Exatecan mesylate  (Synonyms: DX8951f)

Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor, with an IC₅₀ of 2.2 μM (0.975 μg/mL), and can be used in cancer research^[1][2][3].

Exatecan mesylate 对 PC-6/SN2-5 (SN-38 抗性细胞系) 仅有两倍抗性^[1]。
Exatecan mesylate (10 μM，30 min) 在 PC-6 和 PC-6/SN2-5 细胞内积累差异小^[1]。
Exatecan mesylate 抑制肿瘤生长，对乳腺癌，结肠癌，胃癌，肺癌细胞系的 GI₅₀ 均值为 2.02，2.92，1.53，0.877 ng/mL^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Exatecan mesylate (15-25 mg/kg; 每周一次; 三周) 在 BxPC-3-GFP 和 MIA-PaCa-2GFP 原位植入小鼠模型中抑制肿瘤生长，阻止肺转移^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

531.55

C₂₅H₂₆FN₃O₇S

169869-90-3

固体

Light yellow to yellow

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

• [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]