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Size | Price | Stock |
---|---|---|
250mg | $1250 | Check With Us |
500mg | $1850 | Check With Us |
1g | $2775 | Check With Us |
Cat #: V4195 CAS #: 1554458-53-5 Purity ≥ 98%
Description: BAY 1217389 (BAY-1217389) is a novel, potent, orally bioavailable and selective inhibitor of the serine/threonine kinase monopolar spindle 1 (MPS1) (IC50 < 10 nM) with potential cancer activity by selectively binding to and inhibiting the activity of Mps1.
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Molecular Weight (MW) | 561.50 |
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Molecular Formula | C27H24F5N5O3 |
CAS No. | 1554458-53-5 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent |
Protocol | 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 |
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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 |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.7809 mL | 8.9047 mL | 17.8094 mL | 35.6189 mL |
5mM | 0.3562 mL | 1.7809 mL | 3.5619 mL | 7.1238 mL |
10mM | 0.1781 mL | 0.8905 mL | 1.7809 mL | 3.5619 mL |
20mM | 0.0890 mL | 0.4452 mL | 0.8905 mL | 1.7809 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.