Lurbinectedin (PM01183) is aDNAminor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth withIC₅₀values of 1.25 and 1.16 nM, respectively.

IC50: 1.25 nM (RMG1), 1.16 nM (RMG2)^[1]

PM01183 is a new synthetic tetrahydroisoquinoline alkaloid that is currently in phase I clinical development for the treatment of solid tumours. PM01183–DNA adducts in living cells give rise to double-strand breaks, triggering S-phase accumulation and apoptosis. The potent cytotoxic activity of PM01183 is ascertained in a 23-cell line panel with a mean GI₅₀value of 2.7 nM^[2]. Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant human ovarian clear cell carcinoma (CCC) cellsin vitro^[1].

Mouse CCC cell xenografts reveals that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 results in a significant synergistic effect^[1]. In four murine xenograft models of human cancer, PM01183 inhibits tumour growth significantly with no weight loss of treated animals^[2]. Single lurbinectedin or NSC 119875-combined therapies are effective in treating NSC 119875-sensitive and NSC 119875-resistant preclinical ovarian tumor models. The strongest synergistic effect is observed for combined treatments, especially in NSC 119875-resistant tumors. Lurbinectedin tumor growth inhibition is associated with reduced proliferation, increased rate of aberrant mitosis, and subsequent induced apoptosis^[3].

784.87

Solid

C₄₁H₄₄N₄O₁₀S

497871-47-3

Room temperature in continental US; may vary elsewhere.

DMSO : 20 mg/mL(25.48 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。