Lurbinectedin-d3(Synonyms: PM01183-d3)

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-d3 (Synonyms: PM01183-d3)

Lurbinectedin D3 是 Lurbinectedin 的氘代物。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-d3(Synonyms: PM01183-d3)

Lurbinectedin-d3 Chemical Structure

规格 价格 是否有货 数量
100 μg ¥6800 In-stock
500 μg ¥15000 In-stock
1 mg ¥24000 In-stock
5 mg   询价  
10 mg   询价  

* Please select Quantity before adding items.

生物活性

Lurbinectedin D3 is deuterium labeled Lurbinectedin. 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[1].

分子量

787.89

Formula

C41H41D3N4O10S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Lurbinectedin-d3(Synonyms: PM01183-d3)

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-d3 (Synonyms: PM01183-d3)

Lurbinectedin D3 是 Lurbinectedin 的氘代物。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-d3(Synonyms: PM01183-d3)

Lurbinectedin-d3 Chemical Structure

规格 价格 是否有货 数量
100 μg ¥6800 In-stock
500 μg ¥15000 In-stock
1 mg ¥24000 In-stock
5 mg   询价  
10 mg   询价  

* Please select Quantity before adding items.

生物活性

Lurbinectedin D3 is deuterium labeled Lurbinectedin. 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[1].

分子量

787.89

Formula

C41H41D3N4O10S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Lurbinectedin-d3(Synonyms: PM01183-d3)

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-d3 (Synonyms: PM01183-d3)

Lurbinectedin D3 是 Lurbinectedin 的氘代物。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-d3(Synonyms: PM01183-d3)

Lurbinectedin-d3 Chemical Structure

规格 价格 是否有货 数量
100 μg ¥6800 In-stock
500 μg ¥15000 In-stock
1 mg ¥24000 In-stock
5 mg   询价  
10 mg   询价  

* Please select Quantity before adding items.

生物活性

Lurbinectedin D3 is deuterium labeled Lurbinectedin. 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[1].

分子量

787.89

Formula

C41H41D3N4O10S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Lurbinectedin(Synonyms: PM01183)

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(Synonyms: PM01183)

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  

* Please select Quantity before adding items.

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]

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.

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.

Clinical Trial

分子量

784.87

Formula

C41H44N4O10S

CAS 号

497871-47-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 20 mg/mL (25.48 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2741 mL 6.3705 mL 12.7410 mL
5 mM 0.2548 mL 1.2741 mL 2.5482 mL
10 mM 0.1274 mL 0.6370 mL 1.2741 mL

*

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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-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。

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.

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.

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
  • [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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务