GSK1070916 Inhibitor CAS No. 942918-07-2

Cat. No.	Name	Size	Price
KI1161	GSK1070916	5 mg	$336
	GSK1070916	10 mg	$592
	GSK1070916	50 mg	$1552
	GSK1070916	200 mg	$3952

Chemical Characteristic

Product Name	GSK1070916
CAS No.	942918-07-2
Molecular Weight	507.63
Formula	C₃₀H₃₃N₇O
Chemical 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-dimethylurea
Smiles	N(C(=O)Nc1ccc(cc1)c1nn(cc1c1c2c(ncc1)[nH]c(c2)c1cc(ccc1)CN(C)C)CC)(C)C
Chemical Structure

Biological activities

GSK1070916 is a novel, potent and selective ATP competitive inhibitor of Aurora B and Aurora C kinases with IC50 values of 3.5 and 6.5 nM, respectively. GSK1070916 selectively inhibits Aurora B and Aurora C kinases with Ki of 0.38 and 1.5 nM, and inhibits Aurora A with Ki of 490 nM.^[1] GSK1070916 also inhibits the activity of FLT1, TIE2, SIK, FLT4, and FGFR1 with IC50 values of 42, 59, 70, 74, and 78 nM, respectively.^[2] Human tumor cells (including Colo205, MX-1, HCT116, A549 and HeLa) treated with GSK1070916 shows dose-dependent inhibition of phosphorylation on serine 10 of Histone H3 (a substrate specific for Aurora B kinase) with EC50 values ranging from 8-118 nM. In nude mice implanted with human colon tumor (HCT116) xenografts, GSK1070916 administration (25, 50 and 100 mg/kg) inhibits HH3-S10 phosphorylation in a dose-dependent manner. GSK1070916 (100 mg/kg) also produces antitumor activity with complete or partial regressions in lung cancer cell line A549, colon cancer cell line HCT116, acute myelogenous leukemia (AML) cancer cell line HL60, and chronic myelogenous leukemia cancer cell line K562 tumor models.^[3]

Protocols

In vitro: GSK1070916 is dissolved in DMSO.^[3]

References

[1] Anderson K, et al. Biochemical characterization of GSK1070916, a potent and selective inhibitor of Aurora B and Aurora C kinases with an extremely long residence time1. Biochem J. 2009, 420(2): 259-265. [2] Kimura M, et al. Cell cycle-dependent expression and spindle pole localization of a novel human protein kinase, Aik, related to Aurora of Drosophila and yeast Ipl1. J Biol Chem. 1997, 272(21): 13766-13771. [3] Hardwicke MA, 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. 2009, 8(7): 1808-1817.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com