Topoisomerase I inhibitor 8 

Topoisomerase I inhibitor 8 is a potent topoisomerase I inhibitor. Topoisomerase I inhibitor 8 is a hexacyclic analogue of camptothecin, and displays cytotoxic effect against tumor cells^[1].

Topoisomerase I inhibitor 8 (compound 57) shows antitumor activities against three cell line cultures with IC₅₀s of 0.22 ng/mL (P388), 2.06 ng/mL (HOC-21), 0.17 ng/mL (QG-56), respectively^[1].
Topoisomerase I inhibitor 8 results the change in DNA from the supercoiled form to the relaxed form in the presence of topoisomerase I, shows stronger effective than SN-38 (HY-13704), with IC₅₀ of compound/IC₅₀ of SN-38=0.51^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

420.43

C₂₄H₂₁FN₂O₄

210346-40-0

Solid

Light brown to brown

CC1=C(F)C=C2C3=C1CCCC3=C4C(C(N5C4)=CC([C@](CC)(O)C(OC6)=O)=C6C5=O)=N2

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Sugimori M, et al. Synthesis and antitumor activity of ring A- and F-modified hexacyclic camptothecin analogues. J Med Chem. 1998 Jun 18;41(13):2308-18.  [Content Brief]