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. Author manuscript; available in PMC: 2020 Mar 2.
Published in final edited form as: J Med Chem. 2019 Oct 11;62(20):9236–9245. doi: 10.1021/acs.jmedchem.9b01147

Figure 2.

Figure 2.

Conjugate stability of 1a in physiological conditions. Tumor tissue or cultured U87 cells were homogenized with RIPA buffer on ice before centrifuging to collect supernatant. Conjugates were incubated at 50 μM at 37 °C for up to 72 h. The % compound remaining was calculated based on area under curve from the analytical HPLC trace through a C4 column (Figure S4). (a) Conjugate stability of 1a in U87 tumor homogenate and U87 cell lysate. (b) In serum in vitro at 37 °C, conjugate 1a was metabolized to a new compound in ~3 h. (c) The half-life of 1a in mouse serum at 37 °C was determined to be ~1 h. Compound 5 was identified as 1a metabolite by mass spectrometry.