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).
For research use only. We do not sell to patients.
- Purity: 98.01%
- CAS No.: 606967-53-7
- Formula: C48H64N6O18
- Molecular Weight:1013.05
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Storage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Biological Activity
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.
Chemical Information
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CAS No. 606967-53-7
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Appearance Solid
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Molecular Weight 1013.05
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Formula 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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Synonyms
Doxorubicin-LNAA-Boc
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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 |