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)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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)
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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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
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MedChemExpress（MCE）の使用を引用している文献 Zelebrudomide
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生物活性
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 |
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 (273 KB)
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SDS (252 KB)
- English - EN (252 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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