Mps1-IN-2

Modify Date: 2024-01-10 18:39:39

Mps1-IN-2 Structure
Mps1-IN-2 structure
Common Name Mps1-IN-2
CAS Number 1228817-38-6 Molecular Weight 480.602
Density 1.3±0.1 g/cm3 Boiling Point 772.7±70.0 °C at 760 mmHg
Molecular Formula C26H36N6O3 Melting Point N/A
MSDS Chinese USA Flash Point 421.1±35.7 °C

 Use of Mps1-IN-2


Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.

 Names

Name Msp1-IN-2
Synonym More Synonyms

 Mps1-IN-2 Biological Activity

Description Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.
Related Catalog
Target

Mps1:12 nM (Kd)

GAK:140 nM (Kd)

PLK1:61 nM (Kd)

PLK3:1600 nM (Kd)

PLK4:3100 nM (Kd)

STK33:5000 nM (Kd)

In Vitro Mps1-IN-2 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 145 nM and 12 nM. Mps1-IN-2 also shows high affinity for PLK1 and GAK with Kds of 61 and 140 nM, respectively, but shows little or no inhibition on other 352 member kinases. Mps1-IN-2 can induces bypass of a checkpoint-mediated mitotic arrest in U2OS cells[1].
Kinase Assay The kinase binding assay is used to assess compound binding to TTK by monitoring displacement of a fluorescently labeled, ATP site-directed kinase inhibitor (Kinase Tracer 236) from the kinase active site. Each 15 μL assay contains 5 nM TTK, variable amounts of test compound (Mps1-IN-2), 30 nM Kinase Tracer 236, 2 nM Eu-anti-GST Antibody, and 1% DMSO (residual from compound dilution) in Kinase Buffer A (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% Brij-35). Binding assays are initiated by addition of 5 μL of test compound (from 2-fold dilution series) to 5 μL of a kinase/antibody mixture, followed by addition of 5 μL of antibody. Assay plates are read using using standard Eu-based TR-FRET settings with excitation at 340 nm and emission monitored at 615 nm (donor) and 665 nm (acceptor). Emission intensities are measured over a 200 µs window following a 100 µs post-excitation delay[1].
References

[1]. Kwiatkowski N, et al. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 772.7±70.0 °C at 760 mmHg
Molecular Formula C26H36N6O3
Molecular Weight 480.602
Flash Point 421.1±35.7 °C
Exact Mass 480.284882
PSA 94.06000
LogP 2.05
Vapour Pressure 0.0±2.8 mmHg at 25°C
Index of Refraction 1.633
Storage condition 2-8℃

 Safety Information

RIDADR NONH for all modes of transport

 Synonyms

6H-Pyrimido[4,5-b][1,4]diazepin-6-one, 9-cyclopentyl-2-[[2-ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,7,8,9-tetrahydro-5-methyl-
9-Cyclopentyl-2-{[2-ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino}-5-methyl-5,7,8,9-tetrahydro-6H-pyrimido[4,5-b][1,4]diazepin-6-one
Mps1-IN-2
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: Mps1-IN-2
  • Price: $850.0/100mg $1500.0/250mg $2600.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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Price: $119/10mM*1mLinDMSO

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