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 is only two-fold resistant to PC-6/SN2-5 (SN-38 resistant cell line)^[1].
Exatecan mesylate (10 μM, 30 min) has little difference in the accumulation of PC-6 and PC-6/SN2-5 cells^[1].
Exatecan mesylate inhibits tumor growth, with the average GI₅₀ values of 2.02, 2.92, 1.53 and 0.877 ng/mL for breast cancer, colon cancer, gastric cancer, and lung cancer cell lines^[2].

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

Exatecan mesylate (15-25 mg/kg; once a week; three weeks) inhibits tumor growth and prevents lung metastasis in BxPC-3-GFP and MIA-PaCa-2GFP orthotopic implantation mouse models^[3].

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

531.55

C₂₅H₂₆FN₃O₇S

169869-90-3

Solid

Light yellow to yellow

O=S(C)(O)=O.O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C5C6=C(CC[C@@H]5N)C(C)=C(F)C=C6N=C4C3=C2)=O

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]