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PI3K/Akt/mTOR
mTOR inhibitor
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Torkinib (PP242)
僅限科研使用
Torkinib (PP242)
Torkinib (PP242) 是一種選擇性的mTOR抑制劑，在無細胞試驗中IC50為8 nM；靶向作用于mTOR復(fù)合體，作用于mTOR比作用于PI3Kδ或PI3Kα/β/γ選擇性分別高10倍多和100倍。Torkinib (PP242) 可誘導(dǎo)線粒體自噬和凋亡。
Torkinib (PP242) Chemical Structure
CAS: 1092351-67-1
產(chǎn)品質(zhì)控
批次：
純度：
99.50%
99.50
Torkinib (PP242)相關(guān)產(chǎn)品
| 相關(guān)靶點 | mTORC1 mTORC2 | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | AZD8055 Torin 1 Ridaforolimus (Deforolimus, MK-8669) Sapanisertib (MLN0128) Vistusertib (AZD2014) MHY1485 KU-0063794 Torin 2 OSI-027 WYE-354 WYE-125132 (WYE-132) 3BDO Palomid 529 (P529) Zotarolimus (ABT-578) Salidroside WAY-600 GDC-0349 Onatasertib (CC 223) WYE-687 XL388 | 點擊展開 |
| 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 細胞周期化合物庫 NF-κB信號通路庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)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(PMID) |
|---|---|---|---|---|---|
| HT-p21 | Function Assay | 50-1250 nM | 24 h | inhibits phosphorylation of S6 kinase (target of mTORC1) and its downstream target phospho-S6? | |
| U87vIII? | Function Assay | 0.04-2.5 μM | 24 h | inhibits mTORC1 and mTORC2 activities? | |
| U87vIII? | Function Assay | 2.5/5 μM | 12 h | inhibits gap closing in a dose-dependent manner | |
| 3T3-L1 | Function Assay | 15 μM | 4 h | suppresses expression of the Egr1 protein? | |
| Rh30 | Function Assay | 1 μM | 2 h | inhibits both mTORC1-mediated phosphorylation of S6K1 and mTORC2-mediated phosphorylation of Akt | |
| HT29 | Function Assay | 1 μM | 2 h | inhibits both mTORC1-mediated phosphorylation of S6K1 and mTORC2-mediated phosphorylation of Akt | |
| Rh30 | Function Assay | 1 μM | 2 h | suppresses the basal or IGF-1-stimulated cell adhesion | |
| HT29 | Function Assay | 1 μM | 2 h | suppresses the basal or IGF-1-stimulated cell adhesion | |
| U87 | Growth Inhibition Assay | 25 nM | 24 h | increases DUSP10 knocked-down induced cell inhibition | |
| AGS | Cell Viability Assay | 0-1000 nM | 24/48 h | decreases cell viability in time and dose dependent manner | |
| MKN45 | Cell Viability Assay | 0-1000 nM | 24/48 h | decreases cell viability in time and dose dependent manner | |
| MKN28 | Cell Viability Assay | 0-1000 nM | 24/48 h | decreases cell viability in time and dose dependent manner | |
| KATO3 | Cell Viability Assay | 0-1000 nM | 24/48 h | decreases cell viability in time and dose dependent manner | |
| SGC7901 | Cell Viability Assay | 0-1000 nM | 24/48 h | decreases cell viability in time and dose dependent manner | |
| N87 | Cell Viability Assay | 0-1000 nM | 24/48 h | decreases cell viability in time and dose dependent manner | |
| HMEC | Cell Viability Assay | 0-1000 nM | 24/48 h | decreases cell viability in time and dose dependent manner | |
| HUVEC | Cell Viability Assay | 0-1000 nM | 24/48 h | decreases cell viability in time and dose dependent manner | |
| MG63 | Function Assay | 50-1000 nM | 0.5 h | dose dependently (50–1000 nM) inhibits phosphorylation of Akt | |
| U2OS? | Function Assay | 50-1000 nM | 0.5 h | dose dependently (50–1000 nM) inhibits phosphorylation of Akt | |
