名称：原装进口| BIIB021, Free Base
Storage: Store at or below -20 ºC.
Solubility: Soluble in DMSO. Disposal: A. BIIB021, Free Base, >99%. M.W. 318.76. C14H15ClN6O.
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A Phase I clinical trail demonstrated that BIIB021 was generally well tolerated in patients with advanced solid tumors or chronic lymphocytic leukemia. BIIB021 inhibited the proliferation of P-gp and/or MRP-1 expressing cancer cell lines. The cytotoxic activity of BIIB021 was also not influenced by loss of NQO1 or Bcl-2 overexpression.
It has significant antitumor activity in N87 stomach, BT474 breast, CWR22 prostate, U87 glioblastoma, SKOV3 ovarian, and Panc-1 pancreatic tumor xenograft models.
It binds in the ATP-binding pocket of Hsp90 (Ki = 1.7 ± 0.4 nM) and induces HER-2 degradation with an EC50 of 38 ± 10 nM in MCF-7 cells. BIIB021 is an orally available, synthetic small-molecule Hsp90 inhibitor. BIIB021 has antitumor activity in Hodgkins lymphoma in vitro and in vivo. BIIB021 selectively induced Hodgkins lymphoma cell death but did not kill normal lymphocytes from healthy individuals.
The maximum tolerated dose of BIIB021 was less than 800 mg twice a week. Serum and intracellular Hsp70 was increased and the serum level of Her-2/neu extracellular domain was decreased after administration. BIIB021 inhibits the proliferation of N87, MCF-7, and BT474 tumor cells with IC50 values of 0.06, 0.31, and 0.14 µM, respectively.