GSK690693

A novel ATP competitive, pan-AKT kinase inhibitor with IC50 values of 2, 13, and 9 nM against AKT1, 2, and 3, respectively. It inhibits GSK3β phosphorylation and tumor growth in human breast carcinoma (BT474) xenografts, and induces growth inhibition and apoptosis in acute lymphoblastic leukemia cell lines.

Store at 0° C (short term), -20° C (long term), desiccated

HPLC-MS, ¹HNMR, Chiral HPLC, and Quantitative Elemental Analysis

1. M.C. Crouthamel, J.A. Kahana, S. Korenchuk, S.Y. Zhang, G. Sundaresan, D.J. Eberwein, K.K. Brown, R. Kumar. Mechanism and management of AKT inhibitor-induced hyperglycemia. Clin. Cancer Res. 2009, 15(1), 217-225.

2. Dirk A. Heerding, Nelson Rhodes, Jack D. Leber, et al., Identification of 4-(2-(4-Amino-1, 2, 5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4, 5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhibitor of AKT Kinase, J. Med. Chem., 2008, 51 (18), 5663-5679.

3. D.S. Levy, J.A. Kahana, R. Kumar. AKT inhibitor, GSK690693, induces growth inhibition and apoptosis in acute lymphoblastic leukemia cell lines, Blood. 2009, 113(8), 1723-1729.