GSK-1070916  (Synonyms: GSK-1070916A)

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 K_is of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A^[1][2].

GSK-1070916 (GMP) potently inhibits Aurora B/INCENP and Aurora C/INCENP kinases with K_is of 0.38 and 1.45 nM, respectively, but is less potent against Aurora A/ TPX2 with a K_i 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.

In nude mice implanted with human colon tumor (HCT116) xenografts, a single dose of GSK-1070916 (GMP) administered i.p. inhibits HH3-S10 phosphorylation in a dose-dependent manner. Repeated i.p. administration of GSK-1070916 (GMP) produces complete or partial antitumor activity in 4 of 8 tumor types [lung, A549; colon, HCT116; acute myelogenous leukemia (AML), HL60; and chronic myelogenous leukemia, K562], stable disease in 3 of 8 (colon, Colo205; lung, H460; and breast, MCF-7), and tumor growth delay in 1 of 8 tumor types (colon, SW620). Daily administration of GSK-1070916 (GMP) is generally well-tolerated^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

507.63

C₃₀H₃₃N₇O

942918-07-2

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]