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Geldanamycin Analog for Conjugation to a Monoclonal Antibody
A geldanamycin analog for conjugation to a monoclonal antibody
17-GMB-APA-GA is a maleimido derivative of geldanamycin that enables the conjugation of GA to a monoclonal antibody (mAb) such as Herceptin, the first mAb approved for therapy of solid tumors.
This geldanamycin immunoconjugate induces less systemic toxicity than GA by being selectively delivered into malignant cells, a property conferred by the mAb that acts as the targeting vehicle.
NCI has reported that Herceptin-GA conjugates deliver a more potent selective cytotoxic impact to Her2-overexpressing tumors than Herceptin alone . To prepare such conjugates, GA is modified to introduce a latent primary amine .
After deprotection, this primary amine provides a site for introduction of a maleimide group that enables linkage to proteins.
1. Mandler R. et al., 2004. Herceptin-geldanamycin immunoconjugates: pharmacokinetics, biodistribution, and enhanced antitumor activity. Cancer Res. 64(4):1460-7.
2. Mandler R. et al., 2002. Modifications in synthesis strategy improve the yield and efficacy of geldanamycin-herceptin immunoconjugates. Bioconjug Chem. 13(4):786-91.
Molecular weight: 768
Solubility: DMSO (10 mg/ml)Back to the top
- 1 mg
17-GMB-APA-GA is shipped at room temperature.
Store lyophilized product at -20°C in the dark.
Protect from light.
Lyophilized productis stable for 6 months when stored properly.Back to the top