"目录号: HY-13704
Cell Cycle/DNA DamageAutophagy-
SN-38 是拓扑异构酶 I (Topoisomerase I) 抑制剂Irinotecan的活性代谢物。
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生物活性
Description
SN-38 is an active metabolite of theTopoisomerase Iinhibitor Irinotecan.
IC50& Target
Topoisomerase I[1]
In Vitro
The IC50values for LoVo, HCT116, and HT29 cell lines is 20 nM, 50 nM, 130 nM, respectively. In all three SN-38 resistant cell lines Top1 activity is maintained in the presence of high concentrations of SN-38[2].
In Vivo
SN-38, the active and toxic metabolite of the anticancer prodrug Irinotecan. At 30 minutes after administration, Irinotecan plasma concentrations inSlco1a/1b(?/?)mice are 1.9-fold higher than in the wild-type mice (1.89 vs. 1.01 μM, respectively), whereas SN-38 plasma concentrations ofSlco1a/1b(?/?)mice are 8-fold higher compare with wild-type mice (0.4 μg/mL vs. 0.05 μg/mL, respectively). Overall plasma exposure [AUC(5-240)] of Irinotecan is 1.7-fold higher in Oatp1a/1b knockout mice versus wild-type mice (209.8±6.7 vs. 120.9±4.4 μM/min; P<0.01), and 2.9-fold higher for SN-38 (50±2.9 vs. 12±2 μM/min; P<0.001)[3].
Clinical Trial
Nippon Kayaku Co.,Ltd.
Small Cell Lung Cancer
July 2009
Phase 2
Nippon Kayaku Co.,Ltd.
Triple Negative Breast Cancer
February 2009
Phase 2
Nippon Kayaku Co.,Ltd.
Cancer
March 2007
Phase 1
Nippon Kayaku Co.,Ltd.
Advanced Solid Tumors-Metastatic Triple Negative Breast Cancer
July 2010
Phase 1
Nippon Kayaku Co.,Ltd.
Advanced Solid Tumors-Metastatic Colorectal Cancer
August 2010
Phase 1
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References
