Triciribine(API-2) (Akt1,2,3 inhibitor)

保质期 ：2 years

英文名 ：Triciribine(API-2) (Akt1,2,3 inhibitor)

库存 ：10

供应商 ：上海伟进生物科技有限公司

CAS号 ：35943-35-2

保存条件 ：-20℃

规格 ：1mg

Biological Activity

Triciribine (TCN) is a synthetic tricyclic nucleoside that is activated to its phosphate TCN-P by adenosine kinase and to inhibit cell growth, purine nucleotide synthesis, and incorporation of amino acids into proteins. In L1210 murine leukemic cells, TCN inhibits DNA synthesis through two mechanisms, either suppression of Okazaki fragment initiation or inhibition of the elongation of existing DNA chains. These two effects have different concentration responses ^[1-2]. TCN and TCN-P displays antiviral activity against a panel of HIV-1 and HIV-2 at IC₅₀ values ranging from 0.02 to 0.46 μM ^[3]. Triciribine (API-2) selectively inhibits the phosphorylation and activation of Akt-1,-2 and -3, but does not directly suppress Akt kinase as well as known upstream activators of Akt including PI 3K and PDK1.API-2 potently inhibits Akt signaling in human tumor cells with aberrant Akt, leading to inhibition of cell growth and induction of apoptosis. In a xenograft nude mice model, API-2 significantly inhibits tumor growth in Akt-overexpressing cells but not in the tumors with low levels of Akt ^[4]. Phase I and II clinic trials of API-2 has been conducted on many advanced tumors, such as metastatic breast cancer ^[5].

Chemical Properties

Cas No.: 35943-35-2	M. Wt.: 320.31
Formula: C13H16N6O4	Purity: >98%
Synonym: TCN, Akt/PKB signaling inhibitor-2 (API-2), NSC 154020, tricyclic nucleoside
Chemical Name: 1,5-Dihydro-5-methyl-1-β-D-ribofuranosyl-1,4,5,6,8-pentaazaacenaphthylen-3-amine
Appearance: Pale yellow solid
Solubility: Soluble in DMSO (30 mg/ml), sparingly soluble in water.
Storage: Store powder at -20 ºC for the stability up to two years.