Tesirine

• 常用名: Tesirine
• 英文名: Tesirine
• CAS号: 1595275-62-9
• 分子量: 1496.651
• 密度: 1.3±0.1 g/cm3
• 沸点: 1428.0±65.0 °C at 760 mmHg
• 分子式: C₇₅H₁₀₁N₉O₂₃
• 熔点: N/A
• 闪点: 817.4±34.3 °C

Tesirine用途

Tesirine(SG3249)是组织蛋白酶B可切割的缬氨酸丙氨酸吡咯并苯并二氮杂卓(PBD)二聚体,作为抗体-药物偶联物(ADC)有效载荷；Tesirine(SG3249)设计用于将有效的抗肿瘤活性与所需的物理化学性质相结合,例如有利的疏水性和改善的缀合特性；Rovalpituzumab Tesirine是针对δ样蛋白3(DLL3)的一流抗体-药物缀合物,DLL3是在肿瘤起始细胞中鉴定并在小细胞肺癌中表达的新靶标。

Tesirine名称

• 英文名: N-[31-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-29-oxo-4,7,10,13,16,19,22,25-octaoxa-28-azahentriacontan-1-oyl]-L-valyl-N-{4-[({[(11S,11aS)-11-hydroxy-7-methoxy-8-[(5-{[(11aS)-7-methoxy-2-methyl-5-oxo-5,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yl]oxy}pentyl)oxy]-2-methyl-5-oxo-11,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-10(5H)-yl]carbonyl}oxy)methyl]phenyl}-L-alaninamide

Tesirine生物活性

• 描述: Tesirine(SG3249)是组织蛋白酶B可切割的缬氨酸丙氨酸吡咯并苯并二氮杂卓(PBD)二聚体,作为抗体-药物偶联物(ADC)有效载荷；Tesirine(SG3249)设计用于将有效的抗肿瘤活性与所需的物理化学性质相结合,例如有利的疏水性和改善的缀合特性；Rovalpituzumab Tesirine是针对δ样蛋白3(DLL3)的一流抗体-药物缀合物,DLL3是在肿瘤起始细胞中鉴定并在小细胞肺癌中表达的新靶标。
• 参考文献: References 1. Tiberghien AC, et al. ACS Med Chem Lett. 2016 May 24;7(11):983-987. 2. Cancer Discov. 2015 Dec;5(12):OF4. doi: 10.1158/2159-8290.CD-NB2015-144. 3. Rudin CM, et al. Lancet Oncol. 2017 Jan;18(1):42-51. View Related Products by Target Drug-Linker Conjugates

Tesirine物理化学性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 1428.0±65.0 °C at 760 mmHg
• 分子式: C₇₅H₁₀₁N₉O₂₃
• 分子量: 1496.651
• 闪点: 817.4±34.3 °C
• 精确质量: 1495.701050
• LogP: -0.60
• InChIKey: HKGATZAPXCCEJR-OWRSNIELSA-N
• SMILES: COc1cc2c(cc1OCCCCCOc1cc3c(cc1OC)C(=O)N1C=C(C)CC1C(O)N3C(=O)OCc1ccc(NC(=O)C(C)NC(=O)C(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCN3C(=O)C=CC3=O)C(C)C)cc1)N=CC1CC(C)=CN1C2=O
• 蒸汽压: 0.0±0.3 mmHg at 25°C
• 折射率: 1.601

Tesirine英文别名

• N-[31-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-29-oxo-4,7,10,13,16,19,22,25-octaoxa-28-azahentriacontan-1-oyl]-L-valyl-N-{4-[({[(11S,11aS)-11-hydroxy-7-methoxy-8-[(5-{[(11aS)-7-methoxy-2-methyl-5-oxo-5,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yl]oxy}pentyl)oxy]-2-methyl-5-oxo-11,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-10(5H)-yl]carbonyl}oxy)methyl]phenyl}-L-alaninamide
• L-Alaninamide, N-[31-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1,29-dioxo-4,7,10,13,16,19,22,25-octaoxa-28-azahentriacont-1-yl]-L-valyl-N-[4-[[[[(11S,11aS)-8-[[5-[[(11aS)-5,11a-dihydro-7-methoxy-2-methyl-5-oxo-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yl]oxy]pentyl]oxy]-11,11a-dihydro-11-hydroxy-7-methoxy-2-methyl-5-oxo-1H-pyrrolo[2,1-c][1,4]benzodiazepin-10(5H)-yl]carbonyl]oxy]methyl]phenyl]-