BIIB021

BIIB021 is a potent, orally-available inhibitor of Hsp90 (K_i = 1.7 nM) that induces the degradation of oncoproteins, including HER2 (EC₅₀ = 38 nM), while up-regulating the expression of Hsp70 and Hsp27.^1,2 It is cytotoxic to cancer cells and, when administered orally to mice, inhibits growth of xenograft tumors.^1,2,3 BIIB021 suppresses growth in various lymphoma cells but not in normal lymphocytes and induces apoptosis in a myelodysplastic syndrome cell line.^4,5,3

WARNING This product is not for human or veterinary use.

1. Kasibhatla, S.R., Hong, K., Biamonte, M.A., et al. Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. J. Med. Chem. 50(12), 2767-2778 (2007).

2. Lindgren, K., Zhang, H., Brekken, J., et al. BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Mol. Cancer Ther. 8(4), 921-929 (2009).

3. Lin, S., Li, J., Zhou, W., et al. BIIB021, an Hsp90 inhibitor, effectively kills a myelodysplastic syndrome cell line via the activation of caspases and inhibition of PI3K/Akt and NF-κB pathway proteins. Exp. Ther. Med. 7, 1539-1544 (2014).

4. Böll, B., Eltaib, F., Reiners, K.S., et al. 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(16), 5108-5116 (2009).

5. Suzuki, M., Takeda, T., Nakagawa, H., et al. The heat shock protein 90 inhibitor of BIIB021 suppresses the growth of T and natural killer cell lymphomas. Front. Microbiol. 6, 280 (2015).