BAY1217389

SKU: orb1695455

Description

BAY1217389

Research Area

Signal Transduction

Key Properties

• CAS Number: 1554458-53-5
• MW: 561.5
• Purity: 99.54%
• Formula: C₂₇H₂₄F₅N₅O₃
• SMILES: COc1ccc(Oc2cc(NCCC(F)(F)F)c3ncc(-c4ccc(C(=O)NC5CC5)c(C)c4)n3n2)c(F)c1F
• Target: Kinesin
• Solubility: DMSO:93 mg/mL (165.63 mM);Ethanol:3 mg/mL (5.34 mM);10% DMSO+90% Corn Oil:3.3 mg/mL (5.88 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  Mps1 < 0 nM
• 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 f Male nMRI mouse (1 mg/kg) and Male Wistar rat (0.5 mg/kg). Peak plasma concentration are observed between 1.5 and 7 hours. Oral bioavailability is high in rat and moderate in mous.
• In Vitro:
  In biochemical assays the IC50 value of BAY 1217389 is 0.6 ± .27 nMol/L. It shows high selectivity against Other kinases and found to bind to PDGFRβ < 0 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.
• 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 usin the company's own software.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, Mps1, Monopolar spindle 1, BAY1217389, BAY-1217389, BAY 1217389

Compound Identifiers

PubChem CID

78320750