交易须知
venetoclax产品活性：venetoclax (gdc-0199; abt-199) 是一种高效，有选择性和口服活性的 bcl-2 抑制剂，ki 小于0.01 nm。
研究领域：apoptosis
作用靶点：bcl-2 family
in vitro: venetoclax (abt-199) potently kills fl5.12-bcl-2 cells (ec50=4 nm), venetoclax (abt-199) shows much weaker activity against fl5.12-bcl-xl cells (ec50=261 nm). abt-199 also shows selectivity in cellular mammalian two-hybrid assays, where it disrupts bcl-2-bim complexes (ec50=3 nm) but is much less effective against bcl-xl-bcl-xs (ec50=2.2 μm) or mcl-1-noxa complexes.
in vivo: after a single oral dose of 12.5 mg per kg body weight in xenografts derived from rs4;11 cells (all), venetoclax (abt-199) causes a maximal tumor growth inhibition (tgimax) of 47% (p<0.001) and tumor growth delay (tgd) of 26% (p<0.05). treatment of established xenografted (a mouse xenograft model of the t-all cell line loucy) tumors with venetoclax (abt-199) 100 mg/kg for 4 days resulted in a significant reduction of leukemic burden (p=0.0048).
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