Legubicin  (Synonyms: Doxorubicin-LNAA-Boc)

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)^[1].

Legubicin (9.05 μmol/kg, i.v., single dose) enhances doxorubicin exposure in tumors and reduces it in heart/kidney in HT1080 tumor-bearing nude mice^[1].
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 legumain^293[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1013.05

C₄₈H₆₄N₆O₁₈

606967-53-7

Solid

Orange to red

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

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

* 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.

• [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]