An inhibitor of CENP-E
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GSK923295

Item No. 18389

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-chloro-N-[(1S)-2-[[2-(dimethylamino)acetyl]amino]-1-[[4-[8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl]phenyl]methyl]ethyl]-4-(1-methylethoxy)-benzamide
CAS Number
1088965-37-0
Synonyms
  • GSK923295A
Molecular Formula
C32H38ClN5O4
Formula Weight
592.1
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml
λmax
209, 251, 317 nm
SMILES
O=C(C1=CC=C(OC(C)C)C(Cl)=C1)N[C@H](CNC(CN(C)C)=O)CC2=CC=C(C3=CN(C=CC=C4[C@H](C)O)C4=N3)C=C2
InChi Code
InChI=1S/C32H38ClN5O4/c1-20(2)42-29-13-12-24(16-27(29)33)32(41)35-25(17-34-30(40)19-37(4)5)15-22-8-10-23(11-9-22)28-18-38-14-6-7-26(21(3)39)31(38)36-28/h6-14,16,18,20-21,25,39H,15,17,19H2,1-5H3,(H,34,40)(H,35,41)/t21-,25-/m0/s1
InChi Key
WHMXDBPHBVLYRC-OFVILXPXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $37

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    5 mg

    $163

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    10 mg

    $289

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    50 mg

    $896

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    Cayman Chemical
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    Product Description

    GSK923295 is a potent inhibitor of centromere-associated protein E (CENP-E; Ki = 3.2 nM), a kinesin motor protein involved in mitotic checkpoint signaling.1,2 GSK923295 causes mitotic cell cycle delay, leading to apoptosis in various cancer cell lines.1 It induces apoptosis in cancer cells in mice bearing xenografts of COLO 205 cells.1,2 GSK923295 can be used with AZ3146, an inhibitor of the spindle checkpoint kinase Mps1, to generate aneuploidy in cells.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wood, K.W., Lad, L., Luo, L., et al. Antitumor activity of an allosteric inhibitor of centromere-associated protein-E. Proc. Natl. Acad. Sci. USA 107(13), 5839-5844 (2010).

    2. Qian, X., McDonald, A., Zhou, H.-J., et al. Discovery of the first potent and selective inhibitor of centromere-associated protein E: GSK923295. ACS Med. Chem. Lett. 1(1), 30-34 (2010).

    3. Bennett, A., Bechi, B., Tighe, A., et al. Cenp-E inhibitor GSK923295: Novel synthetic route and use as a tool to generate aneuploidy. Oncotarget 6(25), 20921-20932 (2015).