供货周期: | 一周 |
品牌: | 爱必信 |
规格: | >98% |
货号: | abs813731 |
CAS号: | 1228960-69-7 |
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抑制剂描述: 产品名称:MLN0905 产品别名:见爱必信官网 英文别名:MLN0905 靶点:PLK CAS:1228960-69-7 纯度:>98% 外观:见爱必信官网 保存方法:store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. 描述: 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。 溶解性:DMSO :90 mg/mL (185 mM) 体外研究: 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. 体内研究: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.
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