GSK-923295

Research use only, not for human use.

The first potent, allosteric inhibitor of CENP-E kinesin motor ATPase activity with Ki of 3.2 nM.

The first potent, allosteric inhibitor of CENP-E kinesin motor ATPase activity with Ki of 3.2 nM; shows excellent selectivity against a panel of mitotic human kinesins; exhibits inhibition of cell proliferation in a broad panel of human cancer cell lines and induces mitotic arrest leading to apoptosis and cell death (SKOV-3 IC50=22 nM; Colo205 IC50=22 nM); induces tumor regressions in vivo.Solid Tumors Phase 1 Clinical

GSK 923295;GSK923295

Cytoskeleton/Cell Adhesion Molecules

Kinesin

CENP-E

Cancer

Solid Tumors

1088965-37-0

592.13

C32H38ClN5O4

>98% (HPLC)

10 mM in DMSO

O=C(N[C@@H](CC1=CC=C(C2=CN3C=CC=C([C@@H](O)C)C3=N2)C=C1)CNC(CN(C)C)=O)C4=CC=C(OC(C)C)C(Cl)=C4

Benzamide, 3-chloro-N-[(1S)-2-[[2-(dimethylamino)acetyl]amino]-1-[[4-[8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl]phenyl]methyl]ethyl]-4-(1-methylethoxy)-

(-20℃)

With Ice Pack

≥ 2 years