PNU-159682, an active nemorubicin metabolite, is a highly potent anthracycline toxin that retains antitumor activity in vivo. Similarly to other anthracyclines PNU-159682 intercalates between the CG base pairs of DNA, but the stability of the complexes is much higher.
The antitumor anthracycline nemorubicin is converted by human liver microsomes to a major metabolite, PNU-159682 (PNU), which was found to be much more potent than its parent drug toward cultured tumor cells and in vivo tumor models. The mechanism of
Clinical cancer research : an official journal of the American Association for Cancer Research, 11(4), 1608-1617 (2005-03-05)
Nemorubicin (3'-deamino-3'-[2''(S)-methoxy-4''-morpholinyl]doxorubicin; MMDX) is an investigational drug currently in phase II/III clinical testing in hepatocellular carcinoma. A bioactivation product of MMDX, 3'-deamino-3'',4'-anhydro-[2''(S)-methoxy-3''(R)-oxy-4''-morpholinyl]doxorubicin (PNU-159682), has been recently identified in an incubate of the drug with NADPH-supplemented rat liver microsomes. The aims
Molecular cancer therapeutics, 16(5), 879-892 (2017-03-05)
Antibody-drug conjugates (ADC) are highly potent and specific antitumor drugs, combining the specific targeting of mAbs with the potency of small-molecule toxic payloads. ADCs generated by conventional chemical conjugation yield heterogeneous mixtures with variable pharmacokinetics, stability, safety, and efficacy profiles.
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