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Torkinib (PP242)

Torkinib (PP242) 是一種選擇性的mTOR抑制劑，在無細(xì)胞試驗(yàn)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

Torkinib (PP242) Chemical Structure

CAS: 1092351-67-1

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 749.83 現(xiàn)貨
5mg 570.16 現(xiàn)貨
50mg 3037.18 現(xiàn)貨
1g 23505.3 現(xiàn)貨
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Torkinib (PP242)相關(guān)產(chǎn)品

相關(guān)信號通路圖

mTOR Signaling Pathways

mTOR信號通路圖

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
HT-p21 Function Assay 50-1250 nM 24 h inhibits phosphorylation of S6 kinase (target of mTORC1) and its downstream target phospho-S6? 26177051
U87vIII? Function Assay 0.04-2.5 μM 24 h inhibits mTORC1 and mTORC2 activities? 26134617
U87vIII? Function Assay 2.5/5 μM 12 h inhibits gap closing in a dose-dependent manner 26134617
3T3-L1 Function Assay 15 μM 4 h suppresses expression of the Egr1 protein? 25814662
Rh30 Function Assay 1 μM 2 h inhibits both mTORC1-mediated phosphorylation of S6K1 and mTORC2-mediated phosphorylation of Akt 25762619
HT29 Function Assay 1 μM 2 h inhibits both mTORC1-mediated phosphorylation of S6K1 and mTORC2-mediated phosphorylation of Akt 25762619
Rh30 Function Assay 1 μM 2 h suppresses the basal or IGF-1-stimulated cell adhesion 25762619
HT29 Function Assay 1 μM 2 h suppresses the basal or IGF-1-stimulated cell adhesion 25762619
U87 Growth Inhibition Assay 25 nM 24 h increases DUSP10 knocked-down induced cell inhibition 25568665
AGS Cell Viability Assay 0-1000 nM 24/48 h decreases cell viability in time and dose dependent manner 25035961
MKN45 Cell Viability Assay 0-1000 nM 24/48 h decreases cell viability in time and dose dependent manner 25035961
MKN28 Cell Viability Assay 0-1000 nM 24/48 h decreases cell viability in time and dose dependent manner 25035961
KATO3 Cell Viability Assay 0-1000 nM 24/48 h decreases cell viability in time and dose dependent manner 25035961
SGC7901 Cell Viability Assay 0-1000 nM 24/48 h decreases cell viability in time and dose dependent manner 25035961
N87 Cell Viability Assay 0-1000 nM 24/48 h decreases cell viability in time and dose dependent manner 25035961
HMEC Cell Viability Assay 0-1000 nM 24/48 h decreases cell viability in time and dose dependent manner 25035961
HUVEC Cell Viability Assay 0-1000 nM 24/48 h decreases cell viability in time and dose dependent manner 25035961
MG63 Function Assay 50-1000 nM 0.5 h dose dependently (50–1000 nM) inhibits phosphorylation of Akt 24840134
U2OS? Function Assay 50-1000 nM 0.5 h dose dependently (50–1000 nM) inhibits phosphorylation of Akt 24840134
Saos-2? Function Assay 50-1000 nM 0.5 h dose dependently (50–1000 nM) inhibits phosphorylation of Akt 24840134
Saos-2 Function Assay 100 nM 0.5 h prevents osteosarcoma cell migration 24840134
MG63 Apoptosis Assay 100 nM 36 h promotes apoptosis 24840134
U2OS? Apoptosis Assay 100 nM 36 h promotes apoptosis 24840134
Saos-2? Apoptosis Assay 100 nM 36 h promotes apoptosis 24840134
DLD-1 Cell Viability Assay 0-1000 nM 24 h inhibits the growth in a dose-dependent manner 23991179
Caco2 Cell Viability Assay 0-1000 nM 24 h inhibits the growth in a dose-dependent manner 23991179
HT29 Cell Viability Assay 0-1000 nM 24 h inhibits the growth in a dose-dependent manner 23991179
H116 Cell Viability Assay 0-1000 nM 24 h inhibits the growth in a dose-dependent manner 23991179
Hct-8 Cell Viability Assay 0-1000 nM 24 h inhibits the growth in a dose-dependent manner 23991179
