Triciribine (API-2)

別名: NSC 154020, VD-0002, vqd-002, TCN 中文名稱：曲西立濱

目錄號(hào)：S1117 Purity: 99.70%

Triciribine (API-2)是一種DNA synthesis抑制劑，也抑制PC3細(xì)胞系中的Akt和CEM-SS，H9，H9IIIB，U1細(xì)胞中的HIV-1，IC50分別為130 nM和20 nM；對(duì)PI3K/PDK1沒有抑制作用；作用于缺乏腺苷激酶的細(xì)胞，活性降低5000倍。Phase 1/2。

Triciribine (API-2) Chemical Structure

CAS: 35943-35-2

規(guī)格	價(jià)格	庫存
10mM (1mL in DMSO)	1235.93	現(xiàn)貨
5mg	984.87	現(xiàn)貨
50mg	4673.78	現(xiàn)貨
200mg	13677.3	現(xiàn)貨
1g	32678.1	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.70%

99.70

Triciribine (API-2)相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	Akt1 Akt2 Akt3	點(diǎn)擊展開
相關(guān)產(chǎn)品	MK-2206 2HCl Perifosine SC79 Capivasertib (AZD5363) GSK690693 Ipatasertib (GDC-0068) CCT128930 Afuresertib (GSK2110183) A-674563 HCl AT7867 Oridonin Akti-1/2 PHT-427 TIC10 (ONC201) Miransertib (ARQ 092) HCl AT13148 Uprosertib (GSK2141795) Miransertib (ARQ-092) SC66 Deguelin ML-9 HCl	點(diǎn)擊展開
相關(guān)化合物庫	激酶抑制劑庫 PI3K/Akt 抑制劑庫凋亡分子化合物庫細(xì)胞周期化合物庫 NF-κB信號(hào)通路庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

