MLN0905是一种有效的PLK1抑制剂，IC50为2 nM。MLN0905是有效的PLK1抑制剂，IC50为2 nM。MLN0905抑制细胞有丝分裂，EC50为9 nM。MLN0905抑制Cdc25C-T96磷酸化,直接抑制PLK1，EC50为29 nM。

>98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

PLK1 Inhibitor

白色粉末

DMSO ：90 mg/mL (185 mM)

PLK1

MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM. MLN0905 inhibits cell mitosis with EC50 of 9 nM. MLN0905 inhibits Cdc25C-T96 phosphorylation, a direct readout of PLK1 inhibition with EC50 of 29 nM. MLN0905 inhibits HT-29 viability with LD50 of 22 nM. MLN0905 possesses reasonable selectivity against a panel of 359 kinases. MLN0905 inhibits a panel of lymphoma cells viability with IC50 of 3 – 24 nM.

Nude mice bearing HT-29 xenografts administered with MLN0905 (6.25 mg/Kg – 50 mg/Kg, p.o.) shows dose-dependent pharmacodynamic responses (48 hours after treatment). OCI LY-19-Luc tumor bearing mice administered with MLN0905 (3.12 mg/Kg – 6.25 mg/Kg, p.o.) shows significant pharmacodynamic responses amd peaks at 8 hours after treatment. MLN0905 shows antitumor efficacy in treatment with OCI LY-19-Luc xenografts bearing scid mice for 21 days. The T/C of 6.25 mg/Kg daily group is 0.15.