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NMS-P715 

Cat. No. M27927
NMS-P715  Structure
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Biological Activity

NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM.

Chemical Information
Molecular Weight 676.73
Formula C35H39F3N8O3
CAS Number 1202055-32-0
Form Solid
Solubility (25°C) DMSO 2 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Orawan Waenphimai, et al. Eur J Pharmacol. Multiple actions of NMS-P715, the monopolar spindle 1 (MPS1) mitotic checkpoint inhibitor in liver fluke-associated cholangiocarcinoma cells

[2] Yuan Chen, et al. Molecules. Insights into Resistance Mechanisms of Inhibitors to Mps1 C604Y Mutation via a Comprehensive Molecular Modeling Study

[3] Yoshitaka Hiruma, et al. J Biol Chem. Understanding inhibitor resistance in Mps1 kinase through novel biophysical assays and structures

[4] Roger B Slee, et al. Mol Cancer Ther. Selective inhibition of pancreatic ductal adenocarcinoma cell growth by the mitotic MPS1 kinase inhibitor NMS-P715

[5] Riccardo Colombo, et al. Cancer Res. Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase

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Mps1-IN-6 is a potent Mps1 inhibitor with an IC50 value of 2.596 nM.

RMS-07 

RMS-07 is a covalent Monopolar Spindle Kinase 1 (MPS1/TTK) inhibitor, with an apparent IC50 of 13.1 nM. RMS-07 targets a poorly conserved cysteine in the kinase's hinge region.

CCT251455 

CCT251455 is a potent and selective mitotic kinase monopolar spindle 1 (MPS1) inhibitor with an IC50 of 3 nM.

  Catalog
Abmole Inhibitor Catalog




Keywords: NMS-P715  supplier, Mps1/TTK, inhibitors, activators


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