MedChemExpress - Model Exatecan (mesylate) (GMP) - 169869-90-3
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].MCE products for research use only. We do not sell to patients.
Exatecan (mesylate)
MCE China：Exatecan (mesylate)
Brand：MedChemExpress (MCE)
Cat. No.HY-13631AG
CAS：169869-90-3
Synonyms：DX8951f
Storage：4°C, sealed storage, away from moisture and light
Shipping：Room temperature in continental US; may vary elsewhere.
Description：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.
In Vitro：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].
In Vivo：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].
IC50 & Target：Camptothecins
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References：
[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]
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