Onatasertib (CC-223) is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC50 value for mTOR kinase of 16 nM. Onatasertib inhibits both mTORC1 and mTORC2[1]. In vitro, Onatasertib has capability to inhibit markers of mTORC1 (S6RP and 4EBP1) and mTORC2 [AKT(S473)] across a range of IC50 values: 27 to 184 nM for pS6RP, 120 to 1,050 nM for p4EBP1, and 11 to 150 nM for pAKT(S473)][1].
体内研究
In vivo, Onatasertib demonstrates significant dose- and schedule-dependent inhibition of PC-3 tumor growth. Administered once daily at doses of 10 or 25 mg/kg, it achieves tumor volume reductions of 46% (P<0.001) and 87% (P<0.001), respectively. Twice-daily dosing at 5 or 10 mg/kg results in 65% (P<0.001) and 80% (P<0.001) reductions in tumor volume, respectively. The dosing regimens are well tolerated, with the exception of the 25 mg/kg/day group, which exhibits a significant body weight loss of about 10% after three weeks[1].
体外研究
Onatasertib (CC-223) is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC50 value for mTOR kinase of 16 nM. Onatasertib inhibits both mTORC1 and mTORC2[1].
In vitro, Onatasertib has capability to inhibit markers of mTORC1 (S6RP and 4EBP1) and mTORC2 [AKT(S473)] across a range of IC50 values: 27 to 184 nM for pS6RP, 120 to 1,050 nM for p4EBP1, and 11 to 150 nM for pAKT(S473)][1].
Onatasertib 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
human PC3 cells
Function assay
1 h
Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr, IC50=0.01 μM
26083478
human PC3 cells
Function assay
1 h
Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr
26083478
human PC3 cells
Function assay
1 h
Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr
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