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 |
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5MG | 68 | In Stock |
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10MG | 104 | In Stock |
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25MG | 192 | In Stock |
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50MG | 286 | In Stock |
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100MG | Get Quote | In Stock |
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200MG | Get Quote | In Stock |
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500MG | Get Quote | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameBAY1217389
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NoteResearch use only, not for human use.
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Brief DescriptionBAY 1217389 is an effective and selective inhibitor of the monopolar spindle 1 (MPS1) kinase (IC50<10 nM).
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DescriptionBAY1217389 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.
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In VitroBAY 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.
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In VivoBAY 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.
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SynonymsBAY1217389 | BAY-1217389 | BAY 1217389
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PathwayOthers
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TargetOther Targets
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RecptorMps1
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number1554458-53-5
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Formula Weight561.5
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Molecular FormulaC27H24F5N5O3
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 28 mg/mL; 49.87 mM
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SMILESCc1c(ccc(c1)c1cnc2n1nc(cc2NCCC(F)(F)F)Oc1c(c(c(cc1)OC)F)F)C(=O)NC1CC1
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Chemical NameN-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
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Wengner AM, et al. Mol Cancer Ther. 2016 Apr;15(4):583-92.
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