1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. Mps1 Apoptosis
  3. MPI-0479605

MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM.

For research use only. We do not sell to patients.

MPI-0479605 Chemical Structure

MPI-0479605 Chemical Structure

CAS No. : 1246529-32-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 176 In-stock
Solution
10 mM * 1 mL in DMSO USD 176 In-stock
Solid
2 mg USD 95 In-stock
5 mg USD 160 In-stock
10 mg USD 260 In-stock
50 mg USD 650 In-stock
100 mg USD 890 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM.

IC50 & Target[1]

Mps1

1.8 nM (IC50)

ALK

0.26 μM (IC50)

B-RAF

3.2 μM (IC50)

ERK2

3.9 μM (IC50)

FAK1

2.7 μM (IC50)

FER

0.59 μM (IC50)

FLT3

0.08 μM (IC50)

INSR

0.38 μM (IC50)

JNK1

0.11 μM (IC50)

PLK4

3.3 μM (IC50)

STK33

1.1 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
> 10 μM
Compound: 2, MPI-0479605
Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay
Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay
[PMID: 23634759]
HCT-116 EC50
0.3 μM
Compound: 1, MPI-0479605
Cell cycle arrest in human HCT116 cells assessed as G2 checkpoint inhibition by Hoescht 33342 staining method
Cell cycle arrest in human HCT116 cells assessed as G2 checkpoint inhibition by Hoescht 33342 staining method
[PMID: 22632936]
In Vitro

MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM. MPI-0479605 (0.1-10 μM) reduces cell viability of HCT-116 cells in a dose-dependent manner. MPI-0479605 shows severe defects in the ability to align chromosomes at the metaphase plate, but causes complete cytokinesis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

MPI-0479605 (30 mg/kg daily or 150 mg/kg every fourth day (Q4D), i.p.) inhibits tumor growth by 49% and 74 % in HCT-116 xenografts. However, MPI-0479605 does not show inhibitory activity via daily dosing on the Colo-205 xenografts, and dosing every four days causes 63% tumor growth inhibition (TGI)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

407.51

Formula

C22H29N7O

CAS No.
Appearance

Solid

Color

White to gray

SMILES

CC(C=C(N1CCOCC1)C=C2)=C2NC3=NC4=C(N=CN4)C(NC5CCCCC5)=N3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 11 mg/mL (26.99 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4539 mL 12.2696 mL 24.5393 mL
5 mM 0.4908 mL 2.4539 mL 4.9079 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Animal Administration
[1]

HCT-116 or Colo-205 cells are transplanted subcutaneously into the flanks of nude (nu+/nu+) mice and compound (MPI-0479605) treatment is initiated when tumor masses reaches an average size of 100 mm3. MPI-0479605 is formulated in 5% dimethylacetamide (DMA)/12% ethanol/40% PEG-300, ispinesib is formulated in 2% cremaphor/2% DMA, and 5-fluorouracil is formulated in 2% sodium bicarbonate. Tumor volume is measured using vernier calipers and tumor growth inhibition (TGI) is calculated as: %TGI= 100-100(change in median tumor volume of treated)/(change in median tumor volume control)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4539 mL 12.2696 mL 24.5393 mL 61.3482 mL
5 mM 0.4908 mL 2.4539 mL 4.9079 mL 12.2696 mL
10 mM 0.2454 mL 1.2270 mL 2.4539 mL 6.1348 mL
15 mM 0.1636 mL 0.8180 mL 1.6360 mL 4.0899 mL
20 mM 0.1227 mL 0.6135 mL 1.2270 mL 3.0674 mL
25 mM 0.0982 mL 0.4908 mL 0.9816 mL 2.4539 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
MPI-0479605
Cat. No.:
HY-12660
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