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EMD534085 Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5764561

EMD534085 is an effective and selective mitotic kinesin-5 inhibitor (IC50: 8nM). More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
EMD534085, Inhibitor
Full Product Name
EMD534085
Product Gene Name
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
476.53
Solubility
DMSO: 25mg/mL (52.46mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C25H31F3N4O2
SMILES
CN(C)CCNC(NC[C@@H](CC[C@H]12)O[C@@H]1c(cc(C(F)(F)F)cc1)c1N[C@H]2c1ccccc1)=O
CAS Number
858668-07-2
Cell Research
Epithelial cell lines HeLa and MCF7 are synchronized in G2-phase using RO-3306. Cells are treated with 10uM RO-3306 for 16 hrs, and then are ished and released to either warm growth medium or medium supplemented with 500nM EMD534085 [2].
In Vitro
In a low dose PK of EMD 534085 in mice, the clearance is 1.8L/h/kg on average, the volume of distribution is 7.4L/kg and the half-life around 2.5 hours. The bioavailability in high dose experiments (>10mg/kg) is always above 50% in mice. Intraperitoneal administration of EMD 534085 enables significant systemic exposure in mice leading to a significant tumor growth reduction without toxic side effects [1].

Product References and Citations for EMD534085, inhibitor

Schiemann K, et al. The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1491-5.
Schiemann K, et al. The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1491-5.
Tang Y, et al. Rapid induction of apoptosis during Kinesin-5 inhibitor-induced mitotic arrest in HL60 cells. Cancer Lett. 2011 Nov 1;310(1):15-24.
Tang Y, et al. Rapid induction of apoptosis during Kinesin-5 inhibitor-induced mitotic arrest in HL60 cells. Cancer Lett. 2011 Nov 1;310(1):15-24.

Other Notes

Small volumes of EMD534085, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for EMD534085 purchase

MBS5764561 is an inhibitor targeting EMD534085.
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