75747-14-7 | 17-AAG (tanespimycin)

Chemical type

• Semisynthetic C-17 amino-substituted derivative of geldanamycin

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• HSP-90 (heat shock protein-90) inhibitor

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Key properties

• More stable than geldanamycin
• Inhibits Hsp90
• Poorly soluble leading to formulation issues
• Hepatotoxicity observed in clinical trials
• Lower reduction potential reduces toxicity compared to parent compound
• Higher binding affinity to tumor cell Hsp90

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• Inhibits HSP-90 to promote apoptosis
• Down-regulates Bcr-Abl levels and NF-κB expression
• Upregulates p53, caspase-3, caspase-8, and caspase-9
• Induces intrinsic and extrinsic apoptotic pathways
• Proapoptotic in leukemia and colon cancer cells

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• Investigated in clinical trials for cancers including melanoma, multiple myeloma, gastrointestinal stromal tumors, prostate cancer, non-small cell lung cancer, and HER2-positive breast cancer

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• Chemotherapeutic agent for colorectal cancer
• Combination therapy with capecitabine and irinotecan
• Apoptosis inducer in HT-29 colon cancer cells
• HSP-90 targeted therapy to overcome chemoresistance

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Classification by use

• Hsp90 inhibitors
• Anticancer agents

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• Chemicals used as apoptosis inducers
• Chemicals used in cancer chemotherapy
• Chemicals used as HSP inhibitors

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A trustworthy factory and manufacturer

1. [Cite:1] Geldanamycin, a Naturally Occurring Inhibitor of Hsp90 and a Lead Compound for Medicinal Chemistry, Journal of Medicinal Chemistry, Volume 67, Issue 20, 24 October 2024, Pages 17946-17963
2. [Cite:2] Combination effects of Irinotecan, irinotecan and 17-AAG on colorectal cancer cell line (HT-29), Annals of Medicine and Surgery, Volume 78, June 2022, 103850