Lurbinectedin (PM01183) 是一种 DNA 小沟共价粘合剂，具有高效的抗肿瘤活性; 抑制RMG1和RMG2的IC₅₀值分别为1.25和1.16 nM。

Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC 50 values of 1.25 and 1.16 nM, respectively.

Solid

IC50: 1.25 nM (RMG1), 1.16 nM (RMG2)

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 GI50 value of 2.7 nM. Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant human ovarian clear cell carcinoma (CCC) cells in vitro . has not independently confirmed the accuracy of these methods. They are for reference only.

Mouse CCC cell xenografts reveals that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 results in a significant synergistic effect. In four murine xenograft models of human cancer, PM01183 inhibits tumour growth significantly with no weight loss of treated animals. 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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；In solvent -80°C 6 months

[1]. Takahashi R, et al. Preclinical Investigations of PM01183 (Lurbinectedin) as a Single Agent or in Combination with Other Anticancer Agents for Clear Cell Carcinoma of the Ovary. PLoS One. 2016 Mar 17;11(3):e0151050.
[2]. Leal JF, et al. PM01183, a new DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Br J Pharmacol. 2010 Nov;161(5):1099-110.

In Vitro: DMSO : 20 mg/mL (25.48 mM; Need ultrasonic)配制储备液