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ABT-199 (D50750)  
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2mg/480.00元
10mg/1480.00元
大包装/询价
产品编号 D50750
英文名称 ABT-199
中文名称
别    名   BCL-2 抑制剂
克 隆 号
CAS 1257044-40-8
理论分子量 868.44 kDa
检测分子量
性    状 Lyophilized
保存条件 Store in dry, dark place for one year.
注意事项 This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications.
产品介绍 ABT-199 is a highly potent, selective, and orally bioavailable BCL-2 inhibitor. ABT-199 has picomolar affinity for BCL-2 (Ki < 0.010 nM) and > 1000 folds selectivity over BCL-XL (Ki = 48 nM) and BCL-W (Ki = 245 nM). Therefore, ABT-199 is a much improved lead compound over the original ABT-263 (navitoclax) to avoid thrombocytopenia caused by BCL-XL inhibition. ABT-199’s cell-killing effect is selective and mechanism dependent. It can potently kill BCL-2-overexpressing FL5.12 cells (EC50 ~ 4 nM) and RS4;11 BCL-2–dependent ALL cells (EC50 ~8 nM), but showed much weaker activity against BCL-XL-overexpressing FL5.12 cells (EC50 ~261 nM) and H146 ALL cells (EC50 ~4, 260 nM). ABT-199 inhibits the growth of BCL-2–dependent human hematological tumors in vivo and spares human platelets as a single agent or in combination with rituximab and bendamustine. A single dose of ABT-199 in three patients with refractory chronic lymphocytic leukemia resulted in tumor lysis within 24 h. These data indicates that selective pharmacological inhibition of BCL-2 shows promise for the treatment of BCL-2–dependent hematological cancers.

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