PF-4942847

PF-4942847 is an orally active HSP90 inhibitor with an IC₅₀ of approximately 50 nM. PF-4942847 induces apoptosis in osteosarcoma cells, increases the proportion of cells in the sub-G1 phase and PARP cleavage, reduces the expression of Akt, Erk, MYC, c-MET and STAT-3, and regulates HSP expression. PF-4942847 can be used in studies related to osteosarcoma and HSP90^[1][2]. In Vitro:PF-4942847 inhibits cell growth in a dose-dependent manner in osteosarcoma cell lines U2OS, SaOS2, MNNG/HOS, KHOS, MG63, G292, CAL72, SJSA1 and 143B, with an IC₅₀ of approximately 50 nM^[1].
PF-4942847 induces apoptosis in osteosarcoma cell lines including U2OS, SaOS2, MNNG/HOS, KHOS, MG63, G292, CAL72, SJSA1 and 143B, as evidenced by increased proportions of cells in the sub-G1 phase and enhanced PARP cleavage^[1].
PF-04942847 decreases the expression of Akt, Erk, MYC, c-MET and STAT-3, and modulates the expression of HSP in osteosarcoma cells^[1].
PF-4942847 inhibits osteoclast differentiation of purified human CD14⁺ monocytes, and its effect differs from that of the control HSP90 inhibitor 17-AAG^[1]. In Vivo:PF-4942847 (25 mg/kg; p.o.; three times per week) significantly inhibits tumor growth by approximately 40% and prolongs survival in athymic mice bearing MNNG/HOS osteosarcoma xenografts^[1].