1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Mps1

BAY1217389 

Cat. No.: HY-12859 Purity: >98.0%
Handling Instructions

BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM.

For research use only. We do not sell to patients.
BAY1217389 Chemical Structure

BAY1217389 Chemical Structure

CAS No. : 1554458-53-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 163 In-stock
2 mg USD 72 In-stock
5 mg USD 132 In-stock
10 mg USD 228 In-stock
25 mg USD 408 In-stock
50 mg USD 732 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM.

IC50 & Target

IC50: <10 nM (MPS1)[1]

In Vitro

BAY 1217389 inhibits Mps1 kinase activity with IC50 value below 10 nM while showing an excellent selectivity profile. In cellular mechanistic assays BAY 1217389 abrogates nocodazole-induced SAC activity and induces premature exit from mitosis resulting in multinuclearity and tumor cell death. BAY 1217389 efficiently inhibits tumor cell proliferation in vitro[1].

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[1].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.7809 mL 8.9047 mL 17.8094 mL
5 mM 0.3562 mL 1.7809 mL 3.5619 mL
10 mM 0.1781 mL 0.8905 mL 1.7809 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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 BAY 1161909 or BAY 1217389. 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[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: For tumor xenograft studies female athymic NMRI nu/nu mice, 50 days old, average body weight 20-22 g, are used. When tumors reaches a size of approximately 20-40 mm2, depending on growth of the tumor model, animals are randomized to treatment and control groups (8-10 mice / group) and treated p.o. with vehicle (70% polyethylene glycol 400, 5% Ethanol, 25% Solutol), BAY 1161909, BAY 1217389, and/or paclitaxel. For analysis of polyploidy and multinuclearity induction in vivo, A2780cis tumor bearing female NMRI nude mice are treated with paclitaxel (i.v. once with 24 mg/kg), BAY 1161909 p.o.twice daily for 2 days with 2.5 mg/kg and in combination with paclitaxel (i.v. once 24 mg/kg) and BAY 1161909 (p.o. twice daily for 2 days 1 mg/kg)[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

561.5

Formula

C₂₇H₂₄F₅N₅O₃

CAS No.

1554458-53-5

SMILES

O=C(NC1CC1)C2=CC=C(C3=CN=C4C(NCCC(F)(F)F)=CC(OC5=CC=C(OC)C(F)=C5F)=NN43)C=C2C

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 28 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
BAY1217389
Cat. No.:
HY-12859
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