Triciribine (API-2)

Triciribine (API-2) is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.

CAS No. 35943-35-2

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
50mg	JPY 85500	国内在庫なし(納期7~10日)
1g	JPY 448500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（90）

製品安全説明書

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99.70

Triciribine (API-2)関連製品

関連ターゲット	Akt1 Akt2 Akt3	もっと見る
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シグナル伝達経路

Aktシグナル伝達経路

Akt阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
184B5	Cytotoxicity assay	20 uM		Cytotoxicity against human 184B5 cells at 20 uM chloroquine by SRB assay, GI50=16.96μM	18691894
MDA-MB-468	Cytotoxicity assay	10 uM		Cytotoxicity against human MDA-MB-468 cells in presence of 10 uM chloroquine by SRB assay, GI50=20.45μM	18691894
184B5	Cytotoxicity assay	10 uM		Cytotoxicity against human 184B5 cells at 10 uM chloroquine by SRB assay, GI50=34μM	18691894
MDA-MB-231	Cytotoxicity assay	10 uM		Cytotoxicity against human MDA-MB-231 cells in presence of 10 uM chloroquine by SRB assay, GI50=37μM	18691894
AA2	Function assay		5 hrs	Intracellular phosphorylation (100 uM) in uninfected AA2 cells was studied after 5 hrs of Incubation., Concentration=9μM	10882373
MDM	Antiviral assay		6 days	Antiviral activity against Human immunodeficiency virus 1 ADA infected in human MDM cells assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50=0.006μM	20086149
CEM-SS	Antiviral assay		6 days	Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 0.78 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50<0.01μM	20086149
MDM	Antiviral assay		6 days	Antiviral activity against Human immunodeficiency virus 1 BAL infected in human MDM cells assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50=0.018μM	20086149
H9	Antiviral assay		6 days	Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 12.5 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50<0.1μM	20086149
H9	Antiviral assay		6 days	Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 6.25 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50<0.1μM	20086149
ACH2	Antiviral assay		3 days	Antiviral activity against 5 x 10'3 cells/well Human immunodeficiency virus 1 infected in human ACH2 cells assessed as inhibition of viral Reverse transcriptase after 3 days by [3H]TTP incorporation assay in presence of 5 ng/ml tumor necrosis factor alpha, IC50=0.15μM	20086149
CEM-SS	Antiviral assay		6 days	Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 1.56 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50=0.19μM	20086149
CEM-SS	Antiviral assay		6 days	Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 3.13 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50=0.24μM	20086149
MCF7	Cytotoxicity assay			Cytotoxicity against human MCF7 cells in presence of 10 uM chloroquine by SRB assay, GI50=0.56μM	18691894
MCF7	Cytotoxicity assay			Cytotoxicity against human MCF7 cells in presence of 20 uM chloroquine by SRB assay, GI50=0.05μM	18691894
Huh-7	Function assay			Compound was tested for its ability to inhibit hepatitis C viral RNA replication in Huh-7 cells (human hepatoma cells), EC50=2μM	15177464
BSC-1	Antiviral assay			Antiviral activity against HSV-1 was determined using BSC-1 cells by an enzyme-linked immunosorbent assay (ELISA), IC50=23μM	10882373
HFF	Antiviral assay			Antiviral activity against HCMV was determined by plaque reduction assay using HFF cells, IC50=2.5μM	10882373
BSC-1	Antiviral assay			Antiviral activity was tested using an enzyme-linked immunosorbent assay (ELISA) to detect HSV-1 (herpes simplex virus type 1) using BSC-1 cells, IC50=23μM	10882371
HFF	Function assay			HCMV plaque assay was performed using HFF cells and effect was calculated as a percentage of reduction in number of plaques, IC50=2.5μM	10882371
L1210	Function assay			Tested in vitro for cytotoxicity against murine L1210 leukemic cells, IC50=0.035μM	10882371
MDA-MB-231	Cytotoxicity assay			Cytotoxicity against human MDA-MB-231 cells in presence of 20 uM chloroquine by SRB assay, GI50=0.69μM	18691894
MCF7	Cytotoxicity assay			Cytotoxicity against human MCF7 cells by SRB assay, GI50=3.64μM	18691894