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

體外研究(In Vitro)
體外研究活性	Triciribine的劑量為1-10 μM時(shí)生長抑制的效果最佳。像dosnstream p70S6K一樣Triciribine基本在100μM (IC50 = 130 nM)時(shí)可以抑制Akt的磷酸化作用。Triciribine抑制Nf1和Trp53突變的腫瘤星型細(xì)胞的生長，這種抑制具有梯度依賴的特性。Triciribine在GI50為1.7 μM時(shí)并不能完全抑制（最高可抑制率為69%）WHO II K1861-10系的生長，而對(duì)于更高級(jí)的腫瘤系(KR158, KR130, and SF295), Triciribine可以在更低的GI50值(0.4–1.1 mM)時(shí)產(chǎn)生更廣泛的抑制（最高抑制率>80%）。重要的是Triciribine能特異性地抑制腫瘤細(xì)胞而對(duì)大多數(shù)普通的星形膠質(zhì)細(xì)胞抑制效率很低(GI50?13.6 mM) ^[1]。Triciribine能抑制HIV-1， IC50為20 nM。用量為0.1μM時(shí)能產(chǎn)生>90%的抑制率，用量為5μM時(shí)能完全抑制多核體的形成。在相同的細(xì)胞系中相關(guān)的細(xì)胞毒性實(shí)驗(yàn)結(jié)果顯示當(dāng) Triciribine 濃度為46 μM時(shí)的選擇性指數(shù)為2250. 利用HIV-1急性感染的CEM-SS, h9, 和持續(xù)感染的H9III _B 和 U1 細(xì)胞研究發(fā)現(xiàn)， Triciribine 可以顯著的抑制HIV-1誘導(dǎo)的 p24 核心抗原的產(chǎn)生, 反轉(zhuǎn)錄酶和傳染性病毒的產(chǎn)生，這種抑制具有劑量依賴的特性^[2]。 Triciribine會(huì)抑制人前列腺癌PC-3 細(xì)胞系中的Akt 308位的酸酸和473位絲氨酸的磷酸化以及Akt 的活性. Triciribine使PC-3 細(xì)胞對(duì)于TRAIL- 和 anti-CD95誘導(dǎo)的細(xì)胞凋亡更加敏感, 但是對(duì)于能引起DNA損傷的化療依然具有抗性^[3]。Triciribine 對(duì)于Akt具有高度的選擇性，并不會(huì)抑制其它激酶的激活，如磷脂酰肌醇3激酶, 磷酸肌醇依賴的激酶1, 蛋白激酶C, serumand 糖皮質(zhì)激素誘導(dǎo)激酶, 蛋白激酶 A, 信號(hào)傳感器和轉(zhuǎn)錄3 活化劑, 胞外信號(hào)調(diào)節(jié)激酶1/2或者c-Jun NH2-末端激酶^[4]。
激酶實(shí)驗(yàn)	Akt磷酸化改變分析
激酶實(shí)驗(yàn)	待細(xì)胞生長到全板80%–90%，加入1–10 ng/mL表皮生長因子(EGF; cat #01-107)或血小板生長因子(PDGF)–AA (cat #01-309) (Upstate Biotechnology)加入或者不加 10–20 mM的 U0126 (cat #EI-282) 或 LY-294002 (cat #ST-420) (Biomol Research Lab)刺激細(xì)胞5到10分鐘。用12%–15% SDS PAGE分離5–20 μg蛋白裂解液，用Akt (cat #cs-9272), 磷酸化的 Akt (磷酸絲氨酸 473; cat #cs-9271), MAPK (cat #cs-9102)和磷酸化 MAPK (p44/42 磷酸蘇氨酸202/Tyr204; cat #cs-01-9101)抗體1:1000稀釋（Cell Signaling Technology)蛋白印跡檢測(cè)蛋白裂解物。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	CEM-SS 細(xì)胞
	濃度	0-500 μM
	孵育時(shí)間	48小時(shí)
	方法	將 CEM-SS細(xì)胞按1萬個(gè)每孔的密度接種在96孔平板中并在生長培養(yǎng)基中培養(yǎng)，用上述細(xì)胞對(duì)triciribine的細(xì)胞毒性進(jìn)行分析評(píng)定. 將連續(xù)稀釋5倍的不同濃度的Triciribine加到細(xì)胞中. 37℃孵育48小時(shí), 通過電轉(zhuǎn)將細(xì)胞用含有放射性同位素³H的 dThd (1 μCi 每孔, 放射性比度為20 Ci/mmol)標(biāo)記6小時(shí)，收取細(xì)胞并測(cè)定總的DNA合成量
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	PMID
	Western blot	PUMA / p-FoxO3a / p-AKT		20978166
	Immunofluorescence	TRF2 / 53BP1		23862686

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	Riciribine按照 1 mg/kg/天的劑量對(duì)裸小鼠腹腔注射，可以抑制 OVCAR3, OVCAR8 和 PANC1 腫瘤的生長, 分別使Akt過量表達(dá)了90%, 88% 和80%。然而, Triciribine 對(duì)OVCAR5 和 COLO357細(xì)胞的生長基本沒有影響^[4]。
動(dòng)物實(shí)驗(yàn)	Animal Models	皮下注射OVCAR3, OVCAR8, PANC1, OVCAR5和 COLO357 腫瘤細(xì)胞的80周齡雌性裸小鼠.
	Dosages	1 mg/kg/天
	Administration	腹腔注射，一天一次.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻(xiàn)
[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

參考文獻(xiàn)

[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

化學(xué)信息&溶解度

分子量	320.3	分子式	C₁₃H₁₆N₆O₄
CAS號(hào)	35943-35-2	SDF	Download Triciribine (API-2) SDF
Smiles	CN1C2=NC=NC3=C2C(=CN3C4C(C(C(O4)CO)O)O)C(=N1)N
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 64 mg/mL ( (199.81 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 16 mg/mL (49.95 mM)

Water : Insoluble

DMSO : 64 mg/mL ( (199.81 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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* 必填項(xiàng)

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):

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