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EMD534085

Cat. No. M8930
EMD534085 Structure
Size Price Availability Quantity
10mg USD 400 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM. EMD534085 induces rapid cell death in HL60 during mitotic arrest. Caspase-8, −9, −3, −7 are activated; Parp1 is cleaved; Mcl1 and XIAP are degraded in EMD534085-treated HL60 cells. EMD534085 treated HL60 cells also shows significantly accumulated phospho-Histone H3 level starting at 6 hrs post thymidine release.

In vivo: In a low dose PK of EMD 534085 in mice the clearance is 1.8 L/h/kg on average, the volume of distribution is 7.4 L/kg and the half life around 2.5 h. The bioavailability in high dose experiments (>10 mg/kg) is always above 50% in mice. Intraperitonal administration of EMD 534085 enables significant systemic exposure in mice leading to a significant tumor growth reduction without toxic side effects.

Protocol
Cell Experiment
Cell lines Epithelial cell lines HeLa and MCF7
Preparation method Epithelial cell lines HeLa and MCF7 are synchronized in G2-phase using RO-3306. Cells are treated with 10 µM RO-3306 for 16 hrs, and then are ished and released to either warm growth medium or medium supplemented with 500 nM EMD534085.
Concentrations 500 nM
Incubation time
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 476.53
Formula C25H31F3N4O2
CAS Number 858668-07-2
Purity >98%
Solubility DMSO: ≥ 20 mg/mL
Storage at -20°C
References

Prolonged mitotic arrest triggers partial activation of apoptosis, resulting in DNA damage and p53 induction.
Orth JD, et al. Mol Biol Cell. 2012 Feb;23(4):567-76. PMID: 22171325.

Rapid induction of apoptosis during Kinesin-5 inhibitor-induced mitotic arrest in HL60 cells.
Tang Y, et al. Cancer Lett. 2011 Nov 1;310(1):15-24. PMID: 21782324.

The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.
Schiemann K, et al. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1491-5. PMID: 20149654.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: EMD534085 supplier, Kinesin, inhibitors

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