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产品展厅

Exatecan
物品单位 品牌
Chemstan
  • 产地:China
  • 型号:
  • 货号:CS00141
  • cas:171335-80-1
  • 发布日期: 2022-07-26
  • 更新日期: 2022-07-28
产品详细说明
产地 China
货号 CS00141
品牌 Chemstan
用途 Research Grade
型号
CAS编号 171335-80-1
别名 DX-8951, 依喜替康
规格
级别 其他
外观性状
产品英文名称 Exatecan
重金属 ppm
纯度 98%
分子式 C24H22FN3O4

产品描述

Exatecan can be used in cancer research.Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL).

靶点活性

Topoisomerase I

体外活性

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.Exatecan 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. 

体内活性

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.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. 

别名 

DX-8951 , 依喜替康 

分子量

435.45

分子式

C24H22FN3O4

CAS No.

171335-80-1 

存储

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

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.

Note

For research use only .

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