BIIB021 is a potent HSP90 inhibitor (IC50 = 30 nM HER-2 degradation).1 It inhibited the proliferation of MCF7 and BT474 breast cancer cell lines (IC50 = 100 nM for each). BIIB021 has shown efficacy as a therapeutic in multiple cancer models.2-5
References:
- Kasibhatla et al. (2007), Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity; J. Med. Chem. 50 2767
- Lundgren et al. (2009), BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90; Mol. Cancer Ther. 8 921
- Boll et al. (2009), Heat shock protein 90 inhibitor BIIB021 (CNF2024) depletes NF-kappaB and sensitizes Hodgkin’s lymphoma cells for natural killer cell-mediated cytotoxicity; Clin. Cancer Res. 15 5108
- Zhang et al. (2010), BIIB021, a synthetic Hsp90 inhibitor, has broad application against tumors with acquired multidrug resistance; Int. J. Cancer 126 1226
- Wang et al. (2014), BIIB021, a novel Hsp90 inhibitor, sensitizes esophageal squamous cell carcinoma to radiation; Biochem. Biophys. Res. Commun. 452 945
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