Triciribine phosphate (TCN-P) is synthesized as a water-soluble derivative of the tricyclic nucleoside TCN. TCN and TCN-P equally inhibits the growth of L1210 cells in vitro. TCN-P is required to be hydrolyzed to TCN and then rephosphorylated intracellularly. This requirement of hydrolysis has also been shown directly in human erythrocytes, which lack ectophosphatases [1]. The intracellular formation of TCN-P from TCN was rapid,concentrative and essentially complete, but TCN-P does not exceed about 1.4 mM (1.4 nmol/106 cells) at 200 μM TCN [2]. TCN-P inhibits in vitro neither Akt kinase activity nor the phosphorylation of purified Akt by PDK1 and mTOR. TCN-P, but not TCN, binds to the PH domain of Akt and blocks its recruitment to the membrane, and that the subsequent inhibition of Akt phosphorylation contributes to TCN-P antiproliferative and proapoptotic activities.TCN-P may act as a beneficial therapeutic agent to patients whose tumors express persistently phosphorylated Akt [3].Triciribine phosphate monohydrate (TCN-PM) has currently been in phase I or phase II clinical trials for many solid tumors containing activated Akt, such as metastatic breast cancer and ovarian cancer.
Chemical Properties
Cas No.: 61966-08-3
M. Wt.: 400.28
Formula: C13H17N6O7P
Purity: >98%
Synonym: VQD-002, TCN-P, NSC-280594
Chemical Name:((2R,3S,4R,5R)-5-(3-amino-5-methyl-1,4,5,6,8-pentaazaacenaphthylen-1(5H)-yl) -3,4-dihydroxytetrahydrofuran- 2-yl)methyl dihydrogen phosphate
Solubility: Soluble in DMSO
Storage:Store solid at -20 ºC for the stability up to two years.