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/ Lurbinectedin

Lurbinectedin {[allProObj[0].p_purity_real_show]}

货号：A724881 同义名： PM01183; LY-01017

Lurbinectedin是一种DNA小沟共价结合剂，具有强效抗肿瘤活性。它通过与DNA的小沟结合，干扰DNA的转录和复制过程，对多种实体瘤表现出良好的治疗效果。

Lurbinectedin 化学结构 CAS号：497871-47-3
Lurbinectedin 化学结构
CAS号：497871-47-3
Lurbinectedin 3D分子结构
CAS号：497871-47-3
Lurbinectedin 化学结构 CAS号：497871-47-3
Lurbinectedin 3D分子结构 CAS号：497871-47-3
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Lurbinectedin 纯度/质量文件 产品仅供科研

货号：A724881 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
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产品名称 DNA synthesis ↓ helicase ↓ RdRp ↓ ribonucleotide reductase ↓ tRNA synthetase ↓ YB-1 ↓ 其他靶点 纯度
Fexinidazole ✔ 98%
Daptomycin ✔ 98%
Blasticidin S·HCl ✔ 98%
Metronidazole ✔ 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

 		98%
Triglycidyl isocyanurate ✔ p53 98+%
Nedaplatin ✔ 99%+
Oxolinic acid ✔ 98+%
Bendamustine ✔ 98+%
Trifluridine ✔ 98%
Robinetin ✔ 99%+
Carboplatin ✔ 99%
Cidofovir ✔ 99%
Cisplatin ✔ 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

 		98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

 		99%+
Oxaliplatin ✔ 98%
YK-4-279 ✔ 99%+
ML216 +

BLMfull-length, IC50: 2.98 μM

BLM636-1298, IC50: 0.97 μM

 		99%+
RK-33 ✔ 98%
Brr2-IN-3 ✔ 99%+
Phen-DC3 Trifluoromethanesulfonate ✔ 95%
Favipiravir ✔ 99%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

 		99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

 		97%
Didox ✔ 98%
(E)-3-AP ✔ 99%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

 		99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, IC50: 46.11 nM

Leucyl-tRNA synthetase, Kd: 42.1 nM

 		98%
SU056 +

YB-1, IC50: 1.73 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Lurbinectedin 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].
体内研究

Furthermore, Lurbinectedin markedly diminishes tumor growth in four murine xenograft models of human cancer without causing weight loss in treated animals[2].

Both single lurbinectedin treatments and those combined with NSC 119875 prove effective in NSC 119875-sensitive and -resistant preclinical ovarian tumor models. The most significant synergistic effect occurs in NSC 119875-resistant tumors, with lurbinectedin's effectiveness linked to reduced cell proliferation, increased aberrant mitosis rates, and induced apoptosis[3].
体外研究

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].

Lurbinectedin 细胞实验

Cell Line
Concentration Treated Time Description References
H720 cells 10 nM 8 hours Evaluate the effect of Lurbinectedin on H720 cells, results showed increased expression of IFNα, IFNβ, IFNγ, CCL5, and CXCL10 Cell Rep Med. 2024 Dec 17;5(12):101852
H661 cells 10 nM 16 hours Evaluate the effect of Lurbinectedin on H661 cells, results showed increased expression of IFNα, IFNβ, IFNγ, and CCL5 Cell Rep Med. 2024 Dec 17;5(12):101852
H1048 cells 10 nM 8 hours Evaluate the effect of Lurbinectedin on H1048 cells, results showed increased micronuclei formation Cell Rep Med. 2024 Dec 17;5(12):101852
H196 cells 10 nM 8 hours Evaluate the effect of Lurbinectedin on H196 cells, results showed STING pathway activation Cell Rep Med. 2024 Dec 17;5(12):101852
DMS114 cells 10 nM 8 hours Evaluate the effect of Lurbinectedin on DMS114 cells, results showed STING pathway activation Cell Rep Med. 2024 Dec 17;5(12):101852
H526 cells 10 nM 8 hours Evaluate the effect of Lurbinectedin on H526 cells, results showed STING pathway activation Cell Rep Med. 2024 Dec 17;5(12):101852
H446 cells 10 nM 8 hours Evaluate the effect of Lurbinectedin on H446 cells, results showed STING pathway activation Cell Rep Med. 2024 Dec 17;5(12):101852
H69 cells 10 nM 24 hours Evaluate the effect of Lurbinectedin on H69 cells, results showed significant reduction in cell viability Cell Rep Med. 2024 Dec 17;5(12):101852
TC32 cells 5 nmol/L 18 hours Suppressed the expression of the EWS-FLI1 downstream target proteins NR0B1, EZH2, and ID2 Cancer Res. 2016 Nov 15;76(22):6657-6668
TC32 cells 5 nmol/L 12 hours Reproduced the effect of siRNA silencing of EWS-FLI1 Cancer Res. 2016 Nov 15;76(22):6657-6668
TC32 cells 5 nmol/L 8 hours Suppressed an EWS-FLI1-driven (NR0B1) luciferase reporter to 42% of control Cancer Res. 2016 Nov 15;76(22):6657-6668
TC32 cells 5 nmol/L 6 hours EWS-FLI1 redistributed to the nucleolus to the same degree as trabectedin at 5 nmol/L Cancer Res. 2016 Nov 15;76(22):6657-6668
H196 10nM 8 hours Activates the cGAS-STING pathway and interferon chemokine signaling Cell Rep Med. 2025 Feb 18;6(2):101944
H446 10nM 8 hours Activates the cGAS-STING pathway and interferon chemokine signaling Cell Rep Med. 2025 Feb 18;6(2):101944
H526 10nM 8 hours Activates the cGAS-STING pathway and interferon chemokine signaling Cell Rep Med. 2025 Feb 18;6(2):101944
H82 10nM 8 hours Activates the cGAS-STING pathway and interferon chemokine signaling Cell Rep Med. 2025 Feb 18;6(2):101944
H69 10nM 8 hours Activates the cGAS-STING pathway and interferon chemokine signaling Cell Rep Med. 2025 Feb 18;6(2):101944
DMS114 10nM 8 hours Activates the cGAS-STING pathway and interferon chemokine signaling Cell Rep Med. 2025 Feb 18;6(2):101944
SCLC-A (H69, H146, H720) 1.905 to 30 nM 24 hours Evaluate the in vitro sensitivity of Lurbinectedin across different SCLC subtypes, showing relative resistance in SCLC-A subtype Clin Cancer Res. 2023 Sep 1;29(17):3526-3540
SCLC-P (H211, H526, CORL-311) 1.905 to 30 nM 24 hours Evaluate the in vitro sensitivity of Lurbinectedin across different SCLC subtypes, showing enhanced sensitivity in SCLC-P and SCLC-N subtypes Clin Cancer Res. 2023 Sep 1;29(17):3526-3540
Malignant pleural mesothelioma cells (MPM) IC50 concentration 24 hours Evaluate cell cycle and apoptosis, results showed Lurbinectedin induced S-phase cell cycle arrest and apoptosis J Exp Clin Cancer Res. 2024 Dec 21;43(1):327
Malignant pleural mesothelioma cells (MPM) 0.01 nM–100 nM 72 hours Evaluate the inhibitory effect on cell proliferation, results showed Lurbinectedin significantly reduced cell proliferation J Exp Clin Cancer Res. 2024 Dec 21;43(1):327
NCI-H82 cells 50 nM 4 h To evaluate the effect of lurbinectedin on NEUROD1-high SCLC cells, results showed 5,247 genes were downregulated EMBO Mol Med. 2022 Apr 7;14(4):e14841
NCI-H510A cells 50 nM 4 h To evaluate the effect of lurbinectedin on ASCL1-high SCLC cells, results showed 5,962 genes were downregulated EMBO Mol Med. 2022 Apr 7;14(4):e14841
DMS-53 cells 50 nM 4 h To study the effect of lurbinectedin on transcriptional activity in SCLC cells, results showed lurbinectedin binds CpG islands and arrests elongating RNAPII, leading to its degradation EMBO Mol Med. 2022 Apr 7;14(4):e14841