MDA-MB-468	Cytotoxicity assay			Cytotoxicity against human MDA-MB-468 cells in presence of 20 uM chloroquine by SRB assay, GI50=10.29μM	18691894
184B5	Cytotoxicity assay			Cytotoxicity against human 184B5 cells by SRB assay, GI50=40μM	18691894
MDA-MB-468	Cytotoxicity assay			Cytotoxicity against human MDA-MB-468 cells by SRB assay, GI50=43.53μM	18691894
ACH2	Cytotoxicity assay			Cytotoxicity against human ACH2 cells infected with latent Human immunodeficiency virus 1 by MTS assay, CC50=0.01μM	20086149
ACH2	Cytotoxicity assay			Cytotoxicity against human ACH2 cells infected with latent Human immunodeficiency virus 1 by MTS assay in presence of tumor necrosis factor alpha, CC50=0.01μM	20086149
H9	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 SK1 infected in human H9 cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.036μM	20086149
CEM-SS	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 3B expressing nef protein infecting in CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.04μM	20086149
CEM-SS	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 0.78 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.08μM	20086149
H9	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 25 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50<0.1μM	20086149
H9	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 12.5 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50<0.1μM	20086149
H9	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 6.25 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50<0.1μM	20086149
CEM-SS	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 SK1 infected in human CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.13μM	20086149
AA5	Antiviral assay			Antiviral activity against of Human immunodeficiency virus 1 3B infected in AA5 cells infected with 3.13 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50<0.17μM	20086149
AA5	Antiviral assay			Antiviral activity against of Human immunodeficiency virus 1 3B infected in AA5 cells infected with 1.56 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50<0.17μM	20086149
AA5	Antiviral assay			Antiviral activity against of Human immunodeficiency virus 1 3B infected in AA5 cells infected with 0.78 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50<0.17μM	20086149
CEM-SS	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 harboring plasmid NL4-3 infected in CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.2μM	20086149
U1	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 infected in human U1 cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.23μM	20086149
U1	Cytotoxicity assay			Cytotoxicity against human U1 cells infected with latent Human immunodeficiency virus 1 by MTS assay, CC50=0.28μM	20086149
U1	Cytotoxicity assay			Cytotoxicity against human U1 cells infected with latent Human immunodeficiency virus 1 by MTS assay in presence of tumor necrosis factor alpha, CC50=0.28μM	20086149
CEM-SS	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 1.56 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.29μM	20086149
CEM-SS	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 3.13 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.3μM	20086149
CEM-SS	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 D1 harboring Tyr127His mutation in nef protein infecting in CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.33μM	20086149
CEM-SS	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 A7 harboring Tyr127His mutation in nef protein infecting in CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.5μM	20086149
MDM	Cytotoxicity assay			Cytotoxicity against human MDM cells infected with Human immunodeficiency virus 1 BAL by MTS assay, TC50=0.66μM	20086149
CEM-SS	Antiviral assay			Antiviral activity against Human immunodeficiency virus 2 ROD infected in human CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=1.4μM	20086149
H9	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 50 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=1.53μM	20086149
H9	Cytotoxicity assay			Cytotoxicity against human H9 cells by MTS assay, IC50=16.3μM	20086149
H9	Cytotoxicity assay			Cytotoxicity against human H9 cells by MTS assay, CC50=19.6μM	20086149
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生物活性

