GSK1070916

  Cat. No.:  DC7140   Featured
GSK1070916
Chemical Structure
942918-07-2
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Field of application
GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM; displays >100-fold selectivity against the closely related Aurora A-TPX2 complex(IC50=490 nM).
Cas No.: 942918-07-2
Chemical Name: 3-(4-(4-(2-(3-((dimethylamino)methyl)phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-ethyl-1H-pyrazol-3-yl)phenyl)-1,1-dimethylurea
Synonyms: GSK1070916,GSK-1070916,GSK 1070916
SMILES: N(C)(C)C(NC1=CC=C(C2C(C3C=CN=C4NC(C5=CC=CC(CN(C)C)=C5)=CC4=3)=CN(CC)N=2)C=C1)=O
Formula: C30H33N7O
M.Wt: 507.63
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:
Description: GSK1070916 selectively inhibits Aurora B and Aurora C with Ki of 0.38 nM and 1.5 nM over Aurora A with Ki of 490 nM. Inhibition of Aurora B and Aurora C is time-dependent, with an enzyme-inhibitor dissociation half-life of >480 min and 270 min respectively. In addition, GSK1070916 is also a competitive inhibitor with respect to ATP. Human tumor cells treated with GSK1070916 shows dose-dependent inhibition of phosphorylation on serine 10 of Histone H3, a substrate specific For Aurora B. Moreover, GSK1070916 inhibits the proliferation of tumor cells with EC50 values of <10 nM in over 100 cell lines spanning a broad range of tumor types, with a median EC50 of 8 nM. Although GSK1070916 has potent activity against proliferating cells, a dramatic shift in potency is observed in primary, nondividing, normal human vein endothelial cells. Furthermore, GSK1070916-treated cells do not arrest in mitosis but instead fails to divide and become polyploid, ultimately leading to apoptosis. In another study, it is also reported high chromosome number associated with resistance to the inhibition of Aurora B and C suggests cells with a mechanism to bypass the high ploidy checkpoint are resistant to GSK1070916. GSK1070916 (25, 50, or 100 mg/kg) shows dose-dependent inhibition of phosphorylation of an Aurora B–specific substrate in mice and consistent with its broad cellular activity, has antitumor effects in 10 human tumor xenograft models including breast, colon, lung, and two leukemia models. For the detailed information of GSK-1070916, the solubility of GSK-1070916 in water, the solubility of GSK-1070916 in DMSO, the solubility of GSK-1070916 in PBS buffer, the animal experiment (test) of GSK-1070916, the cell expriment (test) of GSK-1070916, the in vivo, in vitro and clinical trial test of GSK-1070916, the EC50, IC50,and Affinity of GSK-1070916, Please contact DC Chemicals.
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MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC7140 GSK1070916 GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM; displays >100-fold selectivity against the closely related Aurora A-TPX2 complex(IC50=490 nM).