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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- No. CAS: 3101627-06-6
- Fòrmula: C21H19N5O5
- Peso molecular:421.41
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Actividad biológica
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mTOR 0.17 () |
PI3Kδ 1.8 nM (Ki) |
PI3Kγ 4.9 nM (Ki) |
PI3Kα 47 nM (Ki) |
PI3Kβ 125 nM (Ki) |
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.
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Cell Line:HGC-27, NCI-H1299, T-47D cancer cells
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Concentration:0.3, 1, 3, 10, 30,100 μM
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Incubation Time:2 h, 24 h
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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.
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Cell Line:HGC-27 gastric cancer cells
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Concentration:20, 100 nM
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Incubation Time:48 h
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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.
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Cell Line:HGC-27 gastric cancer cells
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Concentration:100, 500 nM
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Incubation Time:24 h
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Result:Increased the percentage of cells in G1/G0 phase.
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.
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Animal Model:BALB/c (female, 5−6 weeks old, 18-20 g, subcutaneous HGC-27 xenograft model)[1]
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Dosage:30 mg/kg; 60 mg/kg
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Administration:p.o.; daily for 18 days
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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.
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Animal Model:C-NKG (female, 5−6 weeks old, 20-22 g, subcutaneous NCI-H1299 xenograft model)[1]
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Dosage:30 mg/kg; 60 mg/kg
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Administration:p.o.; daily for 26 days
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Result:Effectively suppressed tumor growth in the NCI-H1299 xenograft model.
Showed no associated significant body weight loss or overt toxicity.
Chemical Information
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No. CAS 3101627-06-6
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Peso molecular 421.41
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Fòrmula C21H19N5O5
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
T133 Related Classifications
HY-181650 Related Classifications
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