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MLN0905

Catalog No. T2704 CAS 1228960-69-7

Synonyms: PLK1 Inhibitor

MLN0905 (PLK1 Inhibitor) is an effective PLK1 inhibitor(IC50=2 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

MLN0905, CAS 1228960-69-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 68.00
2 mg	In stock	$ 95.00
5 mg	In stock	$ 147.00
10 mg	In stock	$ 249.00
25 mg	In stock	$ 468.00
50 mg	In stock	$ 669.00
1 mL * 10 mM (in DMSO)	In stock	$ 153.00

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Purity: 97.17%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MLN0905 (PLK1 Inhibitor) is an effective PLK1 inhibitor(IC50=2 nM).
Targets&IC50	PLK1:2 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.

Synonyms	PLK1 Inhibitor
Molecular Weight	486.56
Formula	C24H25F3N6S
CAS No.	1228960-69-7

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)

References and Literature

1. Duffey MO, et al. J Med Chem, 2012, 55(1), 197-208. 2. Shi JQ, et al. Mol Cancer Ther, 2012, 11(9), 2045-2053.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Anti-Cancer Compound Library Bioactive Compounds Library Max Anti-Aging Compound Library Bioactive Compound Library Fluorochemical Library NO PAINS Compound Library

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

MLN0905 1228960-69-7 Cell Cycle/Checkpoint PLK inhibit MLN-0905 PLK1 Inhibitor MLN 0905 Inhibitor Polo-like Kinase (PLK) inhibitor

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