上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
Lurbinectedin (Synonyms: PM01183) 纯度: 99.91%
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 Chemical Structure
CAS No. : 497871-47-3
| 规格 | 价格 | 是否有货 | 数量 |
|---|---|---|---|
| 100 μg | ￥5500 | In-stock | |
| 1 mg | ￥15000 | In-stock | |
| 2 mg | ￥28000 | In-stock | |
| 5 mg | 询价 | ||
| 10 mg | 询价 |
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Lurbinectedin 相关产品
•相关化合物库:
- Drug Repurposing Compound Library Plus
- FDA-Approved Drug Library Plus
- Bioactive Compound Library Plus
| 生物活性 |
Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively. |
IC50 & Target |
IC50: 1.25 nM (RMG1), 1.16 nM (RMG2)[1] |
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| 体外研究 (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[2]. Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant human ovarian clear cell carcinoma (CCC) cells in vitro[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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| 体内研究 (In Vivo) |
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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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| Clinical Trial |
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| 分子量 |
784.87 |
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| Formula |
C41H44N4O10S |
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| CAS 号 |
497871-47-3 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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| 溶解性数据 |
In Vitro:
DMSO : 20 mg/mL (25.48 mM; Need ultrasonic) 配制储备液
*
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。 |
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| 参考文献 |
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| Cell Assay [1] |
The MTS assay is used to analyze the effects of each drug. Cells are plated in 96-well plates and treated with PM01183 (0, 0.1, 0.3, 1, 3 nM) . After 48 hours’ incubation, the number of surviving cells is assessed by determining the A490nm of the dissolved formazan product after the addition of MTS for 1 hour. Cell viability is calculated as follows: Aexp group / Acontrol×100[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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| Animal Administration [3] |
Mice: Mice are transplanted with fragments of OVAX1 and OVAX1R tumors, and when tumors reaches a homogeneous palpable size are randomly allocated into the treatment groups: i) Placebo; ii) Lurbinectedin (0.18 mg/kg); iii) NSC 119875 (3.5 mg/kg); and iv) Lurbinectedin plus NSC 119875 (0.18 + 3.5 mg/kg). Drugs are i.v. administered once per week for 3 consecutive weeks (days 0, 7, and 14). Seven days after the final dose (day 21), animals are sacrificed, their ovaries dissected out, and weighed. Representative fragments are either frozen in nitrogen or fixed and then processed for paraffin embedding[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
| 参考文献 |
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