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。
Description | ABT-199 is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. | ||||||||||||||||
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IC50 & Target |
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In Vitro | ABT-199 potently kills FL5.12-BCL-2 cells (EC50=4 nM), 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[1]. | ||||||||||||||||
In Vivo | After a single oral dose of 12.5 mg per kg body weight in xenografts derived from RS4;11 cells (ALL), ABT-199 causes a maximal tumor growth inhibition (TGImax) of 47% (P<0.001) and tumor growth delay (TGD) of 26% (P<0.05)[1]. Treatment of established xenografted (a mouse xenograft model of the T-ALL cell line LOUCY) tumors with 100 mg ABT-199/kg for 4 days resulted in a significant reduction of leukemic burden (P=0.0048)[2]. | ||||||||||||||||
Solvent & Solubility | In Vitro: DMSO : 150 mg/mL (172.72 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) Ethanol : < 1 mg/mL (insoluble) Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. In Vivo:
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