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BAY1217389

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Purity:98.78%

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COA FNMR HNMR HPLC LCMS

BAY1217389

Catalog No. T3434Cas No. 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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Pack Size	Price	Availability
1 mg	$33	In Stock
2 mg	$47	In Stock
5 mg	$76	In Stock
10 mg	$116	In Stock
25 mg	$213	In Stock
50 mg	$318	In Stock
1 mL x 10 mM (in DMSO)	$94	In Stock

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Product Introduction

Bioactivity

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)

Chemical Properties

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

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 93 mg/mL (165.6 mM)

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

Ethanol: 3 mg/mL (5.34 mM)

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7809 mL	8.9047 mL	17.8094 mL	89.0472 mL
5 mM	0.3562 mL	1.7809 mL	3.5619 mL	17.8094 mL

DMSO

	1mg	5mg	10mg	50mg
10 mM	0.1781 mL	0.8905 mL	1.7809 mL	8.9047 mL
20 mM	0.0890 mL	0.4452 mL	0.8905 mL	4.4524 mL
50 mM	0.0356 mL	0.1781 mL	0.3562 mL	1.7809 mL
100 mM	0.0178 mL	0.0890 mL	0.1781 mL	0.8905 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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