莱龙泰素

• 常用名: 莱龙泰素
• 英文名: Larotaxel
• CAS号: 156294-36-9
• 分子量: 831.901
• 密度: 1.4±0.1 g/cm3
• 沸点: 889.3±65.0 °C at 760 mmHg
• 分子式: C₄₅H₅₃NO₁₄
• 熔点: N/A
• 闪点: 491.7±34.3 °C

莱龙泰素用途

Larotaxel (XRP9881) 是一种紫杉烷类似物,具有抗紫杉烷抗性乳腺癌的临床前活性。Larotaxel (XRP9881) 通过促进微管蛋白装配和稳定微管发挥其细胞毒性作用,并最终通过细胞凋亡导致细胞死亡。Larotaxel (XRP9881) 具有穿越血脑屏障的能力,对 P-糖蛋白 1 的亲和力比 Docetaxel 低得多。

莱龙泰素名称

• 中文名: 莱龙泰素
• 英文名: (3ξ,5β,7β,10β)-4,10-Diacetoxy-1-hydroxy-13-{[(3S)-2-hydroxy-3-({[ (2-methyl-2-propanyl)oxy]carbonyl}amino)-3-phenylpropanoyl]oxy}-9 -oxo-5,20-epoxy-7,19-cyclotax-11-en-2-yl benzoate

莱龙泰素生物活性

• 描述: Larotaxel (XRP9881) 是一种紫杉烷类似物,具有抗紫杉烷抗性乳腺癌的临床前活性。Larotaxel (XRP9881) 通过促进微管蛋白装配和稳定微管发挥其细胞毒性作用,并最终通过细胞凋亡导致细胞死亡。Larotaxel (XRP9881) 具有穿越血脑屏障的能力,对 P-糖蛋白 1 的亲和力比 Docetaxel 低得多。
• 相关类别:
  信号通路 >> 细胞凋亡 >> 细胞凋亡
  研究领域 >> 癌症
• 参考文献:

  [1]. Diéras V, et al. Phase II multicenter study of larotaxel (XRP9881), a novel taxoid, in patients with metastatic breast cancer who previously received taxane-based therapy. Ann Oncol. 2008 Jul;19(7):1255-60.

  [2]. Morris PG, et al. Novel anti-tubulin cytotoxic agents for breast cancer. Expert Rev Anticancer Ther. 2009 Feb;9(2):175-85.

  [3]. Zatloukal P, et al. Randomized multicenter phase II study of larotaxel (XRP9881) in combination with cisplatin or gemcitabine as first-line chemotherapy in nonirradiable stage IIIB or stage IV non-small cell lung cancer. J Thorac Oncol. 2008 Aug;3(8):894-901.

莱龙泰素物理化学性质

• 密度: 1.4±0.1 g/cm3
• 沸点: 889.3±65.0 °C at 760 mmHg
• 分子式: C₄₅H₅₃NO₁₄
• 分子量: 831.901
• 闪点: 491.7±34.3 °C
• 精确质量: 831.346619
• PSA: 213.78000
• LogP: 7.06
• InChIKey: DXOJIXGRFSHVKA-BZVZGCBYSA-N
• SMILES: CC(=O)OC1C(=O)C23CC2CC2OCC2(OC(C)=O)C3C(OC(=O)c2ccccc2)C2(O)CC(OC(=O)C(O)C(NC(=O)OC(C)(C)C)c3ccccc3)C(C)=C1C2(C)C
• 蒸汽压: 0.0±0.3 mmHg at 25°C
• 折射率: 1.613
• 储存条件: -20°C，密封，干燥

莱龙泰素靶点实验

查看更多实验

实验名称：Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay 来源：ChEMBL 靶标：A549 External Id：CHEMBL4273410

实验名称：Resistance factor, ratio of IC50 for human MCF7/ADR cells to IC50 for human MCF7 cell... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4273409

实验名称：Resistance factor, ratio of IC50 for human paclitaxl resistant A549 cells to IC50 for... 来源：ChEMBL 靶标：A549 External Id：CHEMBL4273412

实验名称：Cytotoxicity against human paclitaxl resistant A549 cells after 72 hrs by sulforhodam... 来源：ChEMBL 靶标：A549 External Id：CHEMBL4273411

实验名称：Resistance factor, ratio of IC50 for human KB/VCR cells to IC50 for human KB cells 来源：ChEMBL 靶标：N/A External Id：CHEMBL4273406

实验名称：Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B assay 来源：ChEMBL 靶标：KB External Id：CHEMBL4273405

实验名称：Cytotoxicity against human MCF7/ADR cells after 72 hrs by sulforhodamine B assay 来源：ChEMBL 靶标：NCI/ADR-RES External Id：CHEMBL4273408

实验名称：Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay 来源：ChEMBL 靶标：MCF7 External Id：CHEMBL4273407

实验名称：Cytotoxicity against human KB/VCR cells after 72 hrs by sulforhodamine B assay 来源：ChEMBL 靶标：N/A External Id：CHEMBL4273404

实验名称：Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 40 nM af... 来源：ChEMBL 靶标：A549 External Id：CHEMBL4273414

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莱龙泰素英文别名

• acetylcyclopropyl docetaxel
• Valiolamine hydrate
• Valinolamine
• valiolamine
• acetocyclopropyl taxotere
• (2α,5β,7β,10β,13α)-4,10-Diacetoxy-1-hydroxy-13-{[(2R,3S)-2-hydroxy-3-({[(2-methyl-2-propanyl)oxy]carbonyl}amino)-3-phenylpropanoyl]oxy}-9-oxo-5,20-epoxy-7,19-cyclotax-11-en-2-yl benzo 
ate