[CAS NO. 1554458-53-5]  BAY 1217389

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PRODUCTS SPECIFICATIONS [1554458-53-5]

Catalog
SLK-S8215
Brand
Selleck
CAS
1554458-53-5

DESCRIPTION [1554458-53-5]

Overview

MDL-
Molecular Weight561.50
Molecular FormulaC27H24F5N5O3
SMILES-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.7809 mL8.9047 mL17.8094 mL
5 mM0.3562 mL1.7809 mL3.5619 mL
10 mM0.1781 mL0.8905 mL1.7809 mL
50 mM0.0356 mL0.1781 mL0.3562 mL

Description

BAY 1217389 is an orally bioavailable, selective inhibitor of the serine/threonine kinase 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).

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.