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Torkinib (PP242)

Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. Torkinib (PP242) induces mitophagy and apoptosis.

Torkinib (PP242)化学構造

CAS No. 1092351-67-1

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 55500 国内在庫あり
JPY 430500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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Torkinib (PP242)関連製品

シグナル伝達経路

mTOR Signaling Pathways

mTORシグナル伝達経路

mTOR阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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

製品説明 Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. Torkinib (PP242) induces mitophagy and apoptosis.
特性 One of the first selective inhibitors that targets ATP domain of mTOR.
Targets
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
In Vitro
In vitro PP242 exhibits potent selectivity for mTOR over other PI3K family kinases such as p110α, p110β, p110γ, p110δ, and DNA-PK with IC50 of 1.96 μM, 2.2 μM, 1.27 μM, 0.102 μM, and 0.408 μM, respectively. PP242 displays some inhibitory activity against Ret, PKCα, PKCβ, and JAK2, while exhibits remarkable selectivity against 215 other protein kinases. Unlike rapamycin, PP242 inhibits both mTORC1 and mTORC2. In BT549 cells, PP242 treatment (0.04-10 μM) inhibits the phosphorylation of Akt, the mTOR substrate p70S6K, and its downstream target S6 in a dose-dependent manner. [1] PP242 potently inhibits PKCα with IC50 of 49 nM. Low concentrations of PP242 inhibit the phosphorylation of Akt S473 and higher concentrations partially inhibit Akt T308-P in addition to S473-P. As PP242 is a more effective mTORC1 inhibitor than rapamycin, PP242 inhibits the proliferation of primary MEFs, and the phosphorylation of 4EBP1 at T36/45 and S65, more potently than rapamycin. PP242 but not rapamycin potently inhibits cap-dependent translation, by causing a higher level of binding between 4EBP1 and eIF4E than rapamycin. [2] PP242 potently inhibits the proliferation of p190-transformed murine BM, SUP-B15, and K562 cells with GI50 of 12 nM, 90 nM, and 85 nM, respectively. PP242 also inhibits the growth of solid tumor cell lines such as SKOV3, PC3, 786-O, and U87 with GI50 of 0.49 μM, 0.19 μM, 2.13 μM, and 1.57 μM, respectively. [3] PP242 is also more effective than rapamycin in achieving cytoreduction and apoptosis in multiple myeloma (MM) cells. [4]
Kinase Assay In vitro mTOR (FRAP1) kinase assay
Recombinant mTOR is incubated with PP242 at 2-fold dilutions over a concentration range of 50-0.001 μM in an assay containing 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), and 3 μg/mL BSA. Rat recombinant PHAS-1/4EBP1 (2 mg/mL) is used as a substrate. Reactions are terminated by spotting onto nitrocellulose, which is washed with 1 M NaCl/1% phosphoric acid (approximately 6 times, 5-10 minutes each). Sheets are dried and the transferred radioactivity quantitated by phosphorimaging. IC50 value is calculated by fitting the data to a sigmoidal dose-response curve using the Prism software package.
細胞実験 細胞株 MEFs
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 72 hours
実験の流れ Cells are treated with increasing concentrations of PP242 for 72 hours in 96-well plates. After 72 hours of treatment, 10 μL of 440 μM resazurin sodium salt is added to each well, and after 18 hours, the florescence intensity in each well is measured using a top-reading florescent plate reader with excitation at 530 nm and emission at 590 nm.
実験結果図 Methods Biomarkers 結果図 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
In Vivo
In Vivo Administration of PP242 is able to completely inhibit the phosphorylation of Akt at S473 and T308 in fat and liver of mice. PP242 only partially inhibits the phosphorylation of Akt in skeletal muscle and is more effective at inhibiting the phosphorylation of T308 than S473, despite able to fully inhibit the phosphorylation of 4EBP1 and S6. [2] Oral administration PP242 potently delays the leukemia onset in the mice model, and induces leukemia regression by inhibiting mTORC2 and mTORC1 activation that correlates with loss in cell size. [3] PP242 treatment potently inhibits the growth of 8226 cells in mice. [4]
動物実験 動物モデル Syngeneic (Balbc/J) mice with mouse p190-transformed BM cells to initiate leukemia, and female NSG mice injected (i.v.) with SUP-B15ffLuc cells or human Ph+ leukemia
投与量 ~60 mg/kg/day
投与経路 Oral gavage

化学情報

分子量 308.34 化学式

C16H16N6O
CAS No. 1092351-67-1 SDF Download Torkinib (PP242) SDFをダウンロードする
Smiles CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(N3)C=CC(=C4)O)N
保管

In vitro
Batch:

DMSO : 61 mg/mL ( (197.83 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問（FAQ）

質問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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