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ABT-263

Navitoclax

ABT-263 (Navitoclax)是一种有效的Bcl-xL， Bcl-2和Bcl-w抑制剂，Ki分别为≤0.5 nM，≤1 nM和≤1 nM，但与Mcl-1和A1结合微弱。

目录号
EY1403
EY1403
EY1403
EY1403
纯度
99.36%
99.36%
99.36%
99.36%
规格
5 mg
10 mg
50 mg
100 mg
原价
590
920
2400
3200
售价
590
920
2400
3200
库存
现货
现货
现货
现货
订购
订购
订购
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  • 生物活性

    ABT-263 is an orally sellecitive inhibitor of B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity. ABT-263 is a small molecular with the formula of C47H55ClF3N5O6S3 and Molecular Weight of 974. As a Bad-like Bh3 minetic, ABT-263 binds to Bcl-2 family proteins Bcl-2, Bcl-xl and Bcl-w, disrupts the interaction between Bcl-2/Bcl-xl /Bcl-w and pro-apoptotic proteins such as Bim, Bad and Bak, which trigger the caspases-initiated cell death pathway to induce apoptosis.

  • 体外研究

  • 体内研究

    10% Ethanol +30% PEG400+60% Phosal 50 PG

  • 激酶实验

  • 细胞实验

    0-1 μM

  • 动物实验

    100 mg/kg/d 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] Tse C, et al. Cancer Res. 2008, 68(9), 3421-3428.
    [2] Adams, J., et al.: Science, 281, 1322 (1998)

    分子式
    C47H55ClF3N5O6S3    		 分子量
    974.61    		 CAS号
    923564-51-6    		 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

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

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00788684 CD20-Positive Lymphoid Malignancies|Chronic Lymphoid Leukemia|Hematological Malignancies|Non-Hodgkin's Lymphoma Drug: ABT-263|Drug: rituximab AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 1 2009-07-01 2017-01-04
    NCT01021358 Lymphoma|Chronic Lymphocytic Leukemia|Solid Tumors Drug: ABT-263|Drug: Ketoconazole Abbott Phase 1 2010-01-01 2010-12-16
    NCT00887757 Solid Tumors Drug: ABT-263|Drug: gemcitabine Abbott|Genentech, Inc. Phase 1 2009-09-01 2011-12-21
    NCT02591095 Platinum-resistant or Refractory Ovarian Cancer Drug: ABT-263 Centre Francois Baclesse|ARCAGY/ GINECO GROUP|French Cancer Research Hospital Program Phase 2 2016-01-01 2016-10-05
    NCT00891605 Solid Tumors Drug: ABT-263|Drug: paclitaxel Abbott|Genentech, Inc. Phase 1 2009-07-01 2012-08-07
    NCT00918450 B-cell Chronic Lymphocytic Leukemia Drug: ABT-263 Abbott|Genentech, Inc. Phase 2 2010-03-01 2010-02-25
    NCT00868413 Chronic Lymphocytic Leukemia Drug: ABT-263|Drug: FCR|Drug: BR AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 1 2009-11-01 2013-06-05
    NCT00888108 Solid Tumor Drug: ABT-263|Drug: Docetaxel Abbott|Genentech, Inc. Phase 1 2009-07-01 2012-05-18
    NCT00878449 Solid Tumors Drug: ABT-263|Drug: etoposide/cisplatin AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 1 2009-10-01 2013-01-24
    NCT01121133 Lymphoma, Including Chronic Lymphocytic Leukemia|Solid Tumors Drug: navitoclax|Drug: Rifampin Abbott Phase 1 2010-05-01 2011-06-04
    NCT00406809 Chronic Lymphoid Leukemia|Lymphoid Malignancies|Non-Hodgkin's Lymphoma|Follicular Lymphoma|Mantle Cell Lymphoma|Peripheral T-cell Lymphoma Drug: ABT-263 AbbVie (prior sponsor, Abbott)|AbbVie Phase 2 2006-11-01 2016-11-10
    NCT00743028 Chronic Lymphocytic Leukemia|Lymphomas|Leukemias Drug: ABT-263|Drug: ABT-263|Drug: ABT-263 Abbott|Genentech, Inc. Phase 1 2008-08-01 2010-10-06
    NCT01557777 Chronic Lymphocytic Leukemia Drug: Navitoclax AbbVie (prior sponsor, Abbott)|AbbVie Phase 2 2012-06-01 2014-07-02
    NCT00481091 Chronic Lymphocytic Leukemia Drug: ABT-263 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 2 2007-07-01 2017-01-04
    NCT00445198 Small Cell Lung Cancer|Small Cell Lung Carcinoma Drug: ABT-263 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 1|Phase 2 2007-04-01 2013-01-17
    NCT01009073 Solid Tumors Drug: ABT-263|Drug: erlotinib|Drug: irinotecan (3-week schedule)|Drug: irinotecan (weekly schedule) AbbVie (prior sponsor, Abbott)|AbbVie Phase 1 2009-10-01 2013-07-02
    NCT01087151 Chronic Lymphocytic Leukemia Drug: ABT-263|Drug: rituximab Genentech, Inc.|AbbVie (prior sponsor, Abbott) Phase 2 2010-08-01 2016-11-01
    NCT02143401 Recurrent Hepatocellular Carcinoma|Solid Neoplasm|Stage IV Hepatocellular Carcinoma Other: Laboratory Biomarker Analysis|Biological: Navitoclax|Other: Pharmacological Study|Drug: Sorafenib Tosylate National Cancer Institute (NCI) Phase 1 2014-11-01 2016-12-28
    NCT00982566 Lymphoid Malignancies|Solid Tumors Drug: ABT-263|Drug: ABT-263|Drug: ABT-263|Drug: ABT-263 Abbott|Genentech, Inc. Phase 1 2009-10-01 2011-01-27
    NCT02079740 Advanced Malignant Solid Neoplasm|KRAS Gene Mutation|Metastatic Malignant Solid Neoplasm|NRAS Gene Mutation|Recurrent Colorectal Carcinoma|Recurrent Lung Carcinoma|Recurrent Pancreatic Carcinoma|Stage III Colorectal Cancer|Stage III Lung Cancer|Stage III Pancreatic Cancer|Stage IIIA Colorectal Cancer|Stage IIIB Colorectal Cancer|Stage IIIC Colorectal Cancer|Stage IV Colorectal Cancer|Stage IV Lung Cancer|Stage IV Pancreatic Cancer|Stage IVA Colorectal Cancer|Stage IVB Colorectal Cancer Other: Laboratory Biomarker Analysis|Biological: Navitoclax|Other: Pharmacological Study|Drug: Trametinib National Cancer Institute (NCI) Phase 1|Phase 2 2014-03-01 2017-03-13

    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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