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依喜替康甲磺酸盐 /Exatecan mesylate {[allProObj[0].p_purity_real_show]}

货号:A537376 同义名: 依沙替康甲磺酸盐 / DX8951f;Exatecan (mesylate)

Exatecan mesylate is a totally synthetic analogue of the topoisomerase I-inhibitor camptothecin, which was synthesised to impart increased aqueous solubility, greater tumour efficacy, and less toxicity than camptothecin itself.

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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+
Exatecan mesylate 化学结构 CAS号:169869-90-3
Exatecan mesylate 化学结构
CAS号:169869-90-3
Exatecan mesylate 3D分子结构
CAS号:169869-90-3
Exatecan mesylate 化学结构 CAS号:169869-90-3
Exatecan mesylate 3D分子结构 CAS号:169869-90-3
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Exatecan mesylate 纯度/质量文件 产品仅供科研

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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+%
Marbofloxacin 98+%
Voreloxin HCl 98%
Mitoxantrone dihydrochloride PKC 98%
Nalidixic acid 98%
Doxorubicin 98%
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 97%
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。

Exatecan mesylate 生物活性

描述 DNA topoisomerases are enzymes that catalyze the alteration of DNA topology with transiently induced DNA strand breakage, essential for DNA replication[3]. Exatecan mesylate is a totally synthetic analogue of the topoisomerase I-inhibitor camptothecin, which was synthesised to impart increased aqueous solubility, greater tumour efficacy, and less toxicity than camptothecin itself. 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[4]. 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[5]. 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, respectively. Exatecan mesylate (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells[6].

Exatecan mesylate 参考文献

[1]Reichardt P, Nielsen OS, et al. Exatecan in pretreated adult patients with advanced soft tissue sarcoma: results of a phase II--study of the EORTC Soft Tissue and Bone Sarcoma Group. Eur J Cancer. 2007 Apr;43(6):1017-22.

[2]Ajani JA, Takimoto C, et al. A phase II clinical and pharmacokinetic study of intravenous exatecan mesylate (DX-8951f) in patients with untreated metastatic gastric cancer. Invest New Drugs. 2005 Oct;23(5):479-84.

[3]Fei You,Changshou Gao. Topoisomerase Inhibitors and Targeted Delivery in Cancer Therapy. Curr Top Med Chem. 2019. 19(9), 713-729.

[4]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. 86(8), 776-82.

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

[6]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. 72(4), 680-6.

Exatecan mesylate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.41mL

1.88mL

0.94mL

18.81mL

3.76mL

1.88mL

Exatecan mesylate 技术信息

CAS号169869-90-3
分子式C25H26FN3O7S
分子量 531.553
别名 依沙替康甲磺酸盐 ;DX8951f;Exatecan (mesylate);DX-8951 Mesylate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 14 mg/mL(26.34 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

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