Legubicin
Based on 1 Customer Validation
Legubicin (Doxorubicin-LNAA-Boc) is a novel conjugate of Doxorubicin (HY-15142A) and a Legumain-cleavable peptide linker. Legubicin is activated by Legumain to release leucine-doxorubicin while sparing normal tissues. Legubicin inhibits tumor cell growth and reduces DNA binding in non-legumain expressing cells. Legubicin completely arrests tumor growth in mice bearing CT26 tumors. Legubicin can be used for the study of colon carcinoma (CRC).
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 : 98.01%
- CAS 番号: 606967-53-7
- 分子式: C48H64N6O18
- 分子量:1013.05
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
生物活性
製品説明
体内実験
Legubicin (i.v., single dose, 56-day observation) shows higher MTD than conventional Doxorubicin (HY-15142A) in female SD rats and in beagle dogs, with milder toxicity signs[1].
Legubicin (5-25 mg/kg, i.v., once weekly, 4 weeks) induces dose-dependent toxicity in SD rats[1].
Legubicin (3/1.5-20/10 mg/kg, i.v., once weekly, 4 weeks) causes 80% mortality at 20/10 mg/kg in beagle dogs[1].
Legubicin (5-50 mg/kg, i.p., 2-day intervals, 3 times) completely arrests tumor growth without evident toxicity in Balb/C mice bearing CT26 tumors or WEHI nude mice bearing legumain293[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 606967-53-7
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性状 Solid
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分子量 1013.05
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分子式 C48H64N6O18
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Color Orange to red
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SMILES
OC1=C2C(C(C3=C(OC)C=CC=C3C2=O)=O)=C(O)C([C@H]4O[C@@H]5C[C@@H]([C@@H]([C@@H](O5)C)O)NC([C@H](CC(C)C)NC([C@H](CC(N)=O)NC([C@H](C)NC([C@H](C)NC(OC(C)(C)C)=O)=O)=O)=O)=O)=C1C[C@](O)(C4)C(CO)=O
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別名
Doxorubicin-LNAA-Boc
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (49.36 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, 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 (protect from light, 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.
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 (276 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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取扱説明書 (2659 KB)
参考文献
[1]. Wang Y, et al. Biodistribution and preclinical safety profile of legubicin: A novel conjugate of doxorubicin and a legumain-cleavable peptide linker. J Appl Toxicol. 2024 Sep;44(9):1426-1445. [Content Brief]
[2]. Liu C, et al. Overexpression of legumain in tumors is significant for invasion/metastasis and a candidate enzymatic target for prodrug therapy. Cancer Res. 2003 Jun 1;63(11):2957-64. [Content Brief]
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, 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9871 mL | 4.9356 mL | 9.8712 mL | 24.6780 mL |
| 5 mM | 0.1974 mL | 0.9871 mL | 1.9742 mL | 4.9356 mL | |
| 10 mM | 0.0987 mL | 0.4936 mL | 0.9871 mL | 2.4678 mL | |
| 15 mM | 0.0658 mL | 0.3290 mL | 0.6581 mL | 1.6452 mL | |
| 20 mM | 0.0494 mL | 0.2468 mL | 0.4936 mL | 1.2339 mL | |
| 25 mM | 0.0395 mL | 0.1974 mL | 0.3948 mL | 0.9871 mL | |
| 30 mM | 0.0329 mL | 0.1645 mL | 0.3290 mL | 0.8226 mL | |
| 40 mM | 0.0247 mL | 0.1234 mL | 0.2468 mL | 0.6169 mL |