Exatecan mesylate|169869-90-3|(依喜替康甲磺酸盐; DX8951f)-陌孚医药/Medlife

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Exatecan mesylate (Synonyms: 依喜替康甲磺酸盐; DX8951f)

目录号: PL12382 纯度: ≥99%

CAS No. :169869-90-3

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PL12382-1g	1g	询价	询价
PL12382-5g	5g	询价	询价

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中文名称	Exatecan mesylate
中文别名	依沙替康甲磺酸盐;甲磺酸依喜替康;依喜替康甲磺酸盐
英文名称	Exatecan mesylate
英文别名	(1S,9S)-1-Amino-9-ethyl-5-fluoro-9-hydroxy-4-methyl-2,3,9,10,13,15-hexahydro-1H,12H-benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinoline-10,13-dione mesylate;Exatecan mesilate;DX-8951f;DX-8951(free base);(1S,9S)-1-Amino-9-ethyl-5-fluoro-9-hydroxy-4-methyl-2,3,9,10,13,15-hexahydro-1H,12H-benzo[de]pyrano[3',4':6,7]indolizino[1,2-;Exatecan mesylate;DX8951f;Exatecan Meslate;Exatecan (Mesylate);Exatecan mesylate anhydrous;Y76278R9RJ;BCP02365;API0010083;5-(2,5-Dimethyl-4-(prop-1-en-1-yl)phenoxy)-2,2-dimethylpentanoic acid;DX 8951f;DX8951f;DX 8951f;DX-8951f;http:////www.amadischem.com/proen/491263/
Cas No.	169869-90-3
分子式	C₂₅H₂₆FN₃O₇S
分子量	531.55
包装储存	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

产品详情

Exatecan mesylate (DX8951f) 是一种 DNA 拓扑异构酶 I (topoisomerase I) 抑制剂，IC₅₀ 值为 2.2 μM (0.975 μg/mL)，可用于癌症研究。

生物活性

Exatecan mesylate (DX8951f) is a DNA topoisomerase I inhibitor, with an IC 50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research.

性状

Solid

IC50 & Target[1][2]

Topoisomerase I 0.975 μg/mL (IC50)

体外研究(In Vitro)

Exatecan mesylate is a potent topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL. Exatecan mesylate (DX-8951f) significantly inhibits the proliferation of several cancer cell lines, with mean GI50s of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast cancer cells, colon cancer cells, stomach cancer cells and lung cancer cells, respectively. Exatecan mesylate (DX-8951f) displays cytotoxic activities against PC-6, PC-6/SN2-5 cells, with mean GI50s of 0.186 and 0.395 ng/mL, respctively. Exatecan mesylate (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Exatecan mesylate (DX-8951f, 3.325-50 mg/kg, i.v.) exhibits antitumor activities in the mice model bearing tumor cells, without toxic death. Exatecan mesylate (15, 25 mg/kg, i.v.) hightly inhibits MIA-PaCa, BxPC-3 primary tumor growth in the MIA-PaCa-2 early-stage model and early-stage model of BxPC-3. Exatecan mesylate (15, 25 mg/kg, i.v.) also significantly suppresses BxPC-3 lymphatic metastasis and completely eliminates lung metastasis in the BxPC-3 late-stage cancer model. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 11.76 mg/mL (22.12 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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