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Lurbinectedin

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Chemical Structure| 497871-47-3 同义名 : PM01183;LY-01017;Tryptamicidin;PM-1183
CAS号 : 497871-47-3
货号 : A724881
分子式 : C41H44N4O10S
纯度 : 98%
分子量 : 784.874
MDL号 : MFCD22665743
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(22.93 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Lurbinectedin, a synthetic tetrahydroisoquinoline alkaloid in phase I clinical trials for solid tumors, forms DNA adducts causing double-strand breaks, S-phase accumulation, and apoptosis, with potent cytotoxicity confirmed by a mean GI50 value of 2.7 nM in a 23-cell line panel[2]. Lurbinectedin significantly reduces tumor growth in both chemosensitive and chemoresistant human ovarian clear cell carcinoma (CCC) cells in vitro and in mouse CCC cell xenografts. The combination of lurbinectedin and SN-38 exhibits a remarkable synergistic effect[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.27mL

0.25mL

0.13mL

6.37mL

1.27mL

0.64mL

12.74mL

2.55mL

1.27mL
参考文献

[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.

[3]Vidal A, et al. Lurbinectedin (PM01183), a new DNA minor groove binder, inhibits growth of orthotopic primary graft of NSC 119875-resistant epithelial ovarian cancer. Clin Cancer Res. 2012 Oct 1;18(19):5399-411.