A potent inhibitor of Aurora B and C kinases
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GSK1070916

Item No. 22953

Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N'-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethyl-1H-pyrazol-3-yl]phenyl]-N,N-dimethyl-urea
CAS Number
942918-07-2
Molecular Formula
C30H33N7O
Formula Weight
507.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 3 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.2 mg/ml
λmax
252, 334 nm
SMILES
CN(C)CC1=CC=CC(C2=CC3=C(C4=CN(CC)N=C4C5=CC=C(NC(N(C)C)=O)C=C5)C=CN=C3N2)=C1
InChi Code
InChI=1S/C30H33N7O/c1-6-37-19-26(28(34-37)21-10-12-23(13-11-21)32-30(38)36(4)5)24-14-15-31-29-25(24)17-27(33-29)22-9-7-8-20(16-22)18-35(2)3/h7-17,19H,6,18H2,1-5H3,(H,31,33)(H,32,38)
InChi Key
QTBWCSQGBMPECM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    GSK1070916 is a potent and ATP-competitive inhibitor of Aurora kinases B and C (Kis = 0.38 and 1.5 nM, respectively).1 It is >250-fold selective for Aurora B and C over Aurora A. GSK1070916 inhibits proliferation of A549 lung cancer cells in vitro (EC50 = 7 nM). It also inhibits proliferation in a panel of 100 tumor cell lines (EC50s = <10 nM) via induction of polyploidy and apoptosis.2 In vivo, GSK1070916 inhibits histone H3 phosphorylation in a COLO 205 mouse xenograft model and induces tumor regression in an HL-60 mouse xenograft model.1 It also reduces tumor growth in 10 mouse xenograft models, including models of breast, colon, and lung carcinomas as well as leukemias.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Adams, N.D., Adams, J.L., Burgess, J.L., et al. Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J. Med. Chem. 53(10), 3973-4001 (2010).

    2. Hardwicke, M.A., Oleykowski, C.A., Plant, R.N., et al. GSK1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models. Mol. Cancer. Ther. 8(7), 1808-1817 (2009).