PT-88
PT-88 is a potent and selective ATP-competitive mTOR kinase inhibitor, IC50 = 1.2 nM. PT-88 inhibits both mTORC1 and mTORC2 and blocks the phosphorylation of their downstream proteins (such as p70S6K, 4EBP1, and Akt), thereby inducing cancer cell cycle arrest, autophagy, and apoptosis. PT-88 can be used for research on human breast cancer.
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- No. CAS: 2803307-04-0
- Fòrmula: C30H31N7O5
- Peso molecular:569.61
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
mTOR 1.2 nM (IC50) |
TORC1 |
mTORC2 |
p70S6K |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.74 μM
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Cytotoxicity against human MCF-7 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
Cytotoxicity against human MCF-7 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
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38661655 |
| MDA-MB-231 | IC50 |
2.29 μM
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Cytotoxicity against human MDA-MB-231 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
Cytotoxicity against human MDA-MB-231 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
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38661655 |
| HepG2 | IC50 |
3.46 μM
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Cytotoxicity against human HepG2 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
Cytotoxicity against human HepG2 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
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38661655 |
| HeLa | IC50 |
10.27 μM
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Cytotoxicity against human HeLa cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
Cytotoxicity against human HeLa cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
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38661655 |
| HCT-116 | IC50 |
2.24 μM
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Cytotoxicity against human HCT116 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
Cytotoxicity against human HCT116 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
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38661655 |
| CNE-2 | IC50 |
2.13 μM
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Cytotoxicity against human CNE2 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
Cytotoxicity against human CNE2 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
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38661655 |
| L02 | IC50 |
11.56 μM
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Cytotoxicity against human L02 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
Cytotoxicity against human L02 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.
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38661655 |
In Vitro
PT-88 (1-10 μM; 24 h) suppresses mTORC1/mTORC2 downstream phosphorylation in MCF-7 cells[1].
PT-88 (0.5-2 μM; 2 weeks) inhibits MCF-7 colony formation[1].
PT-88 (1-2 μM; 24-48 h) reduces MCF-7 wound healing[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:1, 10 μM
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Incubation Time:24 h
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Result:Phosphorylation of p70S6K (T389), 4EBP1 (T37/46), and Akt (S473) was extensively prevented at 1 and 10 μM.
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Cell Line:MCF-7 cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:2 weeks
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Result:MCF-7 colony formation was significantly inhibited at 0.5, 1, and 2 μM.
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Cell Line:MCF-7 cells
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Concentration:1, 1.5, 2 μM
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Incubation Time:24 and 48 h
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Result:MCF-7 migration was inhibited in a concentration-dependent manner at 24 and 48 h.
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Cell Line:MCF-7 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:24 h
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Result:With increasing concentration, the G2/M-phase fraction increased from 27.90% to 48.90%, and the S-phase fraction decreased.
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Cell Line:MCF-7 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:24 h
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Result:Total apoptotic cells were 18.2%, 13.0%, and 21.4% at 2.5, 5, and 10 μM, respectively.
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Cell Line:MCF-7 cells
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Concentration:0.1, 1, 10 μM
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Incubation Time:24 h
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Result:P62 decreased in a concentration-dependent manner; LC3I-to-LC3II conversion increased, with the increased effect higher at 1 μM.
Parmacokinetics
| Species | Dose | Route | AUC0-24 | AUCinf | T1/2 | Cmax |
|---|---|---|---|---|---|---|
| Mice[1] | 5 mg/kg | i.v. | 3782 μg/L·h | 3783 μg/L·h | 2.8 h | 11852 μg/L |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 6 weeks old)[1]
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Dosage:20 mg/kg
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Administration:i.v.; once every other day for a total of 10 doses; continuous observation for 19 days
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Result:Resulted in a tumor growth inhibition (TGI) value of 45.6%.
Had high biosafety profiles.
- Western Blot
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Protocol for Cell Cycle
- Breast Cancer Modeling
- Kinase activity and phosphorylation assays
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Autophagy
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
- Lysosome and acidic-vesicle live-cell staining
- Macroautophagy Solutions
Chemical Information
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No. CAS 2803307-04-0
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Peso molecular 569.61
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Fòrmula C30H31N7O5
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SMILES
O=C(NC1=CC=C(C2=NC(N3C4COCC3CC4)=NC(N5[C@@H]6COC[C@H]5CC6)=N2)C=C1)NC7=CC8=C(C=C7)C(OC8)=O
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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)
PT-88 Related Classifications
HY-161509 Related Classifications
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