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BAY 1217389

Cat. No. M8918
BAY 1217389 Structure
Size Price Availability Quantity
10mg USD 200 In stock
25mg USD 360 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

BAY 1217389 selectively binds to and inhibits the activity of Mps1. This inactivates the spindle assembly checkpoint (SAC), accelerates mitosis, causes chromosomal misalignment and missegregation, and mitotic checkpoint complex destabilization. This induces cell death in Mps1-overexpressing cancer cells. BAY 1217389 efficiently inhibits tumor cell proliferation in vitro.

In vivo: BAY 1217389 achieves moderate efficacy in monotherapy in tumor xenograft studies. However, in line with its unique mode of action, when combines with paclitaxel, low doses of Mps1 inhibitor reduces paclitaxel-induced mitotic arrest in line with weakening of SAC activity. As a result, combination therapy strongly improves efficacy over paclitaxel or Mps1 inhibitor monotreatment at the respective MTDs in a broad range of xenograft models including those showing acquired or intrinsic paclitaxel-resistance. BAY 1217389 shows good tolerability without adding toxicity to paclitaxel monotherapy.

Protocol
Cell Experiment
Cell lines Tumor cell lines HeLa-MaTu and HeLa-MaTu-ADR cells
Preparation method Cells were 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 were treated in quadruplicates with serial dilutions of compounds. After further 96 hours, adherent cells were fixed with glutaraldehyde and stained with crystal violet. IC50 values were calculated by means of a 4-parameter fit using the company's own software.
Concentrations
Incubation time 96 h
Animal Experiment
Animal models Male Wistar rats and female CD1 or NMRI nu/nu mice
Formulation 50% PEG 400, 10% ethanol, and 40% water
Dosages 1, 2, 4, or 8 mg/kg (p.o.)
Administration i.v. or p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 561.5
Formula C27H24F5N5O3
CAS Number 1554458-53-5
Purity >98%
Solubility DMSO: ≥ 60 mg/mL
Storage at -20°C
References

Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity.
Wengner AM, et al. Mol Cancer Ther. 2016 Apr;15(4):583-92. PMID: 26832791.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BAY 1217389 supplier, Kinesin, inhibitors

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