BAY 1217389

Catalog No.S8215

For research use only.

BAY 1217389 is an orally bioavailable, selective inhibitor of the serine/threonine kinase monopolar spindle 1 (Mps1) with IC50 values below 10 nmol/L while showing an excellent selectivity profile.

BAY 1217389 Chemical Structure

CAS No. 1554458-53-5

Selleck's BAY 1217389 has been cited by 4 Publications

Purity & Quality Control

Choose Selective MPS1 Inhibitors

Biological Activity

Description BAY 1217389 is an orally bioavailable, selective inhibitor of the serine/threonine kinase monopolar spindle 1 (Mps1) with IC50 values below 10 nmol/L while showing an excellent selectivity profile.
Targets
Mps1 [1]
(Cell-free assay)
0.63 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].

Protocol (from reference)

Cell Research:[1]
  • Cell lines: Tumor cell lines HeLa-MaTu and HeLa-MaTu-ADR cells
  • Concentrations: --
  • Incubation Time: 96 h
  • Method: 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.
Animal Research:[1]
  • Animal Models: Male Wistar rats and female CD1 or NMRI nu/nu mice
  • Dosages: 1, 2, 4, or 8 mg/kg (p.o)
  • Administration: i.v or p.o

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 561.50
Formula

C27H24F5N5O3

CAS No. 1554458-53-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=CC(=C1)C2=CN=C3N2N=C(C=C3NCCC(F)(F)F)OC4=C(C(=C(C=C4)OC)F)F)C(=O)NC5CC5

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02366949 Completed Drug: BAY1217389|Drug: Paclitaxel Medical Oncology Bayer February 27 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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