Hsp90-IN-42
Hsp90-IN-42 is a heat shock protein 90 (Hsp90) inhibitor with an IC50 of 15.65 nM against human targets. Hsp90-IN-42 destabilizes EGFR and inhibits the activation of the EGFR-Akt signaling pathway. Hsp90-IN-42 suppresses the proliferation and migration of cancer cells, induces cell cycle arrest by downregulating CDK12 and CDK13, and triggers mild apoptosis via downregulating Bcl-2 and upregulating Bax. Hsp90-IN-42 inhibits tumor growth in xenograft mouse models. Hsp90-IN-42 can be used in research related to colorectal cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 分子式: C27H27FN2O2
- 分子量:430.51
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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
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- 純度とドキュメンテーション
- 参考文献
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生物活性
製品説明
IC50 & Target
[1]|
HSP90 15.65 nM (IC50) |
CDK12 |
CDK13 |
Bcl-2 |
Bax |
EGFR |
体外実験
Hsp90-IN-42 (0.5-5.0 μM; 24-48 h) effectively inhibits the migration of HT-29 colorectal cancer cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29
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Concentration:0.5, 1.0, 5.0 μM
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Incubation Time:48 h initial treatment, followed by 14 days of culture
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Result:Inhibited colony formation in a concentration-dependent manner.
Achieved complete inhibition at 1.0 μM.
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Cell Line:HT-29
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Concentration:0.5, 1.0, 5.0 μM
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Incubation Time:24 h, 48 h
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Result:Inhibited HT-29 cell migration in a concentration-dependent manner.
Showed significant inhibition at 1.0 μM after 24 h and 48 h.
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Cell Line:HT-29
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Concentration:0.5, 1.0, 5.0 μM
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Incubation Time:24 h
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Result:Induced dose-dependent G0/G1 phase arrest.
Increased G0/G1 cell population and decreased G2/M cell population.
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Cell Line:HT-29
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Concentration:0.5, 1.0, 5.0 μM
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Incubation Time:24 h
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Result:Induced dose-dependent apoptosis, with total apoptotic cell ratios increasing from 11.36% (control) to 20.56% at 5.0 μM.
Induced both early and late apoptosis, with late apoptosis rates ranging from 3.46% (control) to 4.96% at 5.0 μM.
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Cell Line:HT-29
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Concentration:0.5, 1.0, 5.0 μM
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Incubation Time:24 h
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Result:Downregulated protein expression of CDK12, CDK13, and anti-apoptotic Bcl-2 in a dose-dependent manner.
Upregulated expression of pro-apoptotic Bax (at 5.0 μM) and tumor suppressor p53.\nReduced EGFR protein levels at 0.5 μM and above.
Decreased total Akt protein levels and the ratio of phospho-Akt/Akt in a concentration-dependent manner.\nReduced Hsp90 protein levels only at 5.0 μM.
Increased Hsp70 protein expression in a concentration-dependent manner.
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:BALB/c nude (female, 5-week-old, 18-20 g, subcutaneous HT-29 cell xenograft)[1]
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Dosage:30 mg/kg
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Administration:i.p.; daily; 18 days
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Result:Achieved a tumor growth inhibition (TGI) value of 58.6%.
Caused no obvious body weight loss or adverse effects during treatment.
- Annexin V plus membrane-impermeant dye apoptosis staining
- Cell migration
- BrdU Incorporation Assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- Cell Viability Determination by MTT Colorimetric Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
化学情報
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分子量 430.51
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分子式 C27H27FN2O2
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SMILES
O=C(NC1=CC=C(F)C=C1)C2=CC=C(O[C@@H]3CN(CC4=CC=CC=C4)[C@]5([H])CC[C@@]3([H])C5)C=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
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Hsp90-IN-42 関連分類
HY-176279 関連分類
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