| Name | Exatecan |
| Description | 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. |
| In vitro | 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] |
| In vivo | 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] |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 20 mg/mL (45.93 mM), Sonication is recommended.
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| Keywords | Topoisomerase I | topoisomerase I | Exatecan | DX8951 | DX 8951 | ADCCytotoxin | ADC Cytotoxin |
| Inhibitors Related | Berberine chloride | Methotrexate | EIDD-1931 | Levofloxacin hydrochloride | Norfloxacin | Methotrexate disodium | Prulifloxacin | Ciprofloxacin | Ciprofloxacin monohydrochloride | Dexamethasone | Etoposide | Cholesteryl Hemisuccinate |
| Related Compound Libraries | Bioactive Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Human Metabolite Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
