化合物MLN0905 T2704

Product Introduction
Bioactivity


英文名: MLN0905

描述: MLN0905 (PLK1 Inhibitor) 是一种 PLK1的有效抑制剂，IC50值为 2 nM。

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.

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。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 90 mg/mL (185 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: inhibit | MLN-0905 | MLN 0905 | Inhibitor | Polo-like Kinase (PLK) | MLN0905

相关产品: Poloxime | T521 | Rigosertib | Rigosertib sodium | TAK-960 | PHA-680632 | LFM-A13 | Ro3280 | 7-O-Prenylscopoletin | Poloxin-2

相关库: Anti-Aging Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途