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ABT-199

ABT199,GDC-0199,ABT 199,GDC 0199,GDC0199,Venetoclax

ABT-199 (GDC-0199)是一种Bcl-2选择性抑制剂，Ki为<0.01 nM，比作用于Bcl-xL和Bcl-w选择性高4800倍以上，对Mcl-1没有抑制活性。

目录号
EY0728
EY0728
EY0728
EY0728
纯度
99.14%
99.14%
99.14%
99.14%
规格
1 mg
5 mg
10 mg
50 mg
原价
120
490
720
988
售价
120
490
720
988
库存
现货
现货
现货
现货
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  • 生物活性

    ABT-199, developed through a structure-based reverse engineering process, is a novel and specific inhibitor of B-cell lymphoma/leukemia 2 (BCL-2) maintaining a sub-nanomolar affinity towards BCL-2 and over three orders of magnitude less affinity towards BCL-XL. It kills a diverse array of non-Hodgkin lymphoma (NHL) and acute myelogenous leukemia cell lines as well as BCL-2 dependent but not BCL-XL dependent cells via suppressing mitochondrial pathway of apoptosis, exhibiting potent antitumor activity against a wide variety of hematologic malignancies while sparing platelets. According to previous studies, ABT-199 is capable of suppressing tumor growth in several human hematologic tumor xenograft models.

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% Propylene glycol

  • 激酶实验

  • 细胞实验

    ~1 μM

  • 动物实验

    ~100 mg/kg 口服处理

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Souers AJ, et al. Nat Med, 2013, 19(2), 202-208.

    分子式
    C45H50ClN7O7S    		 分子量
    868.44    		 CAS号
    1257044-40-8    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度
    5 mg/mL

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01969682 Non-Hodgkin's Lymphoma Drug: ABT-199|Drug: Rifampin AbbVie|Genentech, Inc. Phase 1 2014-04-01 2014-05-22
    NCT01969669 Non-Hodgkin's Lymphoma Drug: ABT-199|Drug: Ketoconazole AbbVie|Genentech, Inc. Phase 1 2013-12-01 2014-10-14
    NCT02419560 Lymphoma, Mantle-Cell|Recurrent Lymphoma, Mantle-Cell Drug: ABT-199 and Ibrutinib Combination Craig Portell, MD|AbbVie|University of Virginia Phase 1 2015-04-01 2017-03-16
    NCT01969695 Non-Hodgkin's Lymphoma Drug: ABT-199 AbbVie|Genentech, Inc. Phase 1 2013-12-01 2017-01-18
    NCT02095574 Relapsed/Refractory Non-Hodgkin's Lymphoma Drug: [14C]ABT-199 (GDC-0199) AbbVie|Genentech, Inc. Phase 1 2014-09-01 2014-08-12
    NCT02677324 Waldenstrom Macroglobulinemia Drug: ABT199 Dana-Farber Cancer Institute|AbbVie Phase 2 2016-04-01 2016-09-26
    NCT01682616 Small Lymphocytic Lymphoma|Chronic Lymphocytic Leukemia Drug: ABT-199|Drug: Rituximab AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 1 2012-08-01 2017-01-09
    NCT02141282 Chronic Lymphocytic Leukemia Drug: ABT-199 AbbVie|Genentech/Roche Phase 2 2014-09-01 2017-01-23
    NCT01328626 Chronic Lymphocytic Leukemia|Non-Hodgkin Lymphoma Drug: ABT-199 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 1 2011-06-01 2017-01-25
    NCT01994837 Acute Myelogenous Leukemia|AML|Acute Myeloid Leukemia Drug: ABT-199 AbbVie|Genentech, Inc. Phase 2 2013-11-01 2015-12-18
    NCT01794507 Relapsed/Refractory Multiple Myeloma Drug: ABT-199|Drug: bortezomib|Drug: dexamethasone AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 1 2012-11-01 2017-01-06
    NCT02401503 Chronic Lymphocytic Leucemia Drug: Bendamustine|Drug: GA101|Drug: ABT-199 German CLL Study Group Phase 2 2015-05-01 2016-09-23
    NCT01794520 Relapsed/Refractory Multiple Myeloma Drug: ABT-199|Drug: Dexamethasone AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 1 2012-10-01 2017-01-23
    NCT01594229 Non-Hodgkin's Lymphoma Drug: ABT-199|Drug: Bendamustine|Drug: Rituximab AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 1 2012-06-01 2017-01-06
    NCT02471391 Mantle Cell Lymphoma Drug: ABT-199|Drug: Ibrutinib Peter MacCallum Cancer Centre, Australia Phase 2 2015-06-01 2015-08-27
    NCT03000660 AL Amyloidosis Drug: Venetoclax|Drug: Dexamethasone Tufts Medical Center Phase 1 2017-01-01 2017-01-10
    NCT02203773 Acute Myelogenous Leukemia|Myelogenous Leukemia|Treatment Naive AML Drug: ABT-199|Drug: Decitabine|Drug: Azacitidine|Drug: Posaconazole AbbVie|Genentech, Inc. Phase 1 2014-11-01 2017-01-17
    NCT01889186 Chronic Lymphocytic Leukemia|17 p Deletion|Cancer of the Blood and Bone Marrow Drug: ABT-199 AbbVie|Genentech, Inc. Phase 2 2013-06-01 2017-03-13
    NCT01686555 Lupus Erythematosus Drug: ABT-199|Other: Placebo AbbVie (prior sponsor, Abbott)|AbbVie Phase 1 2012-11-01 2015-07-07
    NCT02558816 Mantle Cell Lymphoma Drug: Ibrutinib + GA101 +GDC-0199 Nantes University Hospital|Janssen, LP|Roche Pharma AG Phase 1|Phase 2 2015-10-14 2017-01-27
    NCT01685892 Lymphocytic Leukemia, Chronic Drug: Obinutuzumab|Drug: Venetoclax (GDC-0199; ABT-199) Genentech, Inc.|AbbVie (prior sponsor, Abbott) Phase 1 2012-11-01 2016-11-01

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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