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, 静脉注射, 单次给药) 可增强 HT1080 肿瘤小鼠肿瘤组织中 Doxorubicin (HY-15142A) 的暴露，同时降低心脏和肾脏中的暴露^[1]。
Legubicin (静脉注射, 单次给药, 56 天观察) 在雌性 SD 大鼠和比格犬中显示出高于常规 Doxorubicin (HY-15142A) 的最大耐受剂量 (MTD)，且毒性表现较轻^[1]。
Legubicin (5-25 mg/kg, 静脉注射, 每周一次, 4 周) 在 SD 大鼠中诱导剂量依赖性毒性^[1]。
Legubicin (3/1.5-20/10 mg/kg, 静脉注射, 每周一次, 4 周) 在比格犬中 20/10 mg/kg 剂量导致 80% 死亡率^[1]。
Legubicin (5-50 mg/kg, 腹腔注射, 每隔 2 天一次, 共 3 次) 在携带 CT26 肿瘤的 Balb/C 小鼠或携带 legumain²⁹³ 的 WEHI 裸鼠中可完全抑制肿瘤生长，且未见明显毒性^[2]。

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

1013.05

C₄₈H₆₄N₆O₁₈

606967-53-7

固体

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)

• [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]