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Exatecan

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Chemical Structure| 171335-80-1 同义名 : DX-8951
CAS号 : 171335-80-1
货号 : A619128
分子式 : C24H22FN3O4
纯度 : 98%
分子量 : 435.448
MDL号 : MFCD00926120
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：
生物活性
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].
实验方案
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
参考文献

[1]Mitsui I, et al. A new water-soluble camptothecin derivative, DX-8951f, exhibits potent antitumor activity against human tumors in vitro and in vivo. Jpn J Cancer Res. 1995 Aug;86(8):776-82.

[2]Sun FX, et al. Efficacy of camptothecin analog DX-8951f (Exatecan Mesylate) on human pancreatic cancer in an orthotopic metastatic model. Cancer Res. 2003 Jan 1;63(1):80-5.

[3]Joto N, et al. DX-8951f, a water-soluble camptothecin analog, exhibits potent antitumor activity against a human lung cancer cell line and its SN-38-resistant variant. Int J Cancer. 1997 Aug 7;72(4):680-6.