508 mL | 0.1015 mL | 0.2538 mL |
ZXH-4-130 TFA Related Classifications
HY-132857A Related Classifications
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