BAY1217389

CAS No. 1554458-53-5

BAY1217389( BAY1217389 | BAY-1217389 | BAY 1217389 )

Catalog No. M18080 CAS No. 1554458-53-5

BAY 1217389 is an effective and selective inhibitor of the monopolar spindle 1 (MPS1) kinase (IC50<10 nM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 42 In Stock
5MG 68 In Stock
10MG 104 In Stock
25MG 192 In Stock
50MG 286 In Stock
100MG Get Quote In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    BAY1217389
  • Note
    Research use only, not for human use.
  • Brief Description
    BAY 1217389 is an effective and selective inhibitor of the monopolar spindle 1 (MPS1) kinase (IC50<10 nM).
  • Description
    BAY1217389 is an orally bioavailable, selective inhibitor of the serine/threonine kinase monopolar spindle 1 (Mps1, TTK), with potential antineoplastic activity. Upon administration, the Mps1 inhibitor 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.
  • 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.
  • 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.
  • Synonyms
    BAY1217389 | BAY-1217389 | BAY 1217389
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Mps1
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1554458-53-5
  • Formula Weight
    561.5
  • Molecular Formula
    C27H24F5N5O3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : ≥ 28 mg/mL; 49.87 mM
  • SMILES
    Cc1c(ccc(c1)c1cnc2n1nc(cc2NCCC(F)(F)F)Oc1c(c(c(cc1)OC)F)F)C(=O)NC1CC1
  • Chemical Name
    N-cyclopropyl-4-(6-(2,3-difluoro-4-methoxyphenoxy)-8-((3,3,3-trifluoropropyl)amino)imidazo[1,2-b]pyridazin-3-yl)-2-methylbenzamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Wengner AM, et al. Mol Cancer Ther. 2016 Apr;15(4):583-92.
molnova catalog
related products
  • 3,8-Di-O-methylellag...

    3,3'-Di-O-methylellagic acid reveals moderate antibacterial activity, it also shows strong DPPH radical scavenging activities with SC50 of 123.3 ug/mL.

  • Sphistin Synthetic P...

    Sphistin Synthetic Peptide (12-38, Fitc in N-Terminal-Fluorescently Labeled Peptide) is a truncated fragments of Sphistin Synthetic Peptide that shows potent antimicrobial activity.

  • Oleuropein

    Oleuropein is an antioxidant polyphenol isolated from olive leaf.