Colo320 Cell Viability Assay 0-1000 nM 24 h inhibits the growth in a dose-dependent manner 23991179
Sw948 Cell Viability Assay 0-1000 nM 24 h inhibits the growth in a dose-dependent manner 23991179
Colo205 Cell Viability Assay 0-1000 nM 24 h inhibits the growth in a dose-dependent manner 23991179
Colo320 Function Assay 1 μM 0-24 h abolishes the S6S235/236?but partially reduces the 4E-BP1T36/45 23991179
HT29 Function Assay 1 μM 0-24 h abolishes the S6S235/236?but partially reduces the 4E-BP1T36/45 23991179
Sw948 Function Assay 1 μM 0-24 h abolishes the S6S235/236?but partially reduces the 4E-BP1T36/45 23991179
DLD-1 Function Assay 1 μM 0-24 h abolishes the S6S235/236?but partially reduces the 4E-BP1T36/45 23991179
786-O Function Assay 0.1/0.5 μM 24 h increases E-cadherin mRNA levels dose dependently 23147251
786-O Function Assay 0-0.5 μM 24 h results in a dose dependent increase in E-cadherin protein expression? 23147251
OCI-AML3 Apoptosis Assay 2.5 μM 72 h induces apoptosis 22826565
Jurkat Function Assay 100/200/400 nM 18 h inhibits mTORC1-dependent S6 S235/236 phosphorylation 22566604
p210 BCR-Abl Function Assay 100/200/400 nM 18 h inhibits mTORC1-dependent S6 S235/236 phosphorylation 22566604
Jurkat Growth Inhibition Assay 400nM 24/48 h synergize with 17-AAG to suppress cell proliferation 22566604
p210 BCR-Abl Growth Inhibition Assay 400nM 24/48 h synergize with 17-AAG to suppress cell proliferation 22566604
8226 Function Assay 100-1000 nM 30 min activates ERK? 22556409
MM1.S? Function Assay 100-1000 nM 30 min activates ERK? 22556409
8226 Function Assay 0.5 μM 30 min induces activation of RAF and phosphorylation of MEK 22556409
MM1.S? Function Assay 0.5 μM 30 min induces activation of RAF and phosphorylation of MEK 22556409
MCF-7 Function Assay 50/200/500 nM 30 min dose-dependently (50–500?nM) suppresses phosphorylation of Akt 22476852
T47D Function Assay 50/200/500 nM 30 min dose-dependently (50–500?nM) suppresses phosphorylation of Akt 22476852
MDA-MB-231 Function Assay 50/200/500 nM 30 min dose-dependently (50–500?nM) suppresses phosphorylation of Akt 22476852
Bcap-37 Function Assay 50/200/500 nM 30 min dose-dependently (50–500?nM) suppresses phosphorylation of Akt 22476852
MCF-7 Apoptosis Assay 200?nM 36 h induces apoptosis 22476852
MDA-MB-231 Apoptosis Assay 200?nM 36 h induces apoptosis 22476852
Bcap-37 Apoptosis Assay 200?nM 36 h induces apoptosis 22476852
LS174T Function Assay 10/100/1000 nM 6 h inhibits mTORC1 activity by the dephosphorylation of S6 ribosomal protein 22401294
DLD-1? Function Assay 10/100/1000 nM 6 h inhibits mTORC1 activity by the dephosphorylation of S6 ribosomal protein 22401294
SW480 Function Assay 10/100/1000 nM 6 h inhibits mTORC1 activity by the dephosphorylation of S6 ribosomal protein 22401294
NIH 3T3 Function Assay 2 μM 18 h inhibits mTORC2 phosphorylation of Akt on Ser473 and mTORC1 phosphorylation of 4E-BP1 on Thr37/46 21876130
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 21876130
SW620? Function Assay 0.5/2 μM 4 h blocks all three mTOR outputs 21876130
PC12? Function Assay 40?nM induces lysosomal biogenesis and alleviated α-SYN accumulation? 26001614
DND-1 Growth Inhibition Assay 0.25/0.5/1 μM inhibits cell growth dose dependently 23482748
TMD8 Growth Inhibition Assay 0.25/0.5/1 μM inhibits cell growth dose dependently 23482748
Jurkat Growth Inhibition Assay 0.25/0.5/1 μM inhibits cell growth dose dependently 23482748
KOPT-K1 Growth Inhibition Assay 0.25/0.5/1 μM inhibits cell growth dose dependently 23482748
