Bioactivity | Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research[1]. |
Invitro | Topoisomerase I/II inhibitor 4 (compound F16) (0-100 μM) could intercalate into DNA to inhibit enzymatic activity and inhibit Topo I and II activities in a dose-dependent manner[1].Topoisomerase I/II inhibitor 4 (compound F16) shows a high-expression level of Topo I and II enzymes in A375 and HCT116 cells and exhibits potent anti-proliferative activity with IC50 values of 20 and 50 nM, respectively, 10-fold lower than L02[1].Topoisomerase I/II inhibitor 4 (compound F16) (0-40 nM, A375 cell) inhibits cancer cell colony formation, invasion, migration and induces cell apoptosis[1]. Cell Cycle Analysis[1] Cell Line: |
In Vivo | Topoisomerase I/II inhibitor 4 (compound F16) (10-50 mg/kg; i.v.; per 2 days, for 7 days) suppresses tumor growth in the A375 Xenograft Model[1].Topoisomerase I/II inhibitor 4 (compound F16) of the plasma clearance rate (CL) was 7-fold lower than that of VP-16(0.007 L/min/kg). Topoisomerase I/II inhibitor 4 has a delayed elimination half-life of 151 min[1]. Animal Model: |
Name | Topoisomerase I/II inhibitor 4 |
Formula | C27H21N5O6 |
Molar Mass | 511.49 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Yang X, et al. Optimization of the Natural Product Calothrixin A to Discover Novel Dual Topoisomerase I and II Inhibitors with Improved Anticancer Activity. J Med Chem. 2022 Jun 9;65(11):8040-8061. |