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Obatoclax Mesylate

甲磺酸奥巴克拉,GX15-070

Obatoclax (GX15-070)是Bcl-2 homology domain-3 (BH3)的类似物，对各种抗凋亡的Bcl-2家族蛋白的IC50平均为3 uM，如对Mcl-1(IC50为2.9 uM)和Bfl-1(IC50为5 uM)。

目录号
EY1271
EY1271
EY1271
EY1271
纯度
99.32%
99.32%
99.32%
99.32%
规格
2 mg
5 mg
10 mg
50 mg
原价
580
920
1520
4900
售价
580
920
1520
4900
库存
现货
现货
现货
现货
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订购
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  • 生物活性

    The mesylate salt form of Obatoclax (GX015-070) is a synthetic small molecule inhibitor of Bcl-2 family members, including Bcl-2, Bcl-xl, Mcl-1, Bcl-w, A1, and Bcl-b, with Ki values ranging from 1-7 μM.

  • 体外研究

  • 体内研究

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

  • 激酶实验

  • 细胞实验

    10 μM 左右

  • 动物实验

    0.0313, 0.25, 0.5，和2 mg/kg在鼠尾部静脉注射，每天一次。

  • 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] Nguyen M, et al. Proc Natl Acad Sci, 2007, 104(49), 19512-191517.

    分子式
    C21H23N3O4S    		 分子量
    413.49    		 CAS号
    803712-79-0    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    83 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    2 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
    NCT00427856 Lymphoma, Follicular Drug: Obatoclax mesylate|Drug: Rituximab Gemin X|Teva Pharmaceutical Industries Phase 2 2007-03-01 2016-07-20
    NCT00521144 Recurrent Small Cell Lung Cancer|Unspecified Adult Solid Tumor, Protocol Specific Drug: obatoclax mesylate|Drug: topotecan hydrochloride|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 1|Phase 2 2007-08-01 2015-04-14
    NCT00413114 Myelodysplastic Syndromes Drug: Obatoclax mesylate (GX15-070MS) Gemin X|Teva Pharmaceutical Industries Phase 2 2006-12-01 2013-08-16
    NCT01563601 Extensive-stage Small Cell Lung Cancer Drug: Obatoclax Mesylate, Carboplatine and Etoposide|Drug: Carboplatin and Etoposide Cephalon|Teva Pharmaceutical Industries Phase 3 2012-08-01 2012-08-14
    NCT00600964 Chronic Lymphocytic Leukemia Drug: GX15-070MS|Drug: GX15-070MS Gemin X|Teva Pharmaceutical Industries Phase 1 2004-09-01 2014-05-09
    NCT00359892 Hodgkin's Lymphoma Drug: Obatoclax mesylate (GX15-070MS) Gemin X|Teva Pharmaceutical Industries Phase 2 2006-07-01 2012-08-03
    NCT00405951 Lung Cancer Drug: Obatoclax mesylate 250 ml|Drug: Docetaxel Gemin X|Teva Pharmaceutical Industries Phase 1|Phase 2 2006-10-01 2016-07-19
    NCT00360035 Myelofibrosis Drug: Obatoclax mesylate (GX15-070MS) Gemin X|Teva Pharmaceutical Industries Phase 2 2006-07-01 2013-08-16
    NCT00918931 Leukemia|Systemic Mastocytosis Drug: Obatoclax Mesylate M.D. Anderson Cancer Center|Gemin X Phase 2 2009-06-01 2011-10-14
    NCT00407303 Mantle-Cell Lymphoma Drug: Obatoclax mesylate|Drug: Bortezomib Gemin X|Teva Pharmaceutical Industries Phase 1|Phase 2 2006-10-01 2016-07-19
    NCT00438178 Hematological Malignancies Drug: Obatoclax mesylate (GX15-070MS) Gemin X|Teva Pharmaceutical Industries Phase 1 2005-10-01 2014-05-09
    NCT00612612 B-cell Chronic Lymphocytic Leukemia|Leukemia|Prolymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia|Stage I Chronic Lymphocytic Leukemia|Stage II Chronic Lymphocytic Leukemia|Stage III Chronic Lymphocytic Leukemia|Stage IV Chronic Lymphocytic Leukemia Drug: obatoclax mesylate|Drug: fludarabine phosphate|Biological: rituximab|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 1 2008-01-01 2013-09-27
    NCT01238146 Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Splenic Marginal Zone Lymphoma Drug: bendamustine hydrochloride|Drug: obatoclax mesylate|Biological: rituximab National Cancer Institute (NCI) Phase 1|Phase 2 2010-10-01 2013-06-05
    NCT00933985 Acute Leukemias of Ambiguous Lineage|Acute Undifferentiated Leukemia|Angioimmunoblastic T-cell Lymphoma|Blastic Phase Chronic Myelogenous Leukemia|Childhood Burkitt Lymphoma|Childhood Chronic Myelogenous Leukemia|Childhood Diffuse Large Cell Lymphoma|Childhood Immunoblastic Large Cell Lymphoma|Childhood Nasal Type Extranodal NK/T-cell Lymphoma|Cutaneous B-cell Non-Hodgkin Lymphoma|Hepatosplenic T-cell Lymphoma|Intraocular Lymphoma|Noncutaneous Extranodal Lymphoma|Peripheral T-cell Lymphoma|Recurrent Childhood Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Myeloid Leukemia|Recurrent Childhood Anaplastic Large Cell Lymphoma|Recurrent Childhood Grade III Lymphomatoid Granulomatosis|Recurrent Childhood Large Cell Lymphoma|Recurrent Childhood Lymphoblastic Lymphoma|Recurrent Childhood Small Noncleaved Cell Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent/Refractory Childhood Hodgkin Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Hairy Cell Leukemia|Relapsing Chronic Myelogenous Leukemia|Small Intestine Lymphoma|Unspecified Childhood Solid Tumor, Protocol Specific Drug: dexrazoxane hydrochloride|Drug: doxorubicin hydrochloride|Drug: obatoclax mesylate|Drug: liposomal vincristine sulfate|Other: pharmacological study|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 1 2009-06-01 2014-04-30
    NCT00719901 Refractory Multiple Myeloma|Stage I Multiple Myeloma|Stage II Multiple Myeloma|Stage III Multiple Myeloma Drug: obatoclax mesylate|Drug: bortezomib|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 1|Phase 2 2008-07-01 2015-01-09
    NCT01150656 Leukemia Genetic: gene expression analysis|Genetic: microarray analysis|Genetic: protein expression analysis|Genetic: reverse transcriptase-polymerase chain reaction|Genetic: western blotting|Other: laboratory biomarker analysis|Other: pharmacological study Children's Oncology Group|National Cancer Institute (NCI) 2010-06-01 2016-05-17
    NCT00724841 Metastatic Melanoma Drug: Obatoclax Mesylate|Drug: Temozolomide Gemin X|Teva Pharmaceutical Industries Phase 1|Phase 2 2008-06-01 2016-07-20
    NCT00684918 AML Drug: Obatoclax Gemin X|Teva Pharmaceutical Industries Phase 2 2008-04-01 2013-08-16
    NCT00682981 Extensive-stage Small Cell Lung Cancer Drug: Obatoclax|Drug: Carboplatin/etoposide Gemin X|Cephalon|Teva Pharmaceutical Industries Phase 1|Phase 2 2008-05-01 2016-07-19

    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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