Zelebrudomide
Based on 1 publication(s) in Google Scholar
Zelebrudomide is an orally active BTK-targeting PROTAC degrader, with DC50 values of 4.5 nM and 31 nM against wild-type BTK and BTKC481S mutant, respectively. Zelebrudomide recruits the cereblon E3 ubiquitin ligase complex to mediate the degradation of BTK. Zelebrudomide also acts as a molecular glue to bind the cereblon E3 ubiquitin ligase complex, mediating the degradation of IKZF1 and IKZF3. Zelebrudomide can be used in the research of B-cell malignancies.
(Pink: Btk ligand (HY-168302); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-168348)).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.71%
- CAS 番号: 2416131-46-7
- 分子式: C39H45N9O5
- 分子量:719.83
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Zelebrudomide
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生物活性
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IKZF1 57 nM (DC50) |
IKZF3 36 nM (DC50) |
IL-2 |
Zelebrudomide (NX-2127) potently degrades wild-type BTK in TMD8 cells with a DC50 of 4.5 nM; it also degrades the BTKC481S mutant with a DC50 of 31 nM, despite its reduced binding affinity for this mutant[1].
Zelebrudomide (50 nM; 4 h) selectively degrades BTK in human peripheral blood mononuclear cells (PBMCs) from normal donors[1].
Zelebrudomide (0.001-100 nM; 1-24 h) degrades IKZF1 (DC50 = 57 nM) and IKZF3 (DC50 = 36 nM) in primary human T cells, and induces IL-2 secretion in TCR-activated primary human T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Zelebrudomide (10-100 mg/kg; p.o.; single dose, once daily for 14 consecutive days) induces potent, dose-dependent degradation of BTK and IKZF3 in cynomolgus monkeys[1].
Zelebrudomide (10-90 mg/kg; p.o.; once daily for 5 consecutive days, once daily for 25 consecutive days) induces dose-dependent anti-tumor efficacy in TMD8 BTKWT xenograft tumors and degrades BTK, IKZF1 and IKZF3[1].
Zelebrudomide (10-90 mg/kg; p.o.; daily administration for 25 days) exhibits dose-dependent antitumor efficacy in Ibrutinib (HY-10997)-resistant TMD8 BTKC481S xenograft tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice; CD-1 mice[1]
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Dosage:0.3, 3 mg/kg (single dose)
10, 30, 90 mg/kg (daily x5) -
Administration:p.o.; single dose; daily for 5 days
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Result:Suppressed mouse peripheral BTK in a dose-dependent fashion after single oral dosing across BALB/c and CD-1 strains.
Strengthened BTK suppression in BALB/c circulating B cells following five days of repeated oral administration with elevated inhibitory efficacy.
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Animal Model:BALB/c mice (xenograft model)[1]
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Dosage:10, 30, 90 mg/kg
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Administration:p.o.; daily for 25 days; daily for 5 days
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Result:Exerted dose-dependent tumor growth inhibition of 35%, 73% and 99% following 25 days of daily oral treatment at 10, 30 and 90 mg/kg.
Dose-dependently depleted intratumoral BTK to 24%, 14% and 5% of baseline after five days of oral administration.
Downregulated intratumoral IKZF1 to 74%, 56% and 27% and intratumoral IKZF3 to 82%, 48% and 23% in a dose-responsive manner under the 5-day dosing regimen.
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Animal Model:BALB/c mice (xenograft model)[1]
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Dosage:10, 30, 90 mg/kg
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Administration:p.o.; daily for 25 days
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Result:Achieved 17%, 43%, and 59% tumor growth inhibition (TGI), respectively.
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Animal Model:Cynomolgus monkeys[1]
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Dosage:10, 30, 100 mg/kg
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Administration:p.o.; single dose; daily for 14 days
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Result:Induced dose-dependent BTK downregulation in monkey peripheral B cells upon single-dose treatment, and sustained BTK suppression below 10% baseline after 14 consecutive daily oral doses.
Dose-dependently lowered IKZF3 content in monkey circulating T cells following the 14-day repeated oral dosing regimen.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2416131-46-7
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性状 Solid
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分子量 719.83
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分子式 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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別名
NX-2127
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (278 KB)
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取扱説明書 (2659 KB)
参考文献
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 |
Zelebrudomide 関連分類
HY-153220 関連分類
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