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MLN0905

MLN0905
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Purity:97.17%
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MLN0905

Catalog No. T2704Cas No. 1228960-69-7
MLN0905 (PLK1 Inhibitor) is an effective PLK1 inhibitor(IC50=2 nM).
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Pack SizePrice/USDAvailabilityQuantity
1 mg$68In Stock
2 mg$95In Stock
5 mg$147In Stock
10 mg$249In Stock
25 mg$468In Stock
50 mg$669In Stock
1 mL x 10 mM (in DMSO)$153In Stock
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Product Introduction

Bioactivity
Description
MLN0905 (PLK1 Inhibitor) is an effective PLK1 inhibitor(IC50=2 nM).
In vitro
In nude mice bearing HT-29 xenografts, oral administration of MLN0905 (6.25 mg / Kg-50 mg / Kg) demonstrated a dose-dependent pharmacological response 48 hours post-treatment. Similarly, in mice harboring OCI LY-19-Luc tumors, oral MLN0905 (3.12 mg / Kg-6.25 mg / Kg) showed a pharmacological response 8 hours after treatment.
In vivo
MLN0905 acts as a potent inhibitor of PLK1, exhibiting an IC50 value of 2 nM. It effectively hampers cell mitosis with an EC50 of 9 nM and inhibits cell proliferation in HT-29 cells, as evidenced by an LD50 of 22 nM. Furthermore, in a range of lymphoma cell lines, MLN0905 demonstrates the ability to diminish cell viability, with IC50 values ranging from 3 to 24 nM.
Kinase Assay
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.
AliasPLK1 Inhibitor
Chemical Properties
Molecular Weight486.56
FormulaC24H25F3N6S
Cas No.1228960-69-7
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 90 mg/mL (185 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0552 mL10.2762 mL20.5524 mL102.7622 mL
5 mM0.4110 mL2.0552 mL4.1105 mL20.5524 mL
10 mM0.2055 mL1.0276 mL2.0552 mL10.2762 mL
20 mM0.1028 mL0.5138 mL1.0276 mL5.1381 mL
50 mM0.0411 mL0.2055 mL0.4110 mL2.0552 mL
100 mM0.0206 mL0.1028 mL0.2055 mL1.0276 mL

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Preparation method for in vivo formula: Take 50 μLDMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μLTween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify.
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