GSK-1070916 (GMP) is GSK-1070916 (HY-70044) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.
For research use only. We do not sell to patients.
- CAS No.: 942918-07-2
- Formula: C30H33N7O
- Molecular Weight:507.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Aurora Kinase Isoforms
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Biological Activity
GSK-1070916 (GMP) potently inhibits Aurora B/INCENP and Aurora C/INCENP kinases with Kis of 0.38 and 1.45 nM, respectively, but is less potent against Aurora A/ TPX2 with a Ki of 492 nM. GSK-1070916 (GMP) also inhibits FLT1, TIE2, SIK, FLT4, and FGFR1 with IC50 values of 42, 59, 70, 74, and 78 nM, respectively. Treatment of A549 human lung cancer cells with GSK-1070916 (GMP) results in a potent antiproliferative effect (EC50=7 nM)[1]. GSK-1070916 (GMP)inhibits a panel of tumor cell lines and is shown o inhibits the phosphorylation of HH3- S10 in all cell lines with average EC50 values ranging from 8 to 118 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 942918-07-2
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Molecular Weight 507.63
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Formula C30H33N7O
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SMILES
O=C(NC1=CC=C(C2=NN(C=C2C3=C4C(NC(C5=CC=CC(CN(C)C)=C5)=C4)=NC=C3)CC)C=C1)N(C)C
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Synonyms
GSK-1070916A (GMP)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)