Lurbinectedin 是一种DNA小沟共价粘合剂，可抑制RMG1和RMG2，IC50值分别为1.25和1.16 nM。它具有高效的抗肿瘤活性。

Lurbinectedin is a DNA minor groove covalent binder. Lurbinectedin also shows effective anti-tumor activity.

Lurbinectedin inhibits RMG1 and RMG2 cell growth (IC50: 1.25 and 1.16 nM, respectively). Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant human ovarian clear cell carcinoma (CCC) cells in vitro[1]. Lurbinectedin-DNA adducts in living cells give rise to double-strand breaks, triggering S-phase accumulation, and apoptosis. Lurbinectedin is a new synthetic tetrahydroisoquinoline alkaloid that is currently in phase I clinical development for the treatment of solid tumors. The potent cytotoxic activity of Lurbinectedin is ascertained in a 23-cell line panel with a mean GI50 value of 2.7 nM[2].

Lurbinectedin inhibits tumor growth significantly with no weight loss of treated animals, in four murine xenograft models of human cancer[2]. Mouse CCC cell xenografts show that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 causes a significant synergistic effect[1].

497871-47-3

C41H44N4O10S

784.87

卢比克替定;PM01183

DMSO:15 mg/mL (19.11 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years