Lurbinectedin 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice TC71 or TC32 xenograft models Intravenously 0.18 mg/kg TC32: days 0 and 7; TC71: days 0, 7, and 14 Lurbinectedin alone or in combination with irinotecan inhibited xenograft growth and led to replacement of tumor tissue with benign fat cells Cancer Res. 2016 Nov 15;76(22):6657-6668.
Mice RPP and RPM genetically engineered mouse models Intravenous (i.v.) 0.2 mg/kg Once a week Evaluate the anti-tumor effect of Lurbinectedin alone or in combination with anti-PD-L1 antibody in SCLC mouse models, results showed significant tumor regression Cell Rep Med. 2024 Dec 17;5(12):101852
Nude mice TC71 or TC32 xenograft models Intravenous 0.18 mg/kg TC32 on days 0 and 7; TC71 on days 0, 7, and 14 Combination therapy with irinotecan led to tumor regression and complete reversal of EWS-FLI1 activity and elimination of established tumors in 30-70% of mice Cancer Res. 2016 Nov 15;76(22):6657-6668
Nude mice SCLC PDX models (LX110, LX33, LX1322) Intravenous 0.2 mg/kg Once a week, until the end of the experiment Evaluate the anti-tumor effect of Lurbinectedin in SCLC PDX models, showing significant response in LX110 (SCLC-A) model Clin Cancer Res. 2023 Sep 1;29(17):3526-3540
NOD SCID-γ (NSG) mice Patient-derived xenograft model (PDX) Intravenous injection 0.18 mg/kg Once per week for three weeks Evaluate the anti-tumor effect of Lurbinectedin in vivo, results showed it significantly reduced tumor growth J Exp Clin Cancer Res. 2024 Dec 21;43(1):327

Lurbinectedin 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.

Lurbinectedin 实验方案

计算器
存储液制备 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

Lurbinectedin 技术信息

CAS号497871-47-3
分子式C41H44N4O10S
分子量 784.87
SMILES Code O[C@@H]1N2[C@@]([C@]3([H])N(C)[C@@]1([H])CC4=CC(C)=C(OC)C(O)=C34)([H])[C@@]5([H])C6=C(OC(C)=O)C(C)=C(OCO7)C7=C6[C@]2([H])COC([C@]8(C9=C(CCN8)C%10=CC(OC)=CC=C%10N9)CS5)=O
MDL No. MFCD22665743
别名 PM01183; LY-01017; Tryptamicidin; PM-1183
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

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

Tags: Lurbinectedin | 497871-47-3 | PM01183 | LY-01017 | PM 01183 | PM-01183 | LY01017 | LY 01017 | LY-01017 | Cell Cycle/DNA Damage | DNA Alkylator/Crosslinker | DNA/RNA Synthesis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Lurbinectedin 纯度/质量文件 | Lurbinectedin 亚型比较 | Lurbinectedin 生物活性 | Lurbinectedin 参考文献 | Lurbinectedin 实验方案 | Lurbinectedin 技术信息

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