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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.
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