HSP90/mTOR-IN-1
HSP90/mTOR-IN-1 is a potent and orally active Hsp90 and mTOR inhibitor with IC50 values of 69 nM and 29 nM, respectively. HSP90/mTOR-IN-1 suppresses the proliferation of SW780 cells through the over-activation of the PI3K/AKT/mTOR pathway. HSP90/mTOR-IN-1 induces apoptosis and autophagy via selective Hsp90 and mTOR inhibition. HSP90/mTOR-IN-1 also has considerable in vivo anti-tumor activity. HSP90/mTOR-IN-1 can be used for researching bladder 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: 3033543-67-5
- 分子式: C36H34ClFN6O5S
- 分子量:717.21
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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
- 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
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mTOR 29 nM (IC50) |
HSP90 69 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| J82 | IC50 |
0.36 μM
Compound: 17o
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Antiproliferative activity against human J82 cells assessed as inhibition of cell proliferation by CCK8 assay
Antiproliferative activity against human J82 cells assessed as inhibition of cell proliferation by CCK8 assay
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[PMID: 35987020] |
| SW780 | IC50 |
0.16 μM
Compound: 17o
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Antiproliferative activity against human SW780 cells assessed as inhibition of cell proliferation by CCK8 assay
Antiproliferative activity against human SW780 cells assessed as inhibition of cell proliferation by CCK8 assay
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[PMID: 35987020] |
| T-24 | IC50 |
0.41 μM
Compound: 17o
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Antiproliferative activity against human T24 cells assessed as inhibition of cell proliferation by CCK8 assay
Antiproliferative activity against human T24 cells assessed as inhibition of cell proliferation by CCK8 assay
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[PMID: 35987020] |
HSP90/mTOR-IN-1 (compound 17o) has antiproliferative activity against J82, T24 and SW780 cells[1].
HSP90/mTOR-IN-1 (0.2 and 0.5 μM; 24 h) induces SW870 apoptosis in a dose-dependent manner, induces the formation of autophagosome[1].
HSP90/mTOR-IN-1 (0.2 and 0.5 μM; 24 h) decreases the expression of several Hsp90 client proteins in SW870[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:J82, T24 and SW780[1]
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Concentration:0-1 μM
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Incubation Time:48 h
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Result:Exhibited antiproliferative activity against J82, T24 and SW780 with IC50s of 0.36 ± 0.03 μM, 0.41 ± 0.06 μM, 0.16 ± 0.03 μM.
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Cell Line:SW870
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Concentration:0.2 and 0.5 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner (total apoptotic cell percentage was 12.4% and 16.5% at 0.2 and 0.5 μM, respectively).
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Cell Line:SW870 (transfected with GFP-LC3)
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Concentration:0.2 and 0.5 μM
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Incubation Time:24 h
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Result:Induced the formation of autophagosome.
The green fluorescent spots were observed to increase in the number and gathered.
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Cell Line:SW870
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Concentration:0.2 and 0.5 μM
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Incubation Time:24 h
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Result:Significantly decreased the expression of several Hsp90 client proteins, CDK4, C-Raf and CDC2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balc/c nude mice (6-8 weeks; subcutaneously injected with 1×106 cells per 100 μL of J82 cells into the mice's dorsal skin)[1]
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Dosage:30 mg/kg
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Administration:PO; for 17 days
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Result:Exhibited significantly superior tumor growth inhibition, and did not showed remarkable weight decline.
Inhibited bladder cancer cell proliferation, induced cell apoptosis, degraded Hsp70, as well as decreased phosphorylation levels of mTOR and increased expression of LC3-II.
化学情報
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CAS 番号 3033543-67-5
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分子量 717.21
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分子式 C36H34ClFN6O5S
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SMILES
ClC1=CC(NC(NC2=CC=C(C=C2)C3=NC(N4CCOCC4)=C5C6=C(SC5=N3)CN(CC6)C(C7=CC(C(C)C)=C(C=C7O)O)=O)=O)=CC=C1F
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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/mTOR-IN-1 関連分類
HY-151137 関連分類
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