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依喜替康 /Exatecan 99%+

货号:A619128 同义名: DX-8951 Ambeed 开学季,买赠积分,赢豪礼

Exatecan (DX-8951) 是一种具有 2.2 μM (0.975 μg/mL) IC50DNA 拓扑异构酶 I 抑制剂,用于癌症研究。

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+
Exatecan 化学结构 CAS号:171335-80-1
Exatecan 化学结构
CAS号:171335-80-1
Exatecan 3D分子结构
CAS号:171335-80-1
Exatecan 化学结构 CAS号:171335-80-1
Exatecan 3D分子结构 CAS号:171335-80-1
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Exatecan 纯度/质量文件 产品仅供科研

货号:A619128 标准纯度: 99%+
批次查询: 批次纯度:

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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。

Exatecan 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].
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].

Exatecan 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.

Exatecan 实验方案

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

Exatecan 技术信息

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

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