製品説明

Triciribine (API-2) is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.

Targets

HIV-1 ^[2] (CEM-SS, H9, H9IIIB, U1 cells)	Akt ^[1] (PC3 cells)
20 nM	130 nM

In Vitro
In vitro	Triciribine exhibits maximum growth inhibition around 1-10 μM and inhibits phosphorylation of Akt, as well as downstream p70S6K, to basal levels at 100μM (IC50 = 130 nM). Triciribine shows particular promise for inhibiting growth in Nf1 and Trp53 mutant astrocytoma cells in a grade-dependent manner. The WHO II K1861-10 line is inhibited, incompletely (69% maximum inhibition), with a GI50 value of 1.7 μM for Triciribine, whereas higher-grade tumor lines (KR158, KR130, and SF295) are inhibited to a greater extent (>80% maximum inhibition) at lower GI50 values (0.4–1.1 mM). Importantly, Triciribine is much less effective at inhibiting primary astrocytes (GI5013.6 mM), suggesting that this inhibitor may show specificity for tumor cells. ^[1] Triciribine inihibits HIV-1with an IC50 of 20 nM. Greater than 90% inhibition is achieved at 0.1μM and complete inhibition of syncytia formation is achieved at 5μM. Associated cell toxicity in the same cell line for Triciribine is 46 μM, resulting in selectivity indices of 2250. Triciribine markedly inhibits HIV-1-induced p24 core antigen production, reverse transcriptase, and infectious virus production in a dose-dependent manner using HIV-1 acutedly infected CEM-SS, H9, and persistently infected H9III _B and U1 cells. ^[2] Triciribine inhibits Akt phosphorylation at Thr308 and Ser473 and Akt activity in the human prostate cancer cell line PC-3. Triciribine sensitizes PC-3 cells to TRAIL- and anti-CD95-induced apoptosis, whereas the cells remain resistant to DNA damaging chemotherapeutics. ^[3] Triciribine is highly selective for Akt and does not inhibit the activation of phosphatidylinositol 3-kinase, phosphoinositide-dependent kinase-1, protein kinase C, serum and glucocorticoid-inducible kinase, protein kinase A, signal transducer and activators of transcription 3, extracellular signal-regulated kinase-1/2, or c-Jun NH2-terminal kinase. ^[4]
Kinase Assay	Akt Phosphorylation Changes Assay
Kinase Assay	Cells are grown to 80%–90% confluency and stimulated for 5–10 minutes with 1–10 ng/mL of epidermal growth factor or platelet derived growth factor (PDGF)–AA with or without 10–20 mM of U0126 or LY-294002. Protein lysates (5–20 μg) are separated by 12%–15% SDS PAGE and analyzed by Western blot for Akt, phosphorylated Akt (phospho-Ser 473), MAPK, and phosphorylated MAPK (p44/42 phospho-Thr202/Tyr204) antibodies (1:1000).
細胞実験	細胞株	CEM-SS cells
	濃度	0-500 μM
	反応時間	48 hours
	実験の流れ	Triciribine is evaluated for cytotoxicity by seeding CEM-SS cells at a density of 1 × 10⁴ cells/well in growth medium, using a 96-well flat-bottom plate. Serial fivefold dilutions of Triciribine are prepared in growth medium and added to the wells as a second overlay. After a 48-hours incubation at 37 °C, the cells are pulse labeled with [³H]dThd (1 μCi per well, specific activity 20 Ci/mmol) for 6 hours and the cells are harvested to measure total DNA synthesis.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	PUMA / p-FoxO3a / p-AKT		20978166
	Immunofluorescence	TRF2 / 53BP1		23862686

In Vivo
In Vivo	1 mg/kg/day i.p. treated Triciribine inhibits OVCAR3, OVCAR8 and PANC1 tumor growth, which overexpressing Akt, by 90%, 88% and 80% in nude mice, respectively. However, Triciribine has little effect on the growth of OVCAR5 and COLO357 cells. ^[4]
動物実験	動物モデル	OVCAR3, OVCAR8, PANC1, OVCAR5 and COLO357 tumor cells are injected s.c. into 80week-old female nude mice.
	投与量	1 mg/kg/day
	投与経路	Triciribine is administrated through i.p. injection once a day.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT02987127	Unknown status	Mucosa-Associated Lymphoid Tissue Lymphoma	National Taiwan University Hospital	February 2016	--
NCT00642031	Completed	Hematologic Malignancies\|Leukemia	Prescient Therapeutics Ltd.\|VioQuest Pharmaceuticals	August 2006	Phase 1

参考
[1] Gursel DB, et al, Nero Oncol, 2011, 13(6), 610-621. [2] Kucera LS, et al, AIDS Res Hum Retroviruses, 1993, 9(4), 307-314. [3] Dieterle A, et al, Int J Cancer , 2009, 125(4), 932-941. [4] Yang L, et al, Cancer Res, 2004, 64(13), 4394-4399. + 展開

参考

[4] Yang L, et al, Cancer Res, 2004, 64(13), 4394-4399.

+ 展開

化学情報

分子量	320.3	化学式	C₁₃H₁₆N₆O₄
CAS No.	35943-35-2	SDF	Download Triciribine (API-2) SDFをダウンロードする
Smiles	CN1C2=NC=NC3=C2C(=CN3C4C(C(C(O4)CO)O)O)C(=N1)N
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 64 mg/mL ( (199.81 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 16 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):