BAY1217389

Additional information:
BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM.|Product information|CAS Number: 1554458-53-5|Molecular Weight: 561.50|Formula: C27H24F5N5O3|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|Smiles: CC1=CC(=CC=C1C(=O)NC1CC1)C1=CN=C2C(=CC(=NN12)OC1=CC=C(OC)C(F)=C1F)NCCC(F)(F)F|InChiKey: WNEILUNVMHVMPH-UHFFFAOYSA-N|InChi: InChI=1S/C27H24F5N5O3/c1-14-11-15(3-6-17(14)26(38)35-16-4-5-16)19-13-34-25-18(33-10-9-27(30,31)32)12-22(36-37(19)25)40-21-8-7-20(39-2)23(28)24(21)29/h3,6-8,11-13,16,33H,4-5,9-10H2,1-2H3,(H,35,38)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : ≥ 100 mg/mL (178.09 mM).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.Narasin Purity & Documentation |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|BAY 1217389 inhibits Mps1 kinase activity with IC50 value below 10 nM while showing an excellent selectivity profile.1-(4-Methoxyphenyl)piperazine Biological Activity 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.PMID:32541433 |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.|References:|Wengner AM, Siemeister G, Koppitz M, Schulze V, Kosemund D, Klar U, Stoeckigt D, Neuhaus R, Lienau P, Bader B, Prechtl S, Raschke M, Frisk AL, von Ahsen O, Michels M, Kreft B, von Nussbaum F, Brands M, Mumberg D, Ziegelbauer K. Novel Mps1 kinase inhibitors with potent anti-tumor activity. Mol Cancer Ther. 2016 Feb 1.Products are for research use only. Not for human use.|