Exatecan Mesylate (DX‑8951f, NSC 714296) is a potent topoisomerase I inhibitor with an IC₅₀ of 2.2 μM (0.975 μg/mL). It is 6 times more potent than SN‑38 and shows average GI₅₀ values of 0.877–2.92 ng/mL across breast, colon, gastric, and lung cancer cell lines. Exatecan Mesylate is a water‑soluble hexacyclic camptothecin analog, derived from the natural product camptothecin. In research and clinical development, it is used as a potent ADC payload (e.g., in HER2‑targeting ADCs) and as a tool for studying topoisomerase I‑mediated DNA damage.
Exatecan Mesylate
$499.00
CAS Number: 169869-90-3
Synonyms: DX-8951f, NSC 714296
Mechanism of Action: Topoisomerase I Inhibitor
| Purity | Size | Price | Stock | Quantity |
|---|---|---|---|---|
| 98% | 1g | $499.00 | In stock |
Description
Additional information
| Size |
1g |
|---|---|
| Purity |
98% |
| M.F. |
C₂₅H₂₆FN₃O₇S |
| M.W. |
531.55 |
| Appearance |
Pale yellow to yellow solid |
| Storage |
Store long-term at -20°C |
| Smiles |
CS(=O)(O)=O.O=C1C@@(O)C2=C(CO1)C(N3CC4=C5C6=C(CC[C@@H]5N)C(C)=C(F)C=C6N=C4C3=C2)=O- |
Biological activity
| Biological target: | DNA Damage Response; Topoisomerase I; Topoisomerase I |
| In vitro activity: | IC₅₀ = 2.2 μM; 6× more potent than SN‑38; average GI₅₀ in breast, colon, gastric, lung cancers: 0.877–2.92 ng/mL. |
| In vivo activity: | Potent antitumor activity in xenografts; used as ADC payload. |
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