MLN0905 是一种PLK1的有效抑制剂，IC50值为 2 nM。
产品描述
MLN0905 is an effective PLK1 inhibitor(IC50=2 nM).
体外活性
在携带HT-29异种移植物的裸鼠中,口服MLN0905（6.25 mg / Kg-50 mg / Kg）能够在治疗48小时后,表现剂量依赖的药效反应.在携带OCI LY-19-Luc肿瘤的小鼠中,口服MLN0905（3.12 mg / Kg-6.25 mg / Kg）在治疗后8小时表现药效反应.
体内活性
MLN0905是PLK1抑制剂（IC50=2 nM）。 LN0905抑制细胞有丝分裂（EC50=9 nM）。在HT-29细胞中（LD50=22 nM）,MLN0905能够抑制细胞增殖。在一组淋巴瘤细胞中（IC50=3 - 24 nM）,MLN0905能够抑制细胞活力。
激酶实验
PLK1 Flash Plate Assay: The human PLK1 enzymatic reaction totaling 30μL contained 50 mM Tris-HCl (pH 8.0), 10 mM MgCl2, 0.02% BSA, 10% glycerol, 1 mM DTT, 100 mM NaCl, 3.3% DMSO, 8 μM ATP, 0.2μCi [γ- 33 P]-ATP, 4 μM peptide substrate (Biotin-AHX-LDETGHLDSSGLQEVHLA-CONH2), and 10 nM recombinant human PLK1[2–369]T210D. The enzymatic reaction mixture, with or without PLK inhibitors, is incubated for 2.5 h at 30℃before termination with 20μL of 150 mM EDTA. Then 25μL of the stopped enzyme reaction mixture is transferred to a 384-well streptavidin coated Image FlashPlate and incubated at room temperature for 3 h. The Image Flash Plate wells are washed three times with 0.02% Tween-20 and then read on the Perkin-Elmer Viewlux.
Cas No.
1228960-69-7
分子式
C24H25F3N6S
分子量
486.56
别名
PLK1 Inhibitor
储存和溶解度
DMSO:90 mg/mL (185 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
