| In Vitro | GDC-0152 can block protein–protein interactions that involve IAP proteins and pro-apoptotic molecules. Using transiently transfected HEK293T cells, GDC-0152 is shown to disrupt XIAP binding to partially processed caspase-9 and to disrupt the association of ML-IAP, cIAP1, and cIAP2 with Smac. |
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| In Vivo | GDC-0152 has moderate predicted hepatic clearance based on metabolic stability assays conducted using human liver microsomes. Plasma–protein binding of GDC-0152 is moderate and comparable among mice (88–91%), rats (89–91%), dogs (81–90%), monkeys (76–85%), and humans (75–83%) over the range of concentrations investigated (0.1–100 μM); higher plasma–protein binding is observed in rabbits (95–96%). |
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| Animal model | Human-tumor xenograft mouse models of MDA-MB-231 breast cancer |
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| Formulation & Dosage | phosphate-buffered saline; 10, 50, 100 mg/kg; Oral |
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| References | [1] Flygare JA, et al. J Med Chem, 2012, 55(9), 4101-4113. |
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