Exatecan (DX-8951) 是一种具有 2.2 μM (0.975 μg/mL) IC50 的 DNA 拓扑异构酶 I 抑制剂,用于癌症研究。
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
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Inaccessible (Haz class 6.1), International | USD 150+ |
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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。 |
描述 | Exatecan is a highly potent inhibitor of topoisomerase I, possessing an IC50 value of 0.975 μg/mL. Exatecan Mesylate (DX-8951f) effectively suppresses the proliferation of various cancer cell lines, with mean GI50 values of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast, colon, stomach, and lung cancer cells, respectively [1]. Exatecan Mesylate (DX-8951f) exhibits cytotoxic effects against PC-6 and PC-6/SN2-5 cells, with mean GI50 values of 0.186 and 0.395 ng/mL, respectively. At a concentration of 34 nM, Exatecan Mesylate stabilizes DNA-TopoI complexes in both PC-6 and SN2-5 cells [3]. |
体内研究 | Exatecan Mesylate (DX-8951f, 3.325-50 mg/kg, i.v.) demonstrates antitumor effects in mouse models bearing tumor cells, without causing toxic fatalities [1]. Exatecan Mesylate (15, 25 mg/kg, i.v.) effectively suppresses primary tumor growth in MIA-PaCa and BxPC-3 models at early stages. Additionally, at the same doses, it significantly inhibits lymphatic metastasis in BxPC-3 and completely eradicates lung metastasis in the late-stage BxPC-3 cancer model [2]. |
体外研究 | Exatecan is a highly potent inhibitor of topoisomerase I, possessing an IC50 value of 0.975 μg/mL. Exatecan Mesylate (DX-8951f) effectively suppresses the proliferation of various cancer cell lines, with mean GI50 values of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast, colon, stomach, and lung cancer cells, respectively [1]. Exatecan Mesylate (DX-8951f) exhibits cytotoxic effects against PC-6 and PC-6/SN2-5 cells, with mean GI50 values of 0.186 and 0.395 ng/mL, respectively. At a concentration of 34 nM, Exatecan Mesylate stabilizes DNA-TopoI complexes in both PC-6 and SN2-5 cells [3]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.30mL 0.46mL 0.23mL |
11.48mL 2.30mL 1.15mL |
22.96mL 4.59mL 2.30mL |
CAS号 | 171335-80-1 |
分子式 | C24H22FN3O4 |
分子量 | 435.448 |
别名 | DX-8951 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 18 mg/mL(41.34 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 |