2. PI3K/Akt/mTOR MAPK/ERK Pathway Apoptosis Autophagy
  3. mTOR Akt Ribosomal S6 Kinase (RSK) Apoptosis Autophagy PI3K
  4. T133

T133 is an orally active ATP-competitive mTOR inhibitor with an IC50 of 0.34 nM and a Ki of 0.17 nM. T133 suppresses phosphorylation of AKT, S6K1, and 4EBP1. T133 inhibits cancer cell proliferation and migration, induces apoptosis, cell cycle arrest, and autophagy. T133 exhibits dose-dependent antitumor efficacy in xenograft mouse models. T133 can be used for the research of cancer, such as gastric cancer and lung cancer.

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T133

T133 Chemical Structure

CAS No. : 3101627-06-6

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T133 Related Antibodies

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mTOR mTORC1 mTORC2

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Akt Akt1 Akt2 Akt3

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p70S6K RSK2 RSK3 RSK4

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Description

T133 is an orally active ATP-competitive mTOR inhibitor with an IC50 of 0.34 nM and a Ki of 0.17 nM. T133 suppresses phosphorylation of AKT, S6K1, and 4EBP1. T133 inhibits cancer cell proliferation and migration, induces apoptosis, cell cycle arrest, and autophagy. T133 exhibits dose-dependent antitumor efficacy in xenograft mouse models. T133 can be used for the research of cancer, such as gastric cancer and lung cancer[1].

IC50 & Target[1]

mTOR

0.17 ()

PI3Kδ

1.8 nM (Ki)

PI3Kγ

4.9 nM (Ki)

PI3Kα

47 nM (Ki)

PI3Kβ

125 nM (Ki)

In Vitro

T133 (Compound 51) potently inhibits recombinant mTOR kinase activity with an IC50 of 0.34 nM and a Ki of 0.17 nM[1].
T133 exhibits over 10-fold selectivity for mTOR over most class I PI3K isoforms, with a PI3Kδ Ki of 1.8 nM, PI3Kγ Ki of 4.9 nM, PI3Kα Ki of 47 nM, and PI3Kβ Ki of 125 nM[1].
T133 (72 h) potently inhibits the proliferation of HGC-27, NCI-H1299, and T-47D cancer cells with IC50 values of 0.82 μM, 1.22 μM, and 0.28 μM respectively[1].
T133 (1-2.5 μM; 16 h) significantly inhibits the migration of HGC-27 gastric cancer cells after 16 h of treatment[1].
T133 (0.3-100 μM; 2 h, 24 h) dose-dependently inhibits the PI3K/AKT/mTOR signaling pathway and induces apoptosis in HGC-27, NCI-H1299, and T-47D cancer cells after 2 h and 24 h of treatment[1].
T133 (20-100 nM; 48 h) induces autophagy in HGC-27 gastric cancer cells after 48 h of treatment[1].
T133 (100-500 nM; 24 h) arrests HGC-27 gastric cancer cells in the G1 phase of the cell cycle after 24 h of treatment[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

T133 Related Antibodies

Western Blot Analysis[1]

Cell Line: HGC-27, NCI-H1299, T-47D cancer cells
Concentration: 0.3, 1, 3, 10, 30,100 μM
Incubation Time: 2 h, 24 h
Result: Inhibited phosphorylation of AKT (Ser473, Thr308), S6 (Ser240/244, Ser235/236), and 4EBP1 (Thr37/46) in a dose-dependent manner across all three cell lines.
Induced cleavage of PARP in HGC-27 cells, indicating apoptosis.

Cell Autophagy Assay[1]

Cell Line: HGC-27 gastric cancer cells
Concentration: 20, 100 nM
Incubation Time: 48 h
Result: Significantly increased monodansylcadaverine (MDC)-labeled autophagic vesicles, with mean fluorescence intensity (MFI) values of ~12 at 20 nM and ~20 at 100 nM, compared to the control.

Cell Cycle Analysis[1]

Cell Line: HGC-27 gastric cancer cells
Concentration: 100, 500 nM
Incubation Time: 24 h
Result: Increased the percentage of cells in G1/G0 phase.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ Vss CL F
Mice[1] 1 mg/kg i.v. 1.25 h 0.08 h 1730 ng/mL 748 ng·h/mL 752 ng·h/mL 0.642 L/kg 1332 mL/h/kg /
Mice[1] 5 mg/kg p.o. 1.88 h 0.50 h 868 ng/mL 1169 ng·h/mL 1220 ng·h/mL / / 31.2 %
In Vivo

T133 (Compound 51) (30-60 mg/kg; p.o.; daily for18 days) produces 83% and 92% tumor growth inhibition, respectively, in HGC-27 gastric cancer xenografts, while maintaining a favorable safety profile[1].
T133 (30-60 mg/kg; p.o.; daily for 26 days) effectively suppresses tumor growth in NCI-H1299 non-small-cell lung cancer xenografts with a favorable safety profile[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c (female, 5−6 weeks old, 18-20 g, subcutaneous HGC-27 xenograft model)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; daily for 18 days
Result: Achieved 83% tumor growth inhibition (TGI) at 30 mg/kg.
Achieved 92% tumor growth inhibition (TGI) at 60 mg/kg.
Maintained normal body weights, with serum ALT, AST, urea, creatinine, and IL-6 levels within physiological ranges.
Showed no significant morphological or pathological changes in liver, kidney, or lung tissues.
Induced dose-dependent reduction in phosphorylated AKT (Ser473) and phosphorylated S6 (Ser240/244) in tumor tissues.
Animal Model: C-NKG (female, 5−6 weeks old, 20-22 g, subcutaneous NCI-H1299 xenograft model)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; daily for 26 days
Result: Effectively suppressed tumor growth in the NCI-H1299 xenograft model.
Showed no associated significant body weight loss or overt toxicity.
Molecular Weight

421.41

Formula

C21H19N5O5
CAS No.
SMILES

NC1=C2C(N(C(C(C3=COC4=C3C=CC(O)=C4)=N2)=O)[C@H]5CC[C@@H](CC5)C(O)=O)=NC=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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T133 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

T1333101627-06-6T 133T-133mTORAktRibosomal S6 Kinase (RSK)ApoptosisAutophagyPI3KMammalian target of RapamycinPKBProtein kinase BS6KPhosphoinositide 3-kinaseS6K1breast cancermTORC1gastric cancerxenograft mouse modelsmTORC2AKTlung cancer4EBP1Inhibitorinhibitorinhibit

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