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- 详细信息
- 技术资料
- 保存条件:
Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
PM01183; LY-01017
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
497871-47-3
- 规格:
100 μg/1 mg/5 mg
| 规格: | 100 μg | 产品价格: | ¥2200.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥6500.0 |
| 规格: | 5 mg | 产品价格: | ¥9800.0 |
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Lurbinectedin
CAS No. : 497871-47-3
MCE 国际站:Lurbinectedin
产品活性: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。
研究领域:Cell Cycle/DNA Damage
作用靶点:DNA Alkylator/Crosslinker | DNA/RNA Synthesis
In Vitro: 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.
In Vivo: 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.
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