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BAY1217389

Catalog No. T3434 CAS 1554458-53-5

BAY 1217389 is an effective and selective inhibitor of the monopolar spindle 1 (MPS1) kinase (IC50<10 nM).

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BAY1217389, CAS 1554458-53-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
2 mg	In stock	$ 47.00
5 mg	In stock	$ 76.00
10 mg	In stock	$ 116.00
25 mg	In stock	$ 213.00
50 mg	In stock	$ 318.00
1 mL * 10 mM (in DMSO)	In stock	$ 94.00

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Purity: 98.78%

Purity: 98.09%

Purity: 95.71%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BAY 1217389 is an effective and selective inhibitor of the monopolar spindle 1 (MPS1) kinase (IC50<10 nM).
Targets&IC50	Mps1:<10 nM
In vitro	In biochemical assays, the IC50 value of BAY 1217389 is 0.63±0.27 nmol/L. It shows high selectivity against other kinases and found to bind to PDGFRβ (<10 nmol/L), Kit (between 10 and 100 nmol/L), CLK1, CLK2, CLK4, JNK1, JNK2, JNK3, LATS1, MAK, MAPKAP2, MERTK, p38β, PDGFRα, PIP5K1C, PRKD1, and RPS6KA5 (between 100 and 1,000 nmol/L). In cellular mechanistic assays, BAY1217389 abrogats nocodazole-induced SAC activity and induced premature exit from mitosis ('mitotic breakthrough'), resulting in multinuclearity and tumor cell death. It is found to inhibit cell proliferation with a median IC50 of 6.7 nmol/L (range 3 to >300 nmol/L)[1].
In vivo	In vivo, BAY 1217389 achieves moderate efficacy in monotherapy in tumor xenograft studies. Its blood clearance is found to be low in the tested species. Vss is high and terminal half-lives were long. BAY 1217389 is administered orally to female NMRI mouse (1 mg/kg) and male Wistar rat (0.5 mg/kg). Peak plasma concentrations are observed between 1.5 and 7 hours. Oral bioavailability is high in rat and moderate in mouse[1].
Kinase Assay	Inhibition of recombinant human Mps1 by BAY 1161909 or BAY 1217389 is assessed in TRFRET-based in vitro kinase assays via phosphorylation of a biotinylated peptide (Biotin-Ahx-PWDPDDADITEILG-NH2). Under standard assay conditions kinase and test compound are preincubated for 15 min before enzyme reaction is started by addition of substrate and ATP upon 10 μM[1].
Cell Research	Cells are seeded into 96-well plates at densities ranging from 1,000 to 5,000 cells per well in the appropriate medium supplemented with 10% FCS. After 24 hours, cells are treated in quadruplicates with serial dilutions of compounds. After further 96 hours, adherent cells are fixed with glutaraldehyde and stained with crystal violet. IC50 values are calculated by means of a 4-parameter fit using the company's own software.(Only for Reference)

Molecular Weight	561.5
Formula	C27H24F5N5O3
CAS No.	1554458-53-5

Storage

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

Solubility Information

DMSO: 93 mg/mL (165.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 3 mg/mL (5.34 mM)

References and Literature

1. Wengner AM, et al. Mol Cancer Ther. 2016, 15(4):583-92.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Inhibitor Library Fluorochemical Library Kinase Inhibitor Library Clinical Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

BAY1217389 1554458-53-5 Cytoskeletal Signaling Kinesin Inhibitor BAY 1217389 Mps1 BAY-1217389 Monopolar spindle 1 inhibit inhibitor

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