Exatecan (GMP) refers to the GMP grade reagents of Exatecan. Exatecan (DX-8951f) is a DNA topoisomerase I (TOP1) inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL).Exatecan has antitumor activity and may be used in cancer research.

Exatecan (DX-8951f) displays cytotoxic activities against PC-6, and PC-6/SN2-5 cells, with mean GI50s of 0.186 and 0.395 ng/mL, respectively.[2]
Exatecan (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells.[2]
Exatecan is a potent topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL.[2]
Exatecan 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.[2]

Exatecan (DX-8951f) (3.325-50 mg/kg; i.v.) exhibits antitumor activities in the mice model bearing tumor cells, without toxic death.[3]
Exatecan (15, 25 mg/kg; i.v.) highly inhibits MIA-PaCa, BxPC-3 primary tumor growth in the MIA-PaCa-2 early-stage model and early-stage model of BxPC-3. Exatecan also significantly suppresses BxPC-3 lymphatic metastasis and completely eliminates lung metastasis in the BxPC-3 late-stage cancer model.[3]