An Eg5 inhibitor
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EMD 534085

Item No. 35719

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-(dimethylamino)ethyl]-N′-[[(2R,4aS,5R,10bS)-3,4,4a,5,6,10b-hexahydro-5-phenyl-9-(trifluoromethyl)-2H-pyrano[3,2-c]quinolin-2-yl]methyl]-urea
CAS Number
858668-07-2
Molecular Formula
C25H31F3N4O2
Formula Weight
476.5
Purity
≥99%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
SMILES
CN(C)CCNC(NC[C@@H]1O[C@@]2([H])[C@](CC1)([H])[C@@](C3=CC=CC=C3)([H])NC4=CC=C(C(F)(F)F)C=C42)=O
InChi Code
InChI=1S/C25H31F3N4O2/c1-32(2)13-12-29-24(33)30-15-18-9-10-19-22(16-6-4-3-5-7-16)31-21-11-8-17(25(26,27)28)14-20(21)23(19)34-18/h3-8,11,14,18-19,22-23,31H,9-10,12-13,15H2,1-2H3,(H2,29,30,33)/t18-,19+,22+,23+/m1/s1
InChi Key
MARIUIDCPUZLKZ-FUKQBSRTSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $44

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    1 mg

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    5 mg

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    10 mg

    $605

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    Cayman Chemical
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    Product Description

    EMD 534085 is an inhibitor of the kinesin spindle protein Eg5 (IC50 = 8 nM).1 It inhibits proliferation of HCT116 colon cancer cells (IC50 = 30 nM), as well as induces mitotic arrest and apoptosis in HL-60 leukemia cells.1,2 EMD 534085 (15 and 30 mg/kg) reduces tumor growth in a COLO 205 colon cancer mouse xenograft model.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schiemann, K., Finsinger, D., Zenke, F., 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. 20(5), 1491-1495 (2010).

    2. Tang, Y., Orth, J.D., Xie, T., et al. Rapid induction of apoptosis during Kinesin-5 inhibitor-induced mitotic arrest in HL60 cells. Cancer Lett. 310(1), 15-24 (2011).