TMD7 Growth Inhibition Assay 0.25/0.5/1 μM inhibits cell growth dose dependently 23482748
THP-1 Growth Inhibition Assay 0.25/0.5/1 μM inhibits cell growth dose dependently 23482748
HT1376 Growth Inhibition Assay IC50=1.88 ± 1.1 μM 24054871
T24 Growth Inhibition Assay IC50=1.37 ± 0.4 μM 24054871
UM-UC-3 Growth Inhibition Assay IC50=0.63 ±0.1 μM 24054871
SW620 Growth Inhibition Assay IC50=7.8 μM 23542178
SW480 Growth Inhibition Assay IC50=4.6 μM 23542178
SK-CO-1 Growth Inhibition Assay IC50=4 μM 23542178
LS-513 Growth Inhibition Assay IC50=3.9 μM 23542178
SW1116 Growth Inhibition Assay IC50=0.84 μM 23542178
LS-174T Growth Inhibition Assay IC50=0.84 μM 23542178
HCT 116 Growth Inhibition Assay IC50=0.41 μM 23542178
HCT 15 Growth Inhibition Assay IC50=0.3 μM 23542178
COLO 205 Growth Inhibition Assay IC50=0.24 μM 23542178
HT-29 Growth Inhibition Assay IC50=0.23 μM 23542178
COLO 201 Growth Inhibition Assay IC50=0.23 μM 23542178
Caco-2 Growth Inhibition Assay IC50=0.22 μM 23542178
SW48 Growth Inhibition Assay IC50=0.09 μM 23542178
SW-48 Growth Inhibition Assay IC50=0.1 μM 22270257
HCT-15 Growth Inhibition Assay IC50=0.3 μM 22270257
HCT 116 Growth Inhibition Assay IC50=0.6 μM 22270257
SW620-R Growth Inhibition Assay IC50=1.3 μM 22270257
SK-CO-1 Growth Inhibition Assay IC50=2.1 μM 22270257
SW620 Growth Inhibition Assay IC50=11 μM 22270257
BaF3 Growth Inhibition Assay GI50=1.449 μM 22223645
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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(xì)胞試驗(yàn)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?yàn)榘悬c(diǎn)的選擇性抑制劑之一。
靶點(diǎn)
mTOR [1]
(Cell-free assay)		 p110δ [1]
(Cell-free assay)		 DNA-PK [1]
(Cell-free assay)		 PDGFR [1]
(Cell-free assay)
8 nM 0.10 μM 0.41 μM 0.41 μM
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(shí)抑制mTORC1和 mTORC2。在BT549細(xì)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(diǎn)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(xì)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(xì)胞增殖，GI50分別為12 nM，90 nM，和85 nM。PP242也會抑制固體腫瘤細(xì)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(xì)胞減少和凋亡。[4]
激酶實(shí)驗(yàn) 體外mTOR (FRAP1)激酶試驗(yàn)
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(yàn)緩沖液中進(jìn)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(diǎn)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(jìn)行計(jì)算。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 MEFs
濃度 在DMSO中溶解，終濃度為~10 μM
孵育時(shí)間 72小時(shí)
方法 細(xì)胞用逐漸增加濃度的PP242在96孔板中處理72小時(shí)。處理72小時(shí)后，將10 μL 440 μM刃天青鈉鹽加入到每孔中，18小時(shí)后，每孔中的熒光強(qiáng)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(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)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(xì)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(xì)胞的生長。[4]
動物實(shí)驗(yàn) Animal Models 負(fù)荷小鼠p190轉(zhuǎn)染的會引發(fā)白血病的BM細(xì)胞的同源(Balbc/J)小鼠，和靜脈注射SUP-B15ffLuc細(xì)胞或人Ph+白血病細(xì)胞的雌性小鼠
Dosages ~60 mg/kg/day
Administration 口服強(qiáng)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
批次：

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(jì)算器

體內(nèi)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(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

動物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(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(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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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.

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