供货周期: | 一周 |
品牌: | 爱必信 |
规格: | ≥98% |
货号: | abs819593 |
CAS号: | 86639-52-3 |
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抑制剂描述: 产品名称:SN 38 产品别名:见爱必信官网 英文别名:SN 38 靶点: CAS:86639-52-3 纯度:≥98% 外观:见爱必信官网 保存方法:Store at -20° C 描述: SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. 溶解性:DMSO :21 mg/mL (53.51 mM) 体外研究: The IC50 values for LoVo, HCT116, and HT29 cell lines is 20 nM, 50 nM, 130 nM, respectively. In all three SN-38 (NK012) resistant cell lines Top1 activity is maintained in the presence of high concentrations of SN-38. 体内研究:SN-38 (NK012), the active and toxic metabolite of the anticancer prodrug Irinotecan. At 30 minutes after administration, Irinotecan plasma concentrations in Slco1a/1b(?/?) mice are 1.9-fold higher than in the wild-type mice (1.89 vs. 1.01 μM, respectively), whereas SN-38 (NK012) plasma concentrations of Slco1a/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).
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