Geldanamycin is a benzoquinone ansamycin antibiotic that binds to Hsp90 (Heat Shock Protein 90) and inhibits its function. It appears as a yellow crystalline powder, melting point is 265ºC - 268ºC. Geldanamycin induces the degradation of proteins that are mutated in tumor cells such as v-src, bcr-abl and p53 preferentially over their normal cellular counterparts. HSP90 client proteins play important roles in the regulation of the cell cycle, cell growth, cell survival, apoptosis, angiogenesis and oncogenesis.
This effect is mediated via HSP90. Despite its potent antitumor potential. Identification: 1. HPLC retention tims. Geldanamycin has several major disadvantages as a remedy candidate that have led to the development of Geldanamycin analogues, in particular analogues containing a substitution on the 17 position:
Specification: Enterprise Standard. Water: 1.6%～0.3%. Selectively inhibits heat shock protein 90 (Hsp90). Binds to the ATP site of Hsp90 (Kd = 1.2 μM) and inhibits its chaperone activity. Consequently inhibits activities of oncogenic kinases (e.g. src, Raf), p53 and steroid receptors. Although geldanamycin was active in preclinical studies, it was a poor candidate for clinical trials due to its in vivo toxicity and instability. Assay (on anhydrous basis): >98.0%
Geldanamycin induces the degradation of proteins that are mutated in tumor cells such as v-Src, Bcr-Abl and p53 preferentially over their normal cellular counterparts. This effect is mediated via HSP90. Despite its potent antitumor potential, geldanamycin presents several major drawbacks as a drug candidate (namely, hepatotoxicity) that have led to the development of geldanamycin analogues, in particular analogues containing a derivatisation at the 17 position:17-AAG，17-DMAG..
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