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Cat. No. M3555
GSK1070916 Structure


Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 160  USD160 In stock
50mg USD 480  USD480 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

GSK1070916 is a novel, highly potent and selective Aurora B/C kinases ATP competitive inhibitor with an EC50 of <10 nM. The protein kinases, Aurora A, B, and C have critical roles in the modulation of mitosis and are frequently overexpressed or amplified in human tumors. Human tumor cells treated with GSK1070916 revealed dose-dependent inhibition of phosphorylation on serine 10 of Histone H3, a substrate specific for Aurora B kinase. Moreover, GSK1070916 supprresses the proliferation of tumor cells. GSK1070916 displays dose-dependent inhibition of phosphorylation of an Aurora B–specific substrate in mice and consistent with its broad cellular activity, possesses antitumor effects in 10 human tumor xenograft models including breast, colon, lung, and two leukemia models. In another study, GSK1070916 selectively prevents AurB-INCENP (Ki=0.38 nM) and AurC-INCENP (Ki=1.5 nM) over AurA-TPX2 (target protein for Xenopus kinesin-like protein 2) (Ki=490 nM). Suppression of AurB-INCENP and AurC-INCENP is time-dependent, with an enzyme-inhibitor dissociation half-life of more than 480 min and 270 min respectively.

Cell Experiment
Cell lines SW48, Colo 201, SW480, WiDr, Colo205, RKO E6, RKO, LoVo, HCT-116, SW620, HT29, W1417, DLD-1, HCT-8, Colo 320HSR, Hep-3B, OVCAR-3, MEC-1 cells
Preparation method Plating cells in 96-well plates in the recommended growth media and incubated at 37 °C in 5% CO2 overnight. The following day, treating the cells with serial dilutions of GSK1070916. At this time, treating one set of cells with CellTiter-Glo for a time equal to 0 (T = 0) measurement. Following a 6- to 7-d incubation with compound, using the CellTiter-Glo reagent to measure cell proliferation according to the manufacture's recommended protocol. As inhibition of Aurora B induces endomitosis, the degree of which differs depending on the cell type, an extended compound treatment time is required to accurately reflect the effects on cell viability across a large panel of cell lines. For analysis of cell viability, values from wells with no cells are subtracted for background correction and the data plotted as a percent of the DMSO-treated control samples using Microsoft Excel XLfit4 software. The EC50 values represent the concentration of GSK1070916 where 50% maximal effect is observed
Concentrations 0-15 mM
Incubation time 6-7 days
Animal Experiment
Animal models Mice tumor xenograft models (A549, SW620, HCT116, H460, MCF-7, HL60, K562, Colo205)
Formulation 2% Cremophor EL, 2% N,N-dimethylacetamide, and 96% acidified water (pH 5.0)
Dosages 25, 50, or 100 mg/kg
Administration Administered via i.p. once daily
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 507.63
Formula C30H33N7O
CAS Number 942918-07-2
Purity >98%
Solubility DMSO 100 mg/mL
Storage at -20°C

[1] Zhuo-Xun Wu, et al. Overexpression of human ATP-binding cassette transporter ABCG2 contributes to reducing the cytotoxicity of GSK1070916 in cancer cells

[2] Christopher Moy, et al. High chromosome number in hematological cancer cell lines is a negative predictor of response to the inhibition of Aurora B and C by GSK1070916

[3] Nicholas D Adams, et al. Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase

[4] Jesus R Medina, et al. Discovery of a new series of Aurora inhibitors through truncation of GSK1070916

[5] Mary Ann Hardwicke, et al. GSK1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models

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Abmole Inhibitor Catalog

Keywords: GSK1070916, GSK-1070916A supplier, Aurora Kinase, inhibitors

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