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Lurbinectedin (PM01183) Sale

(Synonyms: 卢比克替定,PM01183) 目录号 : GC32834

Lurbinectedin (PM01183, PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA), a DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Lurbinectedin inhibits RMG1 and RMG2 cell growth with IC50 of 1.25 nM and 1.16 nM, respectively.

Lurbinectedin (PM01183) Chemical Structure

Cas No.:497871-47-3

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100μg
¥2,145.00
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1mg
¥5,850.00
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2mg
¥10,920.00
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Sample solution is provided at 25 µL, 10mM.

Description

Lurbinectedin (PM01183, PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA), a DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Lurbinectedin inhibits RMG1 and RMG2 cell growth with IC50 of 1.25 nM and 1.16 nM, respectively.

Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant CCC cells in vitro. Lurbinectedin plus SN-38 combination has strong synergistic effects on both the cisplatin-resistant and paclitaxel-resistant CCC cell lines.[1]

An examination of mouse CCC cell xenografts reveals that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 combination results in a significant synergistic effect. Everolimus significantly enhances the antitumor activity of lurbinectedin-based chemotherapies.[1]

[1] Ryoko Takahashi, et al. PLoS One. 2016 Mar 17;11(3):e0151050. [2] J F M Leal, et al. Br J Pharmacol. 2010 Nov;161(5):1099-110.

实验参考方法

Cell experiment:

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].

Animal experiment:

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) Cisplatin (3.5 mg/kg); and iv) Lurbinectedin plus cisplatin (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].

References:

[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 cisplatin-resistant epithelial ovarian cancer. Clin Cancer Res. 2012 Oct 1;18(19):5399-411.

化学性质

Cas No. 497871-47-3 SDF
别名 卢比克替定,PM01183
Canonical SMILES O[C@@H]([C@@](CC1=CC(C)=C2OC)([H])N(C)[C@]3([H])C1=C2O)N([C@](COC4=O)([H])C5=C(OCO6)C6=C7C)[C@@]3([H])[C@@](SC[C@@]4(NCC8)C9=C8C%10=CC(OC)=CC=C%10N9)([H])C5=C7OC(C)=O
分子式 C41H44N4O10S 分子量 784.87
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.2741 mL 6.3705 mL 12.741 mL
5 mM 0.2548 mL 1.2741 mL 2.5482 mL
10 mM 0.1274 mL 0.637 mL 1.2741 mL
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