瀏覽量: 144
- 產(chǎn)品名稱: Exatecan mesylate 依喜替康甲磺酸鹽
- 產(chǎn)品貨號(hào): CS13631A
- 貨期: 現(xiàn)貨
- 價(jià)格與訂購: 1500
- 數(shù)量:
- 規(guī)格: 1g
- 產(chǎn)品信息
- 如何訂購
生物活性
Exatecan mesylate (DX8951f) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research.
體外研究
Exatecan mesylate 是一種有效的拓?fù)洚悩?gòu)酶 I 抑制劑,IC50 為 0.975 μg/mL。Exatecan mesylate (DX-8951f) 顯著抑制多種癌細(xì)胞系的增殖,平均 GI50 分別為 2.02 ng/mL、2.92 ng/mL、1.53 ng/mL 和 0.877 ng/mL分別針對(duì)乳腺癌細(xì)胞、結(jié)腸癌細(xì)胞、胃癌細(xì)胞和肺癌細(xì)胞[1]。Exatecan mesylate (DX-8951f) 對(duì) PC-6、PC-6/SN2-5 細(xì)胞具有細(xì)胞毒活性,平均 GI50 分別為 0.186 和 0.395 ng/mL。Exatecan mesylate (34 nM) 穩(wěn)定 PC-6 和 PC-6/SN2-5 細(xì)胞中的 DNA-TopoI 復(fù)合物[3]。
體內(nèi)研究
Exatecan mesylate (DX-8951f,3.325-50 mg/kg,iv) 在攜帶腫瘤細(xì)胞的小鼠模型中表現(xiàn)出抗腫瘤活性,沒有毒性死亡[1]。Exatecan mesylate (15,25 mg/kg,iv) 在 MIA-PaCa-2 早期模型和 BxPC-3 早期模型中高度抑制 MIA-PaCa、BxPC-3 原發(fā)性腫瘤的生長(zhǎng)。Exatecan mesylate (15 mg/kg,25 mg/kg,iv) 在 BxPC-3 晚期癌癥模型中也顯著抑制 BxPC-3 淋巴轉(zhuǎn)移并完全消除肺轉(zhuǎn)移[2]。
分子量
531.55
性狀
Solid
Formula
C25H26FN3O7S
CAS 號(hào)
169869-90-3
運(yùn)輸條件
Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 1 years; -20°C, 6 months (sealed storage, away from moisture and light)
純度
99.91%
參考文獻(xiàn)
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Note
For research use only .
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