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MLN0905

Name: MLN0905
Brand: Selleck Chemicals
SKU: S2898
Rating: 5 (2 reviews)

Catalog No.S2898

For research use only.

MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM.

CAS No. 1228960-69-7

Selleck's MLN0905 has been cited by 2 Publications

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PLK Signaling Pathway Map

Biological Activity

Description

MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM.

Targets

PLK1 ^[1]

2 nM

In vitro

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. ^[1] MLN0905 inhibits a panel of lymphoma cells viability with IC50 of 3 – 24 nM. ^[2]

In vivo

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. ^[1] 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. ^[2]

Protocol (from reference)

Kinase Assay:^[1]

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, 4μM 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.

References

Solubility (25°C)

In vitro	DMSO	97 mg/mL (199.35 mM)
	Water	Insoluble
	Ethanol	Insoluble

Chemical Information

Molecular Weight	486.56
Formula	C₂₄H₂₅F₃N₆S
CAS No.	1228960-69-7
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1=C(C=C(C=N1)CCCN(C)C)NC2=NC=C3CC(=S)NC4=C(C3=N2)C=CC(=C4)C(F)(F)F

Download MLN0905 SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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