GSK1070916

The Uses of GSK1070916

GSK 1070916 is a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models.

Definition

ChEBI: 3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethyl-3-pyrazolyl]phenyl]-1,1-dimethylurea is a member of pyrazoles and a ring assembly.

Biological Activity

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.