| Saos-2? | Function Assay | 50-1000 nM | 0.5 h | dose dependently (50–1000 nM) inhibits phosphorylation of Akt | |
| Saos-2 | Function Assay | 100 nM | 0.5 h | prevents osteosarcoma cell migration | |
| MG63 | Apoptosis Assay | 100 nM | 36 h | promotes apoptosis | |
| U2OS? | Apoptosis Assay | 100 nM | 36 h | promotes apoptosis | |
| Saos-2? | Apoptosis Assay | 100 nM | 36 h | promotes apoptosis | |
| DLD-1 | Cell Viability Assay | 0-1000 nM | 24 h | inhibits the growth in a dose-dependent manner | |
| Caco2 | Cell Viability Assay | 0-1000 nM | 24 h | inhibits the growth in a dose-dependent manner | |
| HT29 | Cell Viability Assay | 0-1000 nM | 24 h | inhibits the growth in a dose-dependent manner | |
| H116 | Cell Viability Assay | 0-1000 nM | 24 h | inhibits the growth in a dose-dependent manner | |
| Hct-8 | Cell Viability Assay | 0-1000 nM | 24 h | inhibits the growth in a dose-dependent manner | |
| Colo320 | Cell Viability Assay | 0-1000 nM | 24 h | inhibits the growth in a dose-dependent manner | |
| Sw948 | Cell Viability Assay | 0-1000 nM | 24 h | inhibits the growth in a dose-dependent manner | |
| Colo205 | Cell Viability Assay | 0-1000 nM | 24 h | inhibits the growth in a dose-dependent manner | |
| Colo320 | Function Assay | 1 μM | 0-24 h | abolishes the S6S235/236?but partially reduces the 4E-BP1T36/45 | |
| HT29 | Function Assay | 1 μM | 0-24 h | abolishes the S6S235/236?but partially reduces the 4E-BP1T36/45 | |
| Sw948 | Function Assay | 1 μM | 0-24 h | abolishes the S6S235/236?but partially reduces the 4E-BP1T36/45 | |
| DLD-1 | Function Assay | 1 μM | 0-24 h | abolishes the S6S235/236?but partially reduces the 4E-BP1T36/45 | |
| 786-O | Function Assay | 0.1/0.5 μM | 24 h | increases E-cadherin mRNA levels dose dependently | |
| 786-O | Function Assay | 0-0.5 μM | 24 h | results in a dose dependent increase in E-cadherin protein expression? | |
| OCI-AML3 | Apoptosis Assay | 2.5 μM | 72 h | induces apoptosis | |
| Jurkat | Function Assay | 100/200/400 nM | 18 h | inhibits mTORC1-dependent S6 S235/236 phosphorylation | |
| p210 BCR-Abl | Function Assay | 100/200/400 nM | 18 h | inhibits mTORC1-dependent S6 S235/236 phosphorylation | |
| Jurkat | Growth Inhibition Assay | 400nM | 24/48 h | synergize with 17-AAG to suppress cell proliferation | |
| p210 BCR-Abl | Growth Inhibition Assay | 400nM | 24/48 h | synergize with 17-AAG to suppress cell proliferation | |
| 8226 | Function Assay | 100-1000 nM | 30 min | activates ERK? | |
| MM1.S? | Function Assay | 100-1000 nM | 30 min | activates ERK? | |
| 8226 | Function Assay | 0.5 μM | 30 min | induces activation of RAF and phosphorylation of MEK | |
| MM1.S? | Function Assay | 0.5 μM | 30 min | induces activation of RAF and phosphorylation of MEK | |
| MCF-7 | Function Assay | 50/200/500 nM | 30 min | dose-dependently (50–500?nM) suppresses phosphorylation of Akt | |
| T47D | Function Assay | 50/200/500 nM | 30 min | dose-dependently (50–500?nM) suppresses phosphorylation of Akt | |
| MDA-MB-231 | Function Assay | 50/200/500 nM | 30 min | dose-dependently (50–500?nM) suppresses phosphorylation of Akt | |
