Exatecan Mesylate

Research use only, not for human use.

Exatecan Mesylate is a DNA topoisomerase I inhibitor (IC50: 2.2 μM, 0.975 μg/mL).Exatecan Mesylate (DX-8951f) 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.

Exatecan Mesylate is a DNA topoisomerase I inhibitor (IC50: 2.2 μM, 0.975 μg/mL).Exatecan Mesylate (DX-8951f) 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. Exatecan displays cytotoxic activities against PC-6, PC-6/SN2-5 cells, with mean GI50s of 0.186 and 0.395 ng/mL, respectively. Exatecan Mesylate (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells.Exatecan Mesylate (3.325-50 mg/kg, i.v.) exhibits antitumor activities in the mice model bearing tumor cells, without toxic death. Exatecan Mesylate (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 Mesylate (15, 25 mg/kg, i.v.) also significantly suppresses BxPC-3 lymphatic metastasis and completely eliminates lung metastasis in the BxPC-3 late-stage cancer model.

DX8951f

Cell Cycle/DNA Damage

Topoisomerase

Topo I

Cancer

Biliary cancer; Breast cancer; Cervical cancer; Ewing's sarcoma; Gastric cancer; Haematological malignancies; Liver cancer; Myelodysplastic syndromes; Non-small cell lung cancer; Ovarian cancer; Pancreatic cancer; Peritoneal cancer; Prostate cancer; Rhabdomyosarcoma; Solid tumours

169869-90-3

531.55

C25H26FN3O7S

>98% (HPLC)

DMSO:8 mg/mL (15.05 mM; Need ultrasonic);Water:6 mg/mL (11.29 mM; Need ultrasonic and warming)

CS(O)(=O)=O.CC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4cc(F)c(C)c5CC[C@H](N)c(c3Cn1c2=O)c45

——

(-20℃)

With Ice Pack

≥ 2 years