Lurbinectedin CAS# 497871-47-3
Lurbinectedin (PM01183) is a synthetic tetrahydroisoquinoline alkaloid related to trabectedin that binds covalently to the minor groove of DNA, inhibiting oncogenic transcription and inducing DNA double-strand breaks. In preclinical studies, lurbinectedin exhibited potent cytotoxic activity across a range of human tumor cell lines, with mean GI₅₀ values in the low nanomolar range (typically 1–10 nM) in breast, ovarian, small cell lung cancer (SCLC), and melanoma models. In xenograft mouse models, intravenous administration at 0.18–0.3 mg/kg produced significant tumor growth inhibition or regressions in ovarian, SCLC, and Ewing sarcoma models, correlating with suppression of RNA polymerase II–dependent transcription and increased γ-H2AX foci as a marker of DNA damage. Lurbinectedin also demonstrated synergistic antitumor effects when combined with doxorubicin or topotecan, supporting its development for chemoresistant solid tumors
📌 参考资料/链接：
He WM, Zhang ZG, Ma DW. A Scalable Total Synthesis of the Antitumor Agents Et-743 and Lurbinectedin. Agnew. Chem. Int. Ed. 2019, 58(12):3972-3975.
He WM, Zhang ZG, Ma DW. A Scalable Total Synthesis of the Antitumor Agents Et-743 and Lurbinectedin. Agnew. Chem. Int. Ed. 2019, 58(12):3972-3975.
📄 详细内容
CAS No. 497871-47-3 Lurbinectedin synthetic routes
He WM, Zhang ZG, Ma DW. A Scalable Total Synthesis of the Antitumor Agents Et-743 and Lurbinectedin. Agnew. Chem. Int. Ed. 2019, 58(12):3972-3975.
产品链接: CAS No. 497871-47-3 ››
He WM, Zhang ZG, Ma DW. A Scalable Total Synthesis of the Antitumor Agents Et-743 and Lurbinectedin. Agnew. Chem. Int. Ed. 2019, 58(12):3972-3975.
产品链接: CAS No. 497871-47-3 ››