[CAS NO. 1554458-53-5] BAY1217389
PRODUCTS SPECIFICATIONS [1554458-53-5]
DESCRIPTION [1554458-53-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 561.50 |
| Molecular Formula | C27H24F5N5O3 |
| 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 |
2 Publications Citing Use of MCE
Summary
BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 ( MPS1 ) kinase with an IC 50 value less than 10 nM.
IC50 & Target
|
Mps1 0.63 nM (IC 50 ) |
In Vitro
BAY 1217389 inhibits Mps1 kinase activity with IC 50 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02366949 | Bayer |
Medical Oncology
|
February 27, 2015 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 178.09 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent 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 |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.45 mM); Clear solution