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

MPI-0479605 

Cat. No.: HY-12660 Purity: 99.13%
Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 226 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 226 In-stock
Estimated Time of Arrival: December 31
Solid
2 mg USD 156 In-stock
Estimated Time of Arrival: December 31
5 mg USD 252 In-stock
Estimated Time of Arrival: December 31
10 mg USD 456 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1596 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

2 Publications Citing Use of MCE MPI-0479605

  • 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)

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].

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].

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

Molecular Weight

407.51

Formula

C22H29N7O

CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 11 mg/mL (26.99 mM; Need ultrasonic and warming)

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
10 mM 0.2454 mL 1.2270 mL 2.4539 mL
*Please refer to the solubility information to select the appropriate solvent.
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
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Product Name:
MPI-0479605
Cat. No.:
HY-12660
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