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. 2023 Dec 4;14(12):1876–1881. doi: 10.1021/acsmedchemlett.3c00488

Table 5. Key In Vitro Parameters of 30.

parameter 30
HCT116(MTAP–/−) cell proliferation inhibition IC50 (μM) 0.273
PPB, human/dog/rat/mouse (% Fu) 21.6/32.5/32.9/9.1
CLint, (mL/min/kg)a 1.4
CYP inhibition IC50, 3A4/2C9/2C19/2D6 (μM) all > 10
a

Intrinsic clearance rate was determined in human liver microsome.