GSK1070916 (NMI900 or GSK1070916 A)

Alias: GSK-1070916A; GSK 1070916A; GSK1070916A;GSK-1070916; GSK 1070916; GSK1070916; NMI 900; NMI900; NMI-900.
Cat No.:V0355 Purity: ≥98%
GSK1070916 (also known as NMI-900 or GSK-1070916A)is a novel, potent, reversible and ATP-competitive inhibitor of Aurora B/C with potential antitumor activity.
GSK1070916 (NMI900 or GSK1070916 A) Chemical Structure CAS No.: 942918-07-2
Product category: Aurora Kinase
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

GSK1070916 (also known as NMI-900 or GSK-1070916A) is a novel, potent, reversible and ATP-competitive inhibitor of Aurora B/C with potential antitumor activity. It inhibits Aurora B/C with IC50 of 3.5 nM/6.5 nM and displays >100-fold selectivity for Aurora B/C over the closely related Aurora A-TPX2 complex. It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. GSK1070916 A binds to and inhibits the activity of Aurora kinases B and C, which may result in inhibition of cellular division and a decrease in the proliferation of tumor cells that overexpress the Aurora kinases B and C. Aurora kinases play essential roles in mitotic checkpoint control during mitosis, and are overexpressed by a wide variety of cancer cell types.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
GSK-1070916 has a modest inhibitory impact on Aurora A/TPX2, with a Ki of 492±61 nM, while it significantly inhibits the kinases of Aurora B/INCENP and Aurora C/INCENP, with Ki of 0.38±0.29 and 1.45±0.35 nM, respectively. Additionally, FLT1, TIE2, SIK, FLT4, and FGFR1 are inhibited by GSK-1070916, with IC50 values of 42, 59, 70, 74, and 78 nM, respectively. GSK-1070916 treatment of human lung cancer A549 cells can result in a strong anti-proliferative impact (EC50=7 nM) [1]. GSK-1070916 has been demonstrated to suppress HH3-S10 phosphorylation in all tumor cell lines, with average EC50 values ranging from 8 to 118 nM [2]. The compound also inhibits a panel of tumor cell lines.
ln Vivo
GSK-1070916 injected intraperitoneally (i.p.) suppresses HH3-S10 phosphorylation in a dose-dependent manner in nude mice implanted with human colon tumor (HCT116) xenografts. Upon repeated intraperitoneal (i.p.) administration of GSK-1070916, four out of eight tumor types (lung, A549; colon, HCT116; acute myelogenous leukemia (AML), HL60; and chronic myelogenous leukemia, K562) exhibit complete or partial antitumor activity; three of the eight exhibit stable disease (colon, Colo205; lung, H460; and breast, MCF-7); and one of the eight tumor types (colon, SW620) exhibits tumor growth delay. In general, GSK-1070916 is well tolerated when taken daily[2].
Animal Protocol
Formulated in 2% Cremophor EL, 2% N,N-dimethylacetamide, and 96% acidified water (pH 5.0); 25, 50, or 100 mg/kg; i.p. injection.
Mice tumor xenograft models (A549, SW620, HCT116, H460, MCF-7, HL60, K562, Colo205)
References
[1]. Adams ND, et al. Discovery of GSK-1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001.
[2]. Hardwicke MA, et al. GSK-1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models. Mol Cancer Ther. 2009 Jul;8(7):1808-17
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C30H33N7O
Molecular Weight
507.63
CAS #
942918-07-2
SMILES
O=C(N(C([H])([H])[H])C([H])([H])[H])N([H])C1C([H])=C([H])C(=C([H])C=1[H])C1C(=C([H])N(C([H])([H])C([H])([H])[H])N=1)C1C([H])=C([H])N=C2C=1C([H])=C(C1=C([H])C([H])=C([H])C(C([H])([H])N(C([H])([H])[H])C([H])([H])[H])=C1[H])N2[H]
Synonyms
GSK-1070916A; GSK 1070916A; GSK1070916A;GSK-1070916; GSK 1070916; GSK1070916; NMI 900; NMI900; NMI-900.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 102 mg/mL (200.9 mM)
Water:<1 mg/mL
Ethanol: N/a
Solubility (In Vivo)
2% Cremophor EL, 2% N,N-dimethylacetamide, pH 5.0:~30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9699 mL 9.8497 mL 19.6994 mL
5 mM 0.3940 mL 1.9699 mL 3.9399 mL
10 mM 0.1970 mL 0.9850 mL 1.9699 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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