GSK690693

Background Information:

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.

Reference:

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.

APIM050170: GSK690693

CAS No.: 937174-76-0.
Molecular Formula: C₂₁H₂₇N₇O₃ ? 0.6HCl.
Molecular Weight: 447.4.
Purity: >99.5% chem and optical purity (HPLC and chiral HPLC at 220 nm).
QC: HPLC-MS, ¹HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: In DMSO, Water with 1 eq of acid.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.