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7-乙基-10羟基喜树碱 /SN-38 98%

货号:A366170 同义名: 伊立替康杂质B / 7-Ethyl-10-hydroxycamptothecin;NK 012 Ambeed 开学季,买赠积分,赢豪礼

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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SN-38 化学结构 CAS号:86639-52-3
SN-38 化学结构
CAS号:86639-52-3
SN-38 3D分子结构
CAS号:86639-52-3
SN-38 化学结构 CAS号:86639-52-3
SN-38 3D分子结构 CAS号:86639-52-3
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SN-38 纯度/质量文件 产品仅供科研

货号:A366170 标准纯度: 98%
批次查询: 批次纯度:

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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。

SN-38 生物活性

靶点
  • Topo I

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].

SN-38 细胞研究

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

SN-38 动物研究

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
Animal Mice[4]
Dose 5 mg/kg
Administration i.v.
p.o.
Cmax 647 ng/ml (i.v.)
30 ng/ml (p.o.)
AUC0→∞ 279 ng·h/ml (i.v.)
86 ng·h/ml (p.o.)
Tmax 1 h (p.o.)

SN-38 实验方案

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

SN-38 技术信息

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

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