货号:A366170
同义名:
伊立替康杂质B
/ 7-Ethyl-10-hydroxycamptothecin; NK 012
SN-38是 CPT-11 的活性代谢物,通过抑制 DNA 拓扑异构酶 I 和 DNA 合成引发 DNA 单链断裂,IC50 分别为 0.077 μM(DNA 合成)和 1.3 μM(RNA 合成)。
HazMat Fee + There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| 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+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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| 产品名称 | Topo I ↓ ↑ | Topo II ↓ ↑ | Topo IV ↓ ↑ | Topoisomerase ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Ellagic acid | ✔ | 98% | |||||||||||||||||
| β-Lapachone | ✔ | 99%+ | |||||||||||||||||
| (s)-10-hydroxycamptothecin | ✔ | 98+% | |||||||||||||||||
| Camptothecin |
++
Topo I, IC50: 0.68 μM |
98% | |||||||||||||||||
| Betulinic acid |
++
Eukaryotic topoisomerase I, IC50: 5 μM |
98% | |||||||||||||||||
| Topotecan |
++++
Topo I (MCF-7 Luc cells), IC50: 13 nM Topo I (DU-145 Luc cells), IC50: 2 nM |
98% | |||||||||||||||||
| Irinotecan HCl Trihydrate | ✔ | 98% | |||||||||||||||||
| SN-38 | ✔ | 98% | |||||||||||||||||
| Levofloxacin hydrate | ✔ | 98% | |||||||||||||||||
| Dexrazoxane | ✔ | 99%+ | |||||||||||||||||
| Ofloxacin | ✔ | 98+% | |||||||||||||||||
| Enoxacin | ✔ | 99%+ | |||||||||||||||||
| Flumequine |
+
Topo II, IC50: 15 μM |
98% | |||||||||||||||||
| Levofloxacin | ✔ | 97% | |||||||||||||||||
| Etoposide | ✔ | 98% | |||||||||||||||||
| Pefloxacin mesylate dihydrate | ✔ | 99.5% | |||||||||||||||||
| Marbofloxacin | ✔ | 98+% | |||||||||||||||||
| Voreloxin HCl | ✔ | 98% | |||||||||||||||||
| Mitoxantrone 2HCl | ✔ | PKC | 98% | ||||||||||||||||
| Nalidixic acid | ✔ | 98% | |||||||||||||||||
| Doxorubicin | ✔ | 97% | |||||||||||||||||
| Novobiocin sodium | ✔ | 95% | |||||||||||||||||
| 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 | ✔ | 98% | |||||||||||||||||
| Clinafloxacin | ✔ | 99% | |||||||||||||||||
| Gatifloxacin | ✔ | 98% | |||||||||||||||||
| 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]. |
| Concentration | Treated Time | Description | References | |
| CHLA-32 cells | 1 μM | 24 hours | UNC2025 suppressed SN-38-induced Akt and ERK signaling activation | Nat Commun. 2024 Jun 21;15(1):5292. |
| EWS894 cells | 1 μM | 24 hours | UNC2025 suppressed SN-38-induced Akt and ERK signaling activation | Nat Commun. 2024 Jun 21;15(1):5292. |
| SK-N-MC cells | 1 μM | 24 hours | UNC2025 suppressed SN-38-induced Akt and ERK signaling activation | Nat Commun. 2024 Jun 21;15(1):5292. |
| CHLA-10 cells | 1 μM | 24 hours | UNC2025 suppressed SN-38-induced Akt and ERK signaling activation | Nat Commun. 2024 Jun 21;15(1):5292. |
| TC-32 cells | 1 μM | 24 hours | UNC2025 suppressed SN-38-induced Akt and ERK signaling activation | Nat Commun. 2024 Jun 21;15(1):5292. |
| TC-71 cells | 1 μM | 24 hours | UNC2025 suppressed SN-38-induced Akt and ERK signaling activation | Nat Commun. 2024 Jun 21;15(1):5292. |
| MHH-ES-1 cells | 1 μM | 24 hours | UNC2025 suppressed SN-38-induced Akt and ERK signaling activation | Nat Commun. 2024 Jun 21;15(1):5292. |
| A673 cells | 1 μM | 24 hours | UNC2025 suppressed SN-38-induced Akt and ERK signaling activation | Nat Commun. 2024 Jun 21;15(1):5292. |
| TC-32 | 1 μM | 24 hours | SN-38 treatment increased Akt-pT308 and ERK-p42/p44 signals | Nat Commun. 2024 Jun 21;15(1):5292 |
| TC-71 | 1 μM | 24 hours | SN-38 treatment increased Akt-pT308 and ERK-p42/p44 signals | Nat Commun. 2024 Jun 21;15(1):5292 |
| MHH-ES-1 | 1 μM | 24 hours | SN-38 treatment increased Akt-pT308 and ERK-p42/p44 signals | Nat Commun. 2024 Jun 21;15(1):5292 |
| A673 | 1 μM | 24 hours | SN-38 treatment increased Akt-pT308 and ERK-p42/p44 signals | Nat Commun. 2024 Jun 21;15(1):5292 |
| SNU-5 | 100 nM and 10 μM | 72 h | SN-38 inhibited SNU-5 cell proliferation by 51.1% and 84.8% | Mol Cancer Ther. 2022 Jul 5;21(7):1149-1159. |
| MKN-45 | 100 nM and 10 μM | 72 h | SN-38 inhibited MKN-45 cell proliferation by 43.3% and 83.4% | Mol Cancer Ther. 2022 Jul 5;21(7):1149-1159. |
| KATO-III | 100 nM and 10 μM | 72 h | SN-38 inhibited KATO-III cell proliferation by 31.7% and 65.6% | Mol Cancer Ther. 2022 Jul 5;21(7):1149-1159. |
| 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 |
| SMILES Code | O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C(CC)C5=CC(O)=CC=C5N=C4C3=C2)=O |
| MDL No. | MFCD00871873 |
| 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 |
| InChI Key | FJHBVJOVLFPMQE-QFIPXVFZSA-N |
| Pubchem ID | 104842 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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