Irinotecan Hcl Trihydrate

• 产品号: S2217
• CAS号: 136572-09-3
• 分子式: C33H45ClN4O9
• 分子量: 677.1848
• 保 存: -20°C

产品别名

• 标题: Irinotecan Hcl Trihydrate
• IUPAC标准名: (19S)-10,19-diethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.0^{2,11}.0^{4,9}.0^{15,20}]henicosa-1(21),2,4,6,8,10,15(20)-heptaen-7-yl 4-(piperidin-1-yl)piperidine-1-carboxylate trihydrate hydrochloride
• IUPAC传统名: (19S)-10,19-diethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.0^{2,11}.0^{4,9}.0^{15,20}]henicosa-1(21),2,4,6,8,10,15(20)-heptaen-7-yl 4-(piperidin-1-yl)piperidine-1-carboxylate trihydrate hydrochloride
• 别名: Irinotecan; CPT 11; Camptosar; Campto

产品登记号

• CAS号: 136572-09-3

产品性质

• 作用靶点: Topoisomerase
• 成盐信息: hydrate
• 保存条件: -20°C

产品详细信息

详细说明 (English)

Biological Activity:
Irinotecan hydrochloride trihydrate is a hydrochloride trihydrate of irinotecan (Camptosar, Campto, CPT-11) which is a topoisomerase I inhibitor with IC50 of 15.8 and 5.17 μM for LoVo cells and HT-29 cells, respectively. As a Topo I inhibitor, Irinotecan (Camptosar, Campto, CPT-11) inhibits the religation step of the enzyme’s normal action, inducing single stranded DNA breaks. These single stranded breaks are then converted to double-stranded breaks within the course of DNA replication which is reported to induce apoptosis or repair mechanisms as a result. Irinotecan is activated by esterases to produce the activated metabolite and has been reported to be associated with cleavage of poly (ADP-ribose) polymerase (PARP) in colon carcinoma cells. Irinotecan’s active metabolite is additionally noted to activate p53 in the Huh7 cell line. [1][2][3]

参考文献

• Hofmann C et al. Anticancer Res. 2005 Mar-Apr;25(2A):795-804.