TNI-97
TNI-97 is a selective and orally active HDAC6 inhibitor, with an IC50 of 0.2 nM. TNI-97 potently inhibited TNBC cell MDA-MB-453 growth and clonogenicity. TNI-97 induces PANoptosis including apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells. TNI-97 shows antitumor activity in the mice carrying the MDA-MB-453 xenograft or carrying murine-derived TNBC cell allografts. TNI-97 can be used for the study of triple-negative breast cancer.
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- No. CAS: 2790425-52-2
- Fòrmula: C19H15F3N6O2
- Peso molecular:416.36
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Almacenamiento:
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Actividad biológica
Descripciòn
IC50 & Target
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HDAC6 0.2 nM (IC50) |
HDAC1 2890 nM (IC50) |
HDAC2 1306 nM (IC50) |
HDAC3 3177 nM (IC50) |
HDAC8 4130 nM (IC50) |
HDAC4 >5000 nM (IC50) |
HDAC5 >5000 nM (IC50) |
HDAC7 >5000 nM (IC50) |
HDAC9 >5000 nM (IC50) |
HDAC11 >5000 nM (IC50) |
HDAC10 3162 nM (IC50) |
In Vitro
TNI-97 demonstrates antitumor activity with GI50 values of 0.8 μM in MDA-MB-453 cells and 5.4 μM in MDA-MB-468 cells[1]. TNI-97 (1 μM, 24 h) significantly induces α-tubulin acetylation than does Ricolinostat (ACY-1215) (HY-16026) under lower concentrations and does not induce histone H3 acetylation in MDA-MB-453 cells[1]. TNI-97 (1-2 μM, 14 days) dose-dependently inhibits the MDA-MB-453 colony formation[1]. TNI-97 (2.5-5 μM, 48 h) induces apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-453 cells
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Concentration:2.5, 5 μM
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Incubation Time:48 h
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Result:Induced apoptosis in MDA-MB-453 cells in a concentration-dependent manner.
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Cell Line:MDA-MB-453 cells
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Concentration:5 μM
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Incubation Time:48 h
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Result:Increased proportion of YPI/PI dual-positive cells.
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Cell Line:MDA-MB-453 cells
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Concentration:1, 5 μM
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Incubation Time:24 h
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Result:Elevated the expression of cleaved forms of executive caspase 3and caspase 7.
Upregulated cleaved forms of GSDMD and GSDME.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-PrkdcscidlL2rgtm1 (NSIG) female mice (6-8 weeks) carrying the MDA-MB-453 xenograft (1 × 107) [1]
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Dosage:20, 40 mg/kg
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Administration:p.o. 5 on/2 off for 2 weeks
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Result:Exhibited a dose-dependent inhibition of tumor growth, achieving tumor growth inhibition (TGI) rates of 91 and 54% at doses of 40 and 20 mg/kg, respectively. Induced pANoptosis in tumor tissue. Upregulated cleaved-caspase 3, cleavedGSDMD, and phosphorylated MLKL expression. Had no impact on the counts and proportions of white blood cells, red blood cells, and platelets. Showed no significant morphological abnormalities.
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Animal Model:BALB/c mice (6-8 weeks) carrying murine-derived TNBC cell allografts (1 × 106Dosage:40 mg/kgAdministration:p.o. 5 on/2 off for 2 weeksResult:Exhibited significant reductionsin both tumor weight and tumorsize of 4T1 allografts (TGI = 60%). Showed no significant alteration in body weight.
Chemical Information
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No. CAS 2790425-52-2
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Peso molecular 416.36
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Fòrmula C19H15F3N6O2
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SMILES
CN1N=NC2=C1C=CC(C3=NN(CC4=CC=C(C=C4)C(NO)=O)C(C(F)(F)F)=C3)=C2
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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
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Ficha de datos (279 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TNI-97 Related Classifications
HY-175030 Related Classifications
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