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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2790425-52-2
- 分子式: C19H15F3N6O2
- 分子量:416.36
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保管条件:
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]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
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) |
体外実験
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.
体内実験
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.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Breast Cancer Modeling
- Orthotopic Cell-Line Xenograft
- Pyroptosis Solutions
- Intraperitoneal/Peritoneal Dissemination Xenograft
化学情報
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CAS 番号 2790425-52-2
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分子量 416.36
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TNI-97 関連分類
HY-175030 関連分類
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