| Bcap-37 | Function Assay | 50/200/500 nM | 30 min | dose-dependently (50–500?nM) suppresses phosphorylation of Akt | |
| MCF-7 | Apoptosis Assay | 200?nM | 36 h | induces apoptosis | |
| MDA-MB-231 | Apoptosis Assay | 200?nM | 36 h | induces apoptosis | |
| Bcap-37 | Apoptosis Assay | 200?nM | 36 h | induces apoptosis | |
| LS174T | Function Assay | 10/100/1000 nM | 6 h | inhibits mTORC1 activity by the dephosphorylation of S6 ribosomal protein | |
| DLD-1? | Function Assay | 10/100/1000 nM | 6 h | inhibits mTORC1 activity by the dephosphorylation of S6 ribosomal protein | |
| SW480 | Function Assay | 10/100/1000 nM | 6 h | inhibits mTORC1 activity by the dephosphorylation of S6 ribosomal protein | |
| NIH 3T3 | Function Assay | 2 μM | 18 h | inhibits mTORC2 phosphorylation of Akt on Ser473 and mTORC1 phosphorylation of 4E-BP1 on Thr37/46 | |
| HCT15 | Function Assay | 0.5/2 μM | 4 h | prevents S6K1 phosphorylation of ribosomal protein S6 at Ser240/244 and mTORC2 phosphorylation of Akt at Ser473 | |
| SW620? | Function Assay | 0.5/2 μM | 4 h | blocks all three mTOR outputs | |
| PC12? | Function Assay | 40?nM | induces lysosomal biogenesis and alleviated α-SYN accumulation? | ||
| DND-1 | Growth Inhibition Assay | 0.25/0.5/1 μM | inhibits cell growth dose dependently | ||
| TMD8 | Growth Inhibition Assay | 0.25/0.5/1 μM | inhibits cell growth dose dependently | ||
| Jurkat | Growth Inhibition Assay | 0.25/0.5/1 μM | inhibits cell growth dose dependently | ||
| KOPT-K1 | Growth Inhibition Assay | 0.25/0.5/1 μM | inhibits cell growth dose dependently | ||
| TMD7 | Growth Inhibition Assay | 0.25/0.5/1 μM | inhibits cell growth dose dependently | ||
| THP-1 | Growth Inhibition Assay | 0.25/0.5/1 μM | inhibits cell growth dose dependently | ||
| HT1376 | Growth Inhibition Assay | IC50=1.88 ± 1.1 μM | |||
| T24 | Growth Inhibition Assay | IC50=1.37 ± 0.4 μM | |||
| UM-UC-3 | Growth Inhibition Assay | IC50=0.63 ±0.1 μM | |||
| SW620 | Growth Inhibition Assay | IC50=7.8 μM | |||
| SW480 | Growth Inhibition Assay | IC50=4.6 μM | |||
| SK-CO-1 | Growth Inhibition Assay | IC50=4 μM | |||
| LS-513 | Growth Inhibition Assay | IC50=3.9 μM | |||
| SW1116 | Growth Inhibition Assay | IC50=0.84 μM | |||
| LS-174T | Growth Inhibition Assay | IC50=0.84 μM | |||
| HCT 116 | Growth Inhibition Assay | IC50=0.41 μM | |||
| HCT 15 | Growth Inhibition Assay | IC50=0.3 μM | |||
| COLO 205 | Growth Inhibition Assay | IC50=0.24 μM | |||
| HT-29 | Growth Inhibition Assay | IC50=0.23 μM | |||
| COLO 201 | Growth Inhibition Assay | IC50=0.23 μM | |||
| Caco-2 | Growth Inhibition Assay | IC50=0.22 μM | |||
| SW48 | Growth Inhibition Assay | IC50=0.09 μM | |||
| SW-48 | Growth Inhibition Assay | IC50=0.1 μM | |||
| HCT-15 | Growth Inhibition Assay | IC50=0.3 μM | |||
| HCT 116 | Growth Inhibition Assay | IC50=0.6 μM | |||
| SW620-R | Growth Inhibition Assay | IC50=1.3 μM | |||
| SK-CO-1 | Growth Inhibition Assay | IC50=2.1 μM | |||
| SW620 | Growth Inhibition Assay | IC50=11 μM | |||
| BaF3 | Growth Inhibition Assay | GI50=1.449 μM | |||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Torkinib (PP242) 是一種選擇性的mTOR抑制劑，在無細胞試驗中IC50為8 nM；靶向作用于mTOR復(fù)合體，作用于mTOR比作用于PI3Kδ或PI3Kα/β/γ選擇性分別高10倍多和100倍。Torkinib (PP242) 可誘導(dǎo)線粒體自噬和凋亡。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 特性 | 第一批以mTOR的ATP域為靶點的選擇性抑制劑之一。 | ||||||||
