- 抑制劑
- 研究領(lǐng)域
- PI3K/Akt/mTOR信號(hào)通路
- 表觀遺傳
- 甲基化
- 免疫&炎癥
- 酪氨酸蛋白激酶
- 血管生成
- 凋亡
- 自噬
- 內(nèi)質(zhì)網(wǎng)應(yīng)激&UPR響應(yīng)
- JAK/STAT信號(hào)通路
- MAPK信號(hào)通路
- 細(xì)胞骨架
- 細(xì)胞周期
- TGF-beta/Smad信號(hào)通路
- DNA損傷/DNA修復(fù)
- 化合物庫(kù)
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細(xì)胞核與細(xì)胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲(chǔ)液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
- 動(dòng)物實(shí)驗(yàn)
- 鼠尾直接PCR試劑盒(快速基因型鑒定)
- 小鼠CD3+ T細(xì)胞分選試劑盒
- 小鼠CD4+ T細(xì)胞分選試劑盒
- 小鼠CD8+ T細(xì)胞分選試劑盒
- 新產(chǎn)品
- 聯(lián)系我們
A-674563 HCl
A-674563 HCl 是一種Akt抑制劑，在無(wú)細(xì)胞試驗(yàn)中Ki為11 nM，對(duì)PKA適度有效，作用于Akt1比作用于PKC選擇性高30多倍。
A-674563 HCl Chemical Structure
CAS: 2070009-66-2
產(chǎn)品質(zhì)控
批次：
純度：
99.66%
99.66
A-674563 HCl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 Dihydrochloride Perifosine SC79 Capivasertib (AZD5363) GSK690693 Ipatasertib (GDC-0068) Triciribine (API-2) CCT128930 Afuresertib (GSK2110183) AT7867 Oridonin Akti-1/2 PHT-427 TIC10 (ONC201) AT13148 Miransertib (ARQ 092) HCl Uprosertib (GSK2141795) Miransertib (ARQ-092) SC66 Deguelin ML-9 HCl | 點(diǎn)擊展開 |
| 相關(guān)化合物庫(kù) | 激酶抑制劑庫(kù) PI3K/Akt 抑制劑庫(kù) 凋亡分子化合物庫(kù) 細(xì)胞周期化合物庫(kù) NF-κB信號(hào)通路庫(kù) | 點(diǎn)擊展開 |
相關(guān)信號(hào)通路圖
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(PMID) |
|---|---|---|---|---|---|
| MIA PaCa cells | Cytotoxic?assay | Cytotoxicity against human MIA PaCa cells by MTT assay, EC50=0.64 μM | 17523610 | ||
| MiaPaCa2 cell | Proliferation assay | Antiproliferative activity against human MiaPaCa2 cell line, EC50=0.4 μM | 16678413 | ||
| MOLM14 | Cytotoxicity assay | Cytotoxicity against human MOLM14 cells, EC50=0.06μM. | 31207462 | ||
| MV4-11 | Cytotoxicity assay | Cytotoxicity against human MV4-11 cells, EC50=0.092μM. | 31207462 | ||
| MOLM13 | Cytotoxicity assay | Cytotoxicity against human MOLM13 cells, EC50=0.17μM. | 31207462 | ||
| KB-3-1 | Function assay | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 31515284 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 31515284 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 31515284 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | A-674563 HCl 是一種Akt抑制劑，在無(wú)細(xì)胞試驗(yàn)中Ki為11 nM，對(duì)PKA適度有效，作用于Akt1比作用于PKC選擇性高30多倍。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | 口服生物活性化合物(用苯基取代A-443654的吲哚基得到)，比A-443654對(duì)Akt的選擇性差。 | |||||||||||
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | A-674563 HCl 是A-443654上的吲哚基被苯基取代的產(chǎn)物，具有口服活性。A-674563減慢腫瘤細(xì)胞的增殖，EC50為0.4 μM。[1] A-674563自身不會(huì)抑制Akt磷酸化，但是會(huì)劑量依賴性阻斷Akt下游靶點(diǎn)的磷酸化。A-674563誘導(dǎo)的Akt阻塞會(huì)導(dǎo)致STS細(xì)胞下游靶點(diǎn)磷酸化下降和腫瘤細(xì)胞的生長(zhǎng)抑制。A-674563誘導(dǎo)STS 細(xì)胞中G2細(xì)胞周期阻滯和細(xì)胞凋亡。[2] |
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|---|---|---|---|---|
| 激酶實(shí)驗(yàn) | Akt激酶試驗(yàn) | |||
| 激酶試驗(yàn)使用His-Akt1和生物素化的小鼠Bad多肽作為底物。激酶試驗(yàn)在室溫下，50 μL反應(yīng)緩沖液[20 mM HEPES，pH 7.5，10 mM MgCl2，0.1% (w/v) Triton X-100，5 μM ATP (Km = 40 μM)，5 μM 多肽(Km = 15 μM)，1 mM DTT，60 ng Akt1，和0.5 μCi of [γ-33P]ATP]中，不同濃度A-674563存在下進(jìn)行30分鐘。每個(gè)反應(yīng)通過(guò)加入50 μL終止緩沖液(0.1 M EDTA，pH 8.0，和4 M NaCl)停止。生物素化的Bad多肽固定在鏈霉親和素包被的FLASH平板。用PBS-Tween 20 (0.05%)清洗后，F(xiàn)LASH 板上捕獲的33P磷酸肽通過(guò)TopCount Packard Instruments γ計(jì)數(shù)器測(cè)量。 | ||||
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | MiaPaCa-2 細(xì)胞 | ||
| 濃度 | 0-30 μM | |||
| 孵育時(shí)間 | 48小時(shí) | |||
| 方法 | 將96孔板上的細(xì)胞用200 μL PBS緩慢清洗。Alamar Blue試劑以1:10在正常生長(zhǎng)培養(yǎng)基中稀釋。將稀釋的Alamar Blue(100 M)加入到96孔板的每孔中，依據(jù)制造商的說(shuō)明培養(yǎng)到反應(yīng)完全。使用fmax熒光酶標(biāo)儀進(jìn)行分析，激發(fā)波長(zhǎng)設(shè)置為544 nm，發(fā)射波長(zhǎng)設(shè)置為595 nm。數(shù)據(jù)使用制造商提供的SOFTmax PRO軟件分析。 |
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| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | A-674563單一療法沒(méi)有顯著的腫瘤抑制活性；與單獨(dú)療法相比，結(jié)合療法的效能被顯著提高。[1] A674563-處理的(20 mg/kg/bid, p.o.)小鼠體內(nèi)腫瘤生長(zhǎng)減慢，腫瘤體積減少50%，在研究結(jié)束時(shí)，與對(duì)照組相比。[2] A-674563被認(rèn)為顯著地提高了PK性能，在小鼠體內(nèi)口服生物活性為67%，但是比A-443654的活性低70倍。[3] |
|
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | 禁食小鼠 |
| Dosages | 20 或 100 mg/kg | |
| Administration | 1 g/kg葡萄糖刺激前30分鐘給藥A-674563 | |
|
化學(xué)信息&溶解度
| 分子量 | 394.9 | 分子式 | C22H22N4O.CIH |
| CAS號(hào) | 2070009-66-2 | SDF | -- |
| Smiles | CC1=C2C=C(C=CC2=NN1)C3=CC(=CN=C3)OCC(CC4=CC=CC=C4)N | ||
| 儲(chǔ)存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 72 mg/mL ( (182.32 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO) Water : 72 mg/mL (182.32 mM) Ethanol : 18 mg/mL (45.58 mM) |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解配方 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
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(guò)程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
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(guò)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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