Zelebrudomide
Based on 1 publication(s) in Google Scholar
Zelebrudomide (NX-2127) (Compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk). Zelebrudomide inhibits proliferation of BTKC481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). Zelebrudomide catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. Zelebrudomide stimulates T cell activation and increases IL-2 production in primary human T Cells. (Pink: BTK ligand 10 (HY-168302); Black: (R)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168348); Blue: Thalidomide 5-fluoride (HY-W087383)
(Pink: Btk ligand (HY-168302); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-168303)).
For research use only. We do not sell to patients.
- Purity: 98.71%
- CAS No.: 2416131-46-7
- Formula: C39H45N9O5
- Molecular Weight:719.83
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from 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
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Kinase Inhibitor Library
HY-L009
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Protein Tyrosine Kinase Compound Library
HY-L016
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Anti-Cancer Compound Library
HY-L025
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HY-L026
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HY-L061
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HY-L079
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HY-L151
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Serine/Threonine Kinase Inhibitor Library
HY-L164
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HY-L171
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MCE Bioactive Compound Library
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Anti-Rheumatic Arthritis Compound Library
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Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) Zelebrudomide
MoreAll PROTACs Isoforms
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Biological Activity
Zelebrudomide (po) leads to dose-proportional exposure in plasma and BTK degradation to <10% of baseline levels in circulating and splenic B cells[1].
Zelebrudomide results in superior tumor growth inhibition (TGI) in both WT TMD8 and C481S mutant xenograft models in mouse[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2416131-46-7
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Appearance Solid
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Molecular Weight 719.83
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Formula C39H45N9O5
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Color Light yellow to yellow
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SMILES
O=C1C2=CC(N3C[C@H](CN4CCC(C5=CC=C(C=C5)NC6=C(N=CC(N7CCCCC7)=N6)C(N)=O)CC4)CC3)=CC=C2C(N1C8C(NC(CC8)=O)=O)=O
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Synonyms
NX-2127
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Blood Adv
PLCG2 Exon-Skipped Variants: Insights into Their Potential Role in Chronic Lymphocytic Leukemia. [Abstract]2026 Jun 5:bloodadvances.2025019077. PMID: 42263669
Solvent & Solubility
DMSO : 100 mg/mL (138.92 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 (protect from 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 (protect from 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)
Purity & Documentation
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Data Sheet (273 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 (protect from 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 | 1.3892 mL | 6.9461 mL | 13.8922 mL | 34.7304 mL |
| 5 mM | 0.2778 mL | 1.3892 mL | 2.7784 mL | 6.9461 mL | |
| 10 mM | 0.1389 mL | 0.6946 mL | 1.3892 mL | 3.4730 mL | |
| 15 mM | 0.0926 mL | 0.4631 mL | 0.9261 mL | 2.3154 mL | |
| 20 mM | 0.0695 mL | 0.3473 mL | 0.6946 mL | 1.7365 mL | |
| 25 mM | 0.0556 mL | 0.2778 mL | 0.5557 mL | 1.3892 mL | |
| 30 mM | 0.0463 mL | 0.2315 mL | 0.4631 mL | 1.1577 mL | |
| 40 mM | 0.0347 mL | 0.1737 mL | 0.3473 mL | 0.8683 mL | |
| 50 mM | 0.0278 mL | 0.1389 mL | 0.2778 mL | 0.6946 mL | |
| 60 mM | 0.0232 mL | 0.1158 mL | 0.2315 mL | 0.5788 mL | |
| 80 mM | 0.0174 mL | 0.0868 mL | 0.1737 mL | 0.4341 mL | |
| 100 mM | 0.0139 mL | 0.0695 mL | 0.1389 mL | 0.3473 mL |
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