Technology Request

Status: lab scale or above

Geldanamycin and its derivates thereof are a family of a benzoquinone ansamycins, antibiotics originally isolated on the basis of their weak antibiotic activity that were subsequently shown to display potent antitumor activity. Formula: C29H40N2O9 Molecular weight: 560.64 CAS Number : 30562-34-6 Appearance: yellow powder 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 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:17-AAG,17-DMAG and some others. There is no patent on Geldanamycin as a compound. Pharmacology Geldanamycin binds with high affinity into the ATP binding pocket of Hsp 90. Hsp 90 is a ubiquitous molecular chaperone critical for the folding, assembly and activity of multiple mutated and overexpressed signaling proteins that promote the growth and/or survival of tumor cells. Hsp 90 target proteins include mutated p53, Raf-1, Akt, ErbB2 and hypoxia-inducible factor 1a (HIF-1a). Binding of Geldanamycin to Hsp 90 causes the destabilization and degradation of its client proteins.