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | PP242作用于mTOR比作用于其他PI3K家族激酶，比如p110α，p110β，p110γ，p110δ，和DNA-PK(IC50分別為1.96 μM，2.2 μM，1.27 μM，0.102 μM，和0.408 μM)，表現(xiàn)出更有效的選擇性。PP242對Ret，PKCα，PKCβ，和JAK2表現(xiàn)出一定的抑制活性，而對215種其他蛋白激酶具有顯著的選擇性。不同于rapamycin，PP242同時抑制mTORC1和 mTORC2。在BT549細胞中，PP242治療(0.04-10 μM)以劑量依賴的方式抑制Akt，mTOR底物p70S6K，和其下游靶點S6的磷酸化。[1] PP242有效抑制PKCα，IC50 為49 nM。低濃度PP242抑制Akt S473磷酸化，較高濃度部分抑制除S473-P 外的Akt T308-P。PP242作為比rapamycin更有效的mTORC1抑制劑，能夠抑制原代MEFs細胞的增殖，以及4EBP1在T36/45和S65上的磷酸化，比rapamycin更有效。通過比rapamycin引起更高水平的4EBP1 和eIF4E結(jié)合，PP242有效抑制cap依賴性翻譯，而 rapamycin無此作用。[2] PP242有效抑制p190轉(zhuǎn)化的小鼠BM，SUP-B15，和K562細胞增殖，GI50分別為12 nM，90 nM，和85 nM。PP242也會抑制固體腫瘤細胞系，如SKOV3，PC3，786-O，和U87的生長，GI50 分別為0.49 μM，0.19 μM，2.13 μM，和1.57 μM。[3] PP242能夠比rapamycin更有效地使多發(fā)性骨髓瘤(MM)細胞減少和凋亡。[4] | |||
|---|---|---|---|---|
| 激酶實驗 | 體外mTOR (FRAP1)激酶試驗 | |||
| 重組mTOR與50-0.001 μM濃度范圍內(nèi)連續(xù)2倍稀釋的PP242在試驗緩沖液中進行培養(yǎng)，緩沖液包含50 mM HEPES，pH 7.5，1 mM EGTA，10 mM MgCl2，0.01% Tween，10 μM ATP (2.5 μCi of γ-32P-ATP)，和3 μg/mL BSA。大鼠重組PHAS-1/4EBP1 (2 mg/mL)用作底物。通過在1 M NaCl/1%磷酸(大約6次，每次5-10分鐘)洗滌過的硝酸纖維素上點樣終止反應(yīng)。將板片干燥，轉(zhuǎn)移的放射性通過磷光成像定量。IC50值使用Prism軟件包將數(shù)據(jù)擬合到S形劑量反應(yīng)曲線進行計算。 | ||||
| 細胞實驗 | 細胞系 | MEFs | ||
| 濃度 | 在DMSO中溶解，終濃度為~10 μM | |||
| 孵育時間 | 72小時 | |||
| 方法 | 細胞用逐漸增加濃度的PP242在96孔板中處理72小時。處理72小時后，將10 μL 440 μM刃天青鈉鹽加入到每孔中，18小時后，每孔中的熒光強度使用頂端讀取的熒光板閱讀器在530 nm激發(fā)波長和590 nm發(fā)射波長下測量。 | |||
| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
| Western blot | p-mTOR / mTOR / p-AKT / AKT / p-S6 / S6 / p-4E-BP1 / 4E-BP-1 |
|
23991179 | |
| Growth inhibition assay | Cell viability |
|
23991179 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 在小鼠脂肪和肝臟中，PP242給藥能夠完全抑制Akt在S473和T308的磷酸化。PP242僅部分抑制骨骼肌中Akt磷酸化，并且對T308磷酸化的抑制比對S473更有效，盡管其能夠完全抑制4EBP1和S6的磷酸化。[2] PP242口服給藥有效延緩白血病在小鼠模型中的發(fā)病，并通過抑制與細胞大小損失相關(guān)的mTORC2和mTORC1活化，誘導(dǎo)白血病消退。[3] PP242治療有效抑制小鼠體內(nèi)8226細胞的生長。[4] | |
|---|---|---|
| 動物實驗 | Animal Models | 負荷小鼠p190轉(zhuǎn)染的會引發(fā)白血病的BM細胞的同源(Balbc/J)小鼠，和靜脈注射SUP-B15ffLuc細胞或人Ph+白血病細胞的雌性小鼠 |
| Dosages | ~60 mg/kg/day | |
| Administration | 口服強飼 | |
|
化學(xué)信息&溶解度
| 分子量 | 308.34 | 分子式 | C16H16N6O |
| CAS號 | 1092351-67-1 | SDF | Download Torkinib (PP242) SDF |
| Smiles | CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(N3)C=CC(=C4)O)N | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 61 mg/mL ( (197.83 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解配方 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(nèi)配方計算器 | |||||
實驗計算
動物體內(nèi)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(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(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
常見問題及建議解決方法
問題 1:
Do you have any suggestions about potential candidates for vehicles that we could use for in vivo studies?
回答：
S2218 in the recommended solvent (30% PEG400 + 0.5% Tween80 + 5% Propylene glycol) is a suspension, and this formulation is for oral gavage. For IV injection, this compound can be dissolved in 2% DMSO+30% PEG 300+5% Tween 80+ddH2O at 5mg/ml as a clear solution.
