GSK1070916|Aurora B/C inhibitor|CAS# 942918-07-2

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Size	Price	Stock
10mM (in 1mL DMSO)	$150.00	In stock
5mg	$90.00	In stock
10mg	$150.00	In stock
50mg	$400.00	In stock
200mg	$1,200.00	In stock

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Nature.
2017 Jan 19;541(7637):417-420.

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2016 Apr 21;532(7599):398-401.

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2016 Aug 5;353(6299)594-8

Nature Biotechnology.
2017 Jun;35(6):569-576

Cell.
2017 Apr 6;169(2):286-300.

Cell.
2015 Aug 27;162(5):987-1002.

Cell.
2015 Feb 12;160(4):729-44.

Nature Medicine.
2017 Apr;23(4):493-500.

Cancer Cell.
2017 May 8;31(5):635-652.e6.

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2015 May;17(5):627-38.

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2017 Jun;18(6):654-664.

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2015 Oct;18(10):1464-73.

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2016 Sep;26(9):1007-20.

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2017 May 18;66(4):546-557.

Mol Cell.
2017 Jun 1;66(5):698-710.

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2017 Mar 2;65(5):941-955.e8.

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2016 Feb 1;7:10492.

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2015 Jun 30;112(26):E3365-73.

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2015 Jul 28;112(30):9412-7.

Autophagy.
2016 Jul 2;12(7):1129-52.

Cancer Res canres.
2946.2015.

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2016 Jan 14;5. pii: e12203.

Nucleic Acids Res.
2016 Feb 18;44(3):e2.

EMBO Rep.
2015 Sep;16(9):1114-30.

Oncogene.
2016 Mar 21.

Cell Rep.
2015 Sep 29;12(12):1986-96.

Cell Death Differ.
2016 Jun;23(6):1026-37.

Cell Death Differ.
2016 Jan;23(1):76-88.

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Quality Control

Quality Control & MSDS

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Purity = 98.00%

Chemical structure

Biological Activity

Description	GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B and C with IC50 value of 3.5 nM and 6.5 nM, respectively.
Targets	Aurora B	Aurora C
IC50	3.5 nM	6.5 nM

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Chemical Properties

Cas No.	942918-07-2	SDF	Download SDF
Chemical Name	3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethylpyrazol-3-yl]phenyl]-1,1-dimethylurea
Canonical SMILES	CCN1C=C(C(=N1)C2=CC=C(C=C2)NC(=O)N(C)C)C3=C4C=C(NC4=NC=C3)C5=CC(=CC=C5)CN(C)C
Formula	C₃₀H₃₃N₇O	M.Wt	507.63
Solubility	>25.4mg/mL in DMSO	Storage	Store at -20°C
General tips	N/A
Shipping Condition	N/A

Background

GSK1070916 is a potent and selective inhibitor of Aurora B/C Kinase with Ki values of 0.38nM and 1.5nM, respectively [1].

GSK1070916 is a reversible ATP-competitive inhibitor of Aurora B and Aurora C with Ki values of 0.38nM and 1.5nM, respectively. The SPA assay shows GSK1070916 has a good selectivity over Aurora A. It inhibits Aurora B with IC50 value of 5nM but 1259nM for Aurora A. It is also reported that treatment of GSK1070916 suppresses cell proliferation in A549 human lung cancer cells with EC50 value of 7nM. Moreover, both in vitro and in vivo assays demonstrate GSK1070916 can inhibit the phosphorylation of histone H3, which is a substrate of Aurora B. GSK1070916 can also suppress tumor growth in mice with HL-60 tumor xenografts [1].

References:
[1] Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA, Huffman WF, Koretke-Brown KK, Lai ZV, McDonald OB, Nakamura H, Newlander KA, Oleykowski CA, Parrish CA, Patrick DR, Plant R, Sarpong MA, Sasaki K, Schmidt SJ, Silva DJ, Sutton D, Tang J, Thompson CS, Tummino PJ, Wang JC, Xiang H, Yang J, Dhanak D. Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001.