货号:A366170
同义名:
伊立替康杂质B
/ 7-Ethyl-10-hydroxycamptothecin;NK 012
SN-38 is an active metabolite of CPT-11 that inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks.
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | Topo I ↓ ↑ | Topo II ↓ ↑ | Topo IV ↓ ↑ | Topoisomerase ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ellagic acid | ✔ | 99%+ | |||||||||||||||||
β-Lapachone | ✔ | 99%+ | |||||||||||||||||
(s)-10-hydroxycamptothecin | ✔ | 99%+ | |||||||||||||||||
Camptothecin |
++
Topo I, IC50: 0.68 μM |
98% | |||||||||||||||||
Betulinic acid |
++
Eukaryotic topoisomerase I, IC50: 5 μM |
99%+ | |||||||||||||||||
Topotecan |
++++
Topo I (DU-145 Luc cells), IC50: 2 nM Topo I (MCF-7 Luc cells), IC50: 13 nM |
99%+ | |||||||||||||||||
Irinotecan HCl Trihydrate | ✔ | 98% | |||||||||||||||||
SN-38 | ✔ | 98% | |||||||||||||||||
Levofloxacin hydrate | ✔ | 99%+ | |||||||||||||||||
Dexrazoxane | ✔ | 99%+ | |||||||||||||||||
Ofloxacin | ✔ | 98+% | |||||||||||||||||
Enoxacin | ✔ | 99%+ | |||||||||||||||||
Flumequine |
+
Topo II, IC50: 15 μM |
99%+ | |||||||||||||||||
Levofloxacin | ✔ | 99%+ | |||||||||||||||||
Etoposide | ✔ | 98% | |||||||||||||||||
Pefloxacin mesylate dihydrate | ✔ | 99+% | |||||||||||||||||
Marbofloxacin | ✔ | 99%+ | |||||||||||||||||
Voreloxin HCl | ✔ | 98% | |||||||||||||||||
Mitoxantrone dihydrochloride | ✔ | PKC | 99%+ | ||||||||||||||||
Nalidixic acid | ✔ | 99%+ | |||||||||||||||||
Doxorubicin | ✔ | 98% | |||||||||||||||||
Novobiocin sodium | ✔ | 98%+ | |||||||||||||||||
Amonafide | ✔ | 99%+ | |||||||||||||||||
Pirarubicin | ✔ | 98%+ | |||||||||||||||||
Idarubicin HCl |
+++
Topo II (MCF-7 cells), IC50: 3.3 ng/mL |
99%+ | |||||||||||||||||
Genistein | ✔ | EGFR | 98% | ||||||||||||||||
Teniposide | ✔ | 98% | |||||||||||||||||
Moxifloxacin | ✔ | 98% | |||||||||||||||||
Ciprofloxacin | ✔ | 99%+ | |||||||||||||||||
Clinafloxacin | ✔ | 97% | |||||||||||||||||
Gatifloxacin | ✔ | 99%+ | |||||||||||||||||
Daunorubicin HCl |
+++
DNA synthesis, Ki: 20 nM |
98% | |||||||||||||||||
Epirubicin HCl | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | SN-38, derived from the Topoisomerase I inhibitor Irinotecan, serves as its active metabolite. SN-38 impedes DNA and RNA synthesis, with IC50 values of 0.077 μM and 1.3 μM, respectively [1][2][3][4]. |
体内研究 | SN-38 is the active and toxic metabolite of the anticancer prodrug Irinotecan. At 30 minutes post-administration, Irinotecan plasma concentrations in Slco1a/1b(−/−) mice are 1.9-fold higher compared to wild-type mice (1.89 vs. 1.01 μM, respectively), while SN-38 plasma concentrations in Slco1a/1b(−/−) mice are 8-fold higher than in wild-type mice (0.4 μg/mL vs. 0.05 μg/mL, respectively). The overall plasma exposure [AUC(5-240)] of Irinotecan is 1.7-fold higher in Oatp1a/1b knockout mice compared to 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]. |
体外研究 | The IC50 values for LoVo, HCT116, and HT29 cell lines are 20 nM, 50 nM, and 130 nM, respectively. In all three SN-38 resistant cell lines, Top1 activity persists even in the presence of elevated concentrations of SN-38 [2]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
HEK293 cells | Cytotoxic assay | 72 h | Intrinsic cytotoxicity against HEK293 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 25272055 | |
human A2780 cells | Cytotoxic assay | 72 h | Cytotoxicity against human A2780 cells overexpressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay, IC50=9 nM | 22959246 | |
human A549 cells | Cytotoxic assay | 3 days | Cytotoxicity against human A549 cells assessed as growth inhibition after 3 days by SRB assay, IC50=2.72 nM | 24529870 | |
human A549 cells | Cytotoxic assay | Cytotoxicity against human A549 cells, IC50=47 nM | 21470864 | ||
Dose | Rat: 2 mg/kg[3] (i.v.); 40 mg/kg (p.o.) Mice: 5 mg/kg- 75 mg/kg[4] (i.v.) | ||||||||||||
Administration | i.v., p.o. | ||||||||||||
Pharmacokinetics |
|
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.55mL 0.51mL 0.25mL |
12.74mL 2.55mL 1.27mL |
25.48mL 5.10mL 2.55mL |
CAS号 | 86639-52-3 |
分子式 | C22H20N2O5 |
分子量 | 392.4 |
别名 | 伊立替康杂质B ;7-Ethyl-10-hydroxycamptothecin;NK 012;irinotecan metabolite.;10-hydroxy-7-ethylcamptothecin;7-ethyl-10-hydroxy-20(S)-Camptothecin |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 25 mg/mL(63.71 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
IP 2% DMSO+2% Tween80+40% PEG300+water 1 mg/mL clear PO 0.5% CMC-Na 50 mg/mL suspension |