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BAY1217389

CAS No. : 1554458-53-5

MCE 站：BAY1217389

产品活性：BAY 1217389是具有高效性和选择性的(MPS1)激酶抑制剂，IC₅₀值小于10 nM。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton

作用靶点：Mps1

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.

相关产品：Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Cytoskeleton Compound Library  |  MPI-0479605  |  AZ3146  |  Mps1-IN-1  |  Mps1-IN-3  |  TC-Mps1-12  |  Mps1-IN-1 dihydrochloride

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