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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 3101627-06-6
- Formule: C21H19N5O5
- Masse moléculaire:421.41
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
|
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.
-
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 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 Line:HGC-27 gastric cancer cells
-
Concentration:100, 500 nM
-
Incubation Time:24 h
-
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.
-
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.
Chemical Information
-
CAS No. 3101627-06-6
-
Masse moléculaire 421.41
-
Formule C21H19N5O5
-
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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
T133 Related Classifications
HY-181650 Related Classifications
Powered by Bioz