MPI-0479605

Catalog No.S7488

MPI-0479605 Chemical Structure

Molecular Weight(MW): 407.51

MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1 with IC50 of 1.8 nM, >40-fold selectivity over other kinases.

Size Price Stock Quantity  
USD 167 In stock
USD 300 In stock
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 1 publication

Purity & Quality Control

Choose Selective Kinesin Inhibitors

Biological Activity

Description MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1 with IC50 of 1.8 nM, >40-fold selectivity over other kinases.
Targets
Mps1 [1]
1.8 nM
In vitro

MPI-0479605 impairs the SAC and the bipolar attachment of chromosomes to the mitotic spindle, which results in chromosome segregation defects and aneuploidy. MPI-0479605 results in a significant decrease in cell viability with GI50 ranging from 30 to 100 nM in a panel of tumor cell lines. In addition, MPI-0479605 also causes cell growth arrest and ultimately promotes cell death by apoptosis or mitotic catastrophe. [1]

In vivo MPI-0479605 (30 mg/kg daily or 150 mg/kg every 4 days, i.p.) shows antitumor activity in colon cancer xenograft models. [1]

Protocol

Kinase Assay:

[1]
- Collapse

In Vitro Kinase Assays and Selectivity Screening :

To measure Mps1 activity, 25 ng of recombinant, full-length enzyme is incubated in reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.01% Triton X-100 and 5 μM Myelin basic protein (MBP)) containing vehicle (DMSO alone) or inhibitors. Forty μM ATP (2xKm) is added with 1 μCi [γ-33P]ATP and the reaction is incubated at room temperature for 45 minutes. Reactions are terminated with 3% phosphoric acid and transferred to P81 filter plates. Samples are washed in 1% phosphoric acid and 33P radioactivity is measured on a TopCount scintillation reader. In-house kinase assays are all carried out at 2xKm ATP concentrations. MPI-0479605 (500 nM) is also screened against a larger kinase panel.
Cell Research:

[1]
- Collapse
  • Cell lines: A549, Colo205, DU-4475, DU-145, HCC827, HCT116, HT29, MDA MB 231, MiaPaCa2, NCI-H69, NCI-H460, NCI-N87, OPM2, and OVCAR-3 cells.
  • Concentrations: ~10 μM
  • Incubation Time: 3 or 7 days
  • Method:

    Cells are treated for 3 or 7 days with various concentrations of MPI-0479605 and the GI50 is determined. Cell viability is measured with CellTiter-Glo.


    (Only for Reference)
Animal Research:

[1]
- Collapse
  • Animal Models: Mice bearing subcutaneous HCT-116 or Colo-205 human tumor cell xenografts.
  • Formulation: daily with 30 mg/kg or every 4 days with 150 mg/kg
  • Dosages: 5% dimethylacetamide (DMA)/12% ethanol/40% PEG-300
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 62 mg/mL warmed (152.14 mM)
Ethanol 2 mg/mL warmed (4.9 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 407.51
Formula

C22H29N7O
CAS No. 1246529-32-7
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field
selleck catalog

Kinesin Signaling Pathway Map

Related Kinesin Products

  • FRAX597 New

    FRAX597 is a potent, ATP-competitive inhibitor of group I PAKs with IC50 of 8 nM, 13 nM, and 19 nM for PAK1, PAK2, and PAK3, respectively.

  • VER155008 New

    VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.

  • PU-H71 New

    PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.

  • Ispinesib (SB-715992)

    Ispinesib (SB-715992) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with Ki app of 1.7 nM in a cell-free assay, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Phase 2.

    Features:An allosteric, potent, specific, and reversible inhibitor of the mitotic kinesin spindle protein (KSP) (HsEg5).

  • SB743921 HCl

    SB743921 is a kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E. Phase 1/2.

  • AZ 3146

    AZ3146 is a selective Mps1 inhibitor with IC50 of ~35 nM, contributes to recruitment of CENP-E (kinesin-related motor protein), less potent to FAK, JNK1, JNK2, and Kit.

  • GSK923295

    GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183. Phase 1.

    Features:The first potent and selective inhibitor of CENP-E.

  • ARQ 621

    ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1.

  • Paclitaxel

    Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.

  • Docetaxel

    Docetaxel, an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.

Tags: buy MPI-0479605 | MPI-0479605 supplier | purchase MPI-0479605 | MPI-0479605 cost | MPI-0479605 manufacturer | order MPI-0479605 | MPI-0479605 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID