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KU-0063794

KU-0063794是一種有效的，高度特異性的，作用于mTORC1和mTORC2的雙重mTOR抑制劑，在無細胞試驗中IC50約為~10 nM；對PI3Ks沒有作用。

KU-0063794 Chemical Structure

KU-0063794 Chemical Structure

CAS: 938440-64-3

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1464.74 現(xiàn)貨
5mg 727.74 現(xiàn)貨
10mg 1970 現(xiàn)貨
50mg 3857.09 現(xiàn)貨
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KU-0063794相關產品

相關信號通路圖

mTOR Signaling Pathways

mTOR信號通路圖

細胞實驗數(shù)據示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
H1650 Function Assay 7.61 nM 72 h inhibits phosphorylation of p70S6K 23874880
PC9GR Function Assay 6.21 nM 72 h inhibits phosphorylation of p70S6K 23874880
PC9 Function Assay 10.15 nM 72 h inhibits phosphorylation of p70S6K 23874880
H1975 Function Assay 11.15 nM 72 h inhibits mTOR phosphorylation status? 23874880
H1650 Function Assay 7.61 nM 72 h inhibits mTOR phosphorylation status? 23874880
PC9GR Function Assay 6.21 nM 72 h inhibits mTOR phosphorylation status? 23874880
PC9 Function Assay 10.15 nM 72 h inhibits mTOR phosphorylation status? 23874880
HepG3? Function Assay 0.1–50?μM 48 h induces cell autophagy in a dose dependent manner 26278819
HepG2? Function Assay 0.1–50?μM 24 h induces p62 downregulation, Beclin-1 expression and LC3B-I to LC3B-II conversion in a dose dependent manner 26278819
HepG2? Function Assay 5/10 μM 24 h downregulates the levels HIF1α and cyclin D1? 26278819
HepG2? Function Assay 5/10 μM 24 h dramatically inhibits phosphorylation of AKT at Ser-473 26278819
HepG2? Apoptosis Assay 0.1–50?μM 48 h induces apoptosis in a dose dependent manner 26278819
HepG2? Colony Formation Assay 1–50?μM 10 d decreases the number of viable HepG2 colonies?significantly 26278819
HepG2? Cell Viability Assay 0.1–50?μM 72 h decreases cell viability in a dose dependent manner 26278819
H1975 Function Assay 11.15 nM 72 h inhibits phosphorylation of p70S6K 23874880
LNCaP Cell Viability Assay 0-10 μM 24 h? decreases cell viability in a dose dependent manner 23840605
PC-3 Cell Viability Assay 0-10 μM 24 h? decreases cell viability in a dose dependent manner 23840605
MDA-MB-468? Cell Viability Assay 0-10 μM 24 h? decreases cell viability in a dose dependent manner 23840605
LNCaP Function Assay 200–800 nM 24 h? decreases the phosphorylation level of p70S6K in a dose dependent manner 23840605
PC-3 Function Assay 200–800 nM 24 h? decreases the phosphorylation level of p70S6K in a dose dependent manner 23840605
MDA-MB-468? Function Assay 200–800 nM 24 h? decreases the phosphorylation level of p70S6K in a dose dependent manner 23840605
Caki-1? Function Assay 100-2000 nM 10-180 min inhibits both mTORC1 and mTORC2 as indicated by the decrease in phosphorylation of downstream effectors 23349989
786-O Function Assay 100-2000 nM 10-180 min inhibits both mTORC1 and mTORC2 as indicated by the decrease in phosphorylation of downstream effectors 23349989
Caki-1? Cell Viability Assay 300-4000 nM 24-96 h suppresses the cell viability in both time and dose dependent manner 23349989
786-O Cell Viability Assay 300-4000 nM 24-96 h suppresses the cell viability in both time and dose dependent manner 23349989
Caki-1? Function Assay 2 μM 72 h induces G1 cell cycle arrest and autophagy 23349989
786-O Function Assay 2 μM 72 h induces G1 cell cycle arrest and autophagy 23349989
HBCx-10 Function assay 5 mg/kg Potentiation of irinotecan-induced tumor regression against human HBCx-10 cells xenografted in immunocompromised mouse at 5 mg/kg, po qd administered on days 1 to 3 of weekly cycle 19762236
PC3 Function assay 100 mg/kg Inhibition of Akt phosphorylation at Ser473 in PTEN-deficient human PC3 cells xenograft mouse model at 100 mg/kg, po single dose measured up to 8 hrs 29211480
PC3 Antitumor assay 30 mg/kg Antitumor activity against human PC3 cells xenograft mouse model assessed as inhibition of tumor growth at 30 mg/kg, po bid in presence of 1-aminobenzotriazole 29211480
PC3 Antitumor assay 60 mg/kg Antitumor activity against human PC3 cells xenograft mouse model assessed as inhibition of tumor growth at 60 mg/kg, po bid in presence of 1-aminobenzotriazole 29211480
SW620 Function assay 20 mg/kg Potentiation of irinotecan-induced tumor regression against human SW620 cells xenografted in immunocompromised mouse at 20 mg/kg, po qd administered on days 2 to 4 of weekly cycle 29211480
H1975 Growth Inhibition Assay 72 h IC50=11.15±0.93 nM 23874880
H1650 Growth Inhibition Assay 72 h IC50=7.61±0.62 nM 23874880
PC9GR Growth Inhibition Assay 72 h IC50=6.21±1.30 nM 23874880
PC9 Growth Inhibition Assay 72 h IC50=10.15±0.62 nM 23874880
HEK293 Function assay 2 hrs Inhibition of recombinant FLAG-tagged mTOR expressed in HEK293 cells using biotinylated p70S6K substrate after 2 hrs by alphascreen competition assay, IC50=0.003μM 19762236
U87MG Function assay 2 hrs Inhibition of mTORC1 in human U87MG cells assessed as phosphorylated S6 ribosomal protein (Ser235/236) level after 2 hrs by Western blotting, IC50=0.1μM 19762236
U87MG Function assay 2 hrs Inhibition of mTORC2 in human U87MG cells assessed as phosphorylated AKT (Ser473) level after 2 hrs by Western blotting, IC50=0.15μM 19762236
T47D Antiproliferative assay 120 hrs Antiproliferative activity against human T47D cells after 120 hrs by SRB assay, GI50=0.35μM 19762236
MDA-MB-468 Function assay 2 hrs Inhibition of mTORC2 in human MDA-MB-468 cells assessed as reduction of AKT phosphorylation at Ser473 after 2 hrs, IC50=0.24μM 23375793
MDA-MB-468 Function assay 2 hrs Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction of pS6 phosphorylation at Ser235/236 after 2 hrs, IC50=0.66μM 23375793
HEK293 Function assay 30 mins Inhibition of mTORC1 in HEK293 cells using GST-tagged S6K1 or Akt1 as substrate after 30 mins by immunoblotting assay, IC50=0.01μM 29211480
HEK293 Function assay 30 mins Inhibition of mTORC2 in HEK293 cells using GST-tagged S6K1 or Akt1 as substrate after 30 mins by immunoblotting assay, IC50=0.01μM 29211480
NUGC4 Growth Inhibition Assay IC50=2.93 ± 0.31 μM 24597478
MKN45 Growth Inhibition Assay IC50=0.82 ± 0.01 μM 24597478
HGC27 Growth Inhibition Assay IC50=15.0 ± 4.82 μM 24597478
AGS Growth Inhibition Assay IC50=15.0 ± 2.91 μM 24597478
HEK293 Function assay Inhibition of recombinant FLAG-tagged mTOR (1362 to 2549) (unknown origin) expressed in HEK293 cells, IC50=0.0025μM 23375793
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
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 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
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 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
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD 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
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
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生物活性

產品描述 KU-0063794是一種有效的，高度特異性的，作用于mTORC1和mTORC2的雙重mTOR抑制劑，在無細胞試驗中IC50約為~10 nM；對PI3Ks沒有作用。
靶點
mTORC1 [1]
(Cell-free assay)		 mTORC2 [1]
(Cell-free assay)
~10 nM ~10 nM
體外研究(In Vitro)
體外研究活性

與mTOR抑制劑PP242相比, KU-0063794高特異性作用于mTOR,而對PI3Ks或其他76種激酶則無作用活性。30 nM KU-0063794作用于HEK-293細胞，通過抑制疏水基團(Thr389)磷酸化，及隨后的T-環(huán)殘基(Thr229) 磷酸化，而快速切除S6K1活性。300 nM KU-0063794作用于IGF1刺激的血清饑餓處理的 HEK-293細胞，抑制~90%S6K1活性。KU-0063794 為 100-300 nM時，也完全抑制氨基酸誘導的S6K1和 S6蛋白磷酸化。與S6K1類似, KU-0063794抑制mTORC1在 Ser2448位點磷酸化，也抑制mTORC2 在 Ser22481 位點磷酸化，這種作用存在劑量和時間依賴性。在血清存在時，或者IGF1刺激的情況下, KU-0063794抑制Akt 活性，或者Akt在 Ser473和 Thr308（意外的）位點磷酸化，也抑制Akt底物 PRAS40 在 Thr246位點，GSK3α/GSK3β在 Ser21/Ser9位點及Foxo-1/3a 在 Thr24/Thr32位點磷酸化，以上作用存在劑量依賴性。KU-0063794而不是 Rapamycin 抑制SGK1活性和 在Ser422位點磷酸化，也抑制其生理底物NDGR1，與抑制S6K1 和Akt磷酸化程度相似，這種作用存在劑量依賴性，然而KU-0063794 不抑制佛波酯誘導的ERK 或RSK磷酸化和RSK激活。與Rapamycin相比, KU-0063794更有效誘導4E-BP1在 Thr37, Thr46和 Ser65位點完全去磷酸化。KU-0063794抑制野生型和mLST8-缺陷型MEFs細胞生長，也誘導細胞周期停在G1期，比Rapamycin效果更顯著。[1]
激酶實驗 mTOR 復合物激酶檢測實驗
HEK-293細胞新鮮溶解在Hepes裂解液中。溶解產物(1-4 mg) 通過與5-20 μL G蛋白的瓊脂糖凝膠結合免疫前抗體IgG溫育而預先清除。裂解抽提物與5-20 μL G蛋白的瓊脂糖凝膠結合的 5-20 μg抗Rictor或抗Raptor抗體的 免疫前抗體IgG溫育。所有抗體共價結合到蛋白G蛋白瓊脂糖凝膠上。在振動轉載臺上4oC下進行 免疫沉淀1小時。使用Hepes 裂解液沖洗免疫沉淀物四次，隨后使用Hepes激酶buffer沖洗兩次。使用 Raptor免疫沉淀物磷酸化 S6K1, 兩次沖洗的初始步驟中，buffer 含0.5 M NaCl，確保最佳激酶活性。血清饑餓的 HEK-293細胞中分離的GST-Akt1與PI-103(1 μM 進行 1 小時)溫育。從血清饑餓的HEK-293 細胞中純化的GST-S6K1與Rapamycin (0.1 μM進行1小時)溫育。加入0.1 mM ATP和 10 mM MgCl2 ，在不同濃度KU-0063794和GST-Akt1 (0.5 μg)或GST-S6K1 (0.5 μg)存在時，開始mTOR反應。反應在 30oC下在振動轉載臺上進行30分鐘，然后加入SDS樣本緩沖液終止反應。反應混合物在0.22-μm-孔徑大小 Spin-X過濾器上過濾，樣本進行電泳處理，然后使用指定抗體進行免疫印跡分析。
細胞實驗 細胞系 野生型和mLST8缺陷型MEFs
濃度 溶于DMSO,終濃度為~3 μM
孵育時間 24, 48, 和72 小時
方法

使用KU-0063794 處理細胞 24, 48, 和72 小時，每24小時更換一次培養(yǎng)基，加入新鮮溶解的KU-0063794。為了測量細胞生長，使用PBS沖洗細胞一次，然后與4% (v/v) 多聚甲醛在 PBS混合15分鐘。用水沖洗一次后，使用溶于 10% 乙醇的0.1% 結晶紫對細胞染色20分鐘，然后用水沖洗三次。 使用0.5 mL 10% (v/v) 乙酸從細胞中抽提結晶紫20分鐘。然后洗脫液在水中按1:10稀釋，然后在 590 nm 處測量吸光值。為了測量細胞周期分布，通過胰蛋白酶化作用收集細胞，然后在PBS中沖洗一次，再懸浮于冰凍70% (v/v)乙醇中。細胞在 PBS和 1% (w/v) BSA中沖洗兩次，再在 PBS 和含 50 g/mL 碘化丙啶和 50 g/mL RNase A的0.1% (v/v) Triton X-100中染色 20分鐘。使用FACSCalibur流式細胞儀和CellQuest軟件檢測細胞中DNA含量。在線性標度上測量紅色熒光(585 nm)，進行脈沖寬度分析用于排除雙峰值。使用FlowJo軟件測定細胞周期分布。
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot p-S6K / S6K / p-4E-BP1 / E7 / E6 / p53 p-mTOR 28115701
體內研究(In Vivo)
體內研究活性

Ku0063794在腎臟上皮腎細胞癌的臨床前模型中，抑制腫瘤生長和mTOR信號[2]。
動物實驗 Animal Models Nu/Nu裸鼠
Dosages 8 mg/kg
Administration i.p.

化學信息&溶解度

分子量 465.54 分子式

C25H31N5O4
CAS號 938440-64-3 SDF Download KU-0063794 SDF
Smiles CC1CN(CC(O1)C)C2=NC3=C(C=CC(=N3)C4=CC(=C(C=C4)OC)CO)C(=N2)N5CCOCC5
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 16 mg/mL ( (34.36 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 5 mg/mL (10.74 mM)

Water : Insoluble

摩爾濃度計算器

體內溶解度
批次：

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

 動物體內配方計算器

實驗計算

摩爾濃度計算器

質量 濃度 體積 分子量

動物體內配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

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

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

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，請先聯(lián)系Selleck）；

體內配方配制方法：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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