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AT101

(R)-(-)-Gossypol acetic acid,(-)-Gossypol acetic acid,(R)-Gossypol acetic acid

AT101乙酸盐对Bcl-2， Bcl-xL和Mcl-1的结合Ki值分别为0.32，0.48和0.18uM。

目录号
EY1786
EY1786
EY1786
纯度
99.25%
99.25%
99.25%
规格
5 mg
10 mg
50 mg
原价
672
1020
3065
售价
672
1020
3065
库存
现货
现货
现货
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  • 生物活性

    AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. Phase 2.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    10 μM

  • 动物实验

    100 mg/kg 口服饲喂

  • 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] Wang G, et al. J Med Chem. 2006, 49(21), 6139-6142.

    分子式
    C32H34O10    		 分子量
    578.61    		 CAS号
    866541-93-7    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    200 mM    		 Water
    <1 mg/mL    		 Ethanol
    150 mM

    体内溶解度

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

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00934076 Carcinoma, Non Small Cell Lung Drug: Tarceva plus AT-101 University of Alabama at Birmingham|Ascenta Therapeutics Phase 1 2010-02-01 2015-05-06
    NCT00286780 Chronic Lymphocytic Leukemia Drug: AT-101 Ascenta Therapeutics Phase 2 2006-01-01 2010-08-12
    NCT00286793 Prostate Cancer Drug: AT-101 Ascenta Therapeutics Phase 1|Phase 2 2006-02-01 2011-06-27
    NCT00561197 Locally Advanced Esophageal or GE Junction Cancer Drug: AT-101 Ascenta Therapeutics Phase 1|Phase 2 2007-08-01 2013-01-03
    NCT00988169 Lung Cancer Drug: oral erlotinib and pulsed doses of oral AT-101 Memorial Sloan Kettering Cancer Center|Ascenta Therapeutics Phase 2 2009-09-01 2015-10-19
    NCT00848016 Recurrent Adrenocortical Carcinoma|Stage III Adrenocortical Carcinoma|Stage IV Adrenocortical Carcinoma Drug: R-(-)-gossypol acetic acid National Cancer Institute (NCI) Phase 2 2009-02-01 2014-04-17
    NCT00666666 Adenocarcinoma of the Prostate|Stage IV Prostate Cancer Drug: AT-101|Drug: Bicalutamide|Other: LHRH agent National Cancer Institute (NCI) Phase 2 2009-07-01 2014-12-17
    NCT01003769 Recurrent Chronic Lymphocytic Leukemia Drug: Lenalidomide|Drug: R-(-)-Gossypol Acetic Acid|Other: Laboratory Biomarker Analysis Mayo Clinic|National Cancer Institute (NCI) Phase 1|Phase 2 2013-09-01 2016-06-20
    NCT00544960 Non-small Cell Lung Cancer Drug: AT-101 and docetaxel|Drug: placebo and docetaxel Ascenta Therapeutics Phase 2 2007-09-01 2010-08-24
    NCT00571675 Hormone Refractory Prostate Cancer Drug: AT-101, prednisone and docetaxel|Drug: placebo, prednisone and docetaxel Ascenta Therapeutics Phase 2 2007-10-01 2010-11-08
    NCT00397293 Small Cell Lung Cancer Drug: AT-101|Drug: topotecan Ascenta Therapeutics Phase 1|Phase 2 2006-11-01 2010-08-20
    NCT00440388 Follicular Lymphoma Drug: AT-101|Drug: Rituximab Ascenta Therapeutics Phase 2 2006-10-01 2010-08-24
    NCT00275431 Follicular Lymphoma|Diffuse Large Cell Lymphoma|Mantle Cell Lymphoma|Small Lymphocytic Lymphoma|Chronic Lymphocytic Leukemia Drug: AT-101 Ascenta Therapeutics Phase 2 2005-11-01 2011-06-24
    NCT00540722 Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Tumor Drug: R-(-)-gossypol acetic acid|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2008-01-01 2016-12-27
    NCT01285635 Squamous Cell Carcinoma of the Head and Neck (SCCHN) Drug: AT-101|Drug: Docetaxel University of Michigan Cancer Center Phase 2 2010-06-01 2016-03-03
    NCT00544596 Extensive Stage Small Cell Lung Cancer|Unspecified Adult Solid Tumor, Protocol Specific Drug: R-(-)-gossypol acetic acid|Drug: cisplatin|Drug: etoposide National Cancer Institute (NCI) Phase 1 2007-09-01 2014-04-01
    NCT00286806 Hormone Refractory Prostate Cancer Drug: AT-101 Ascenta Therapeutics Phase 1|Phase 2 2005-12-01 2010-08-20
    NCT00773955 Extensive Stage Small Cell Lung Cancer|Recurrent Small Cell Lung Cancer Drug: R-(-)-gossypol acetic acid|Other: pharmacological study|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2008-11-01 2014-04-23
    NCT01633541 Laryngeal Cancer Drug: AT-101|Drug: Docetaxel|Drug: Cisplatin|Drug: Carboplatin University of Michigan Cancer Center Phase 2 2012-03-01 2016-09-13
    NCT02697344 Recurrent Plasma Cell Myeloma Drug: Dexamethasone|Other: Laboratory Biomarker Analysis|Drug: Lenalidomide|Other: Pharmacological Study|Drug: R-(-)-Gossypol Acetic Acid Mayo Clinic|National Cancer Institute (NCI) Phase 1|Phase 2 2016-04-01 2016-10-20
    NCT00891072 Adult Grade III Lymphomatoid Granulomatosis|Adult Nasal Type Extranodal NK/T-cell Lymphoma|Contiguous Stage II Adult Burkitt Lymphoma|Contiguous Stage II Adult Diffuse Large Cell Lymphoma|Contiguous Stage II Adult Diffuse Mixed Cell Lymphoma|Contiguous Stage II Adult Diffuse Small Cleaved Cell Lymphoma|Contiguous Stage II Adult Immunoblastic Large Cell Lymphoma|Contiguous Stage II Adult Lymphoblastic Lymphoma|Contiguous Stage II Grade 1 Follicular Lymphoma|Contiguous Stage II Grade 2 Follicular Lymphoma|Contiguous Stage II Grade 3 Follicular Lymphoma|Contiguous Stage II Mantle Cell Lymphoma|Contiguous Stage II Marginal Zone Lymphoma|Contiguous Stage II Small Lymphocytic Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Noncontiguous Stage II Adult Burkitt Lymphoma|Noncontiguous Stage II Adult Diffuse Large Cell Lymphoma|Noncontiguous Stage II Adult Diffuse Mixed Cell Lymphoma|Noncontiguous Stage II Adult Diffuse Small Cleaved Cell Lymphoma|Noncontiguous Stage II Adult Immunoblastic Large Cell Lymphoma|Noncontiguous Stage II Adult Lymphoblastic Lymphoma|Noncontiguous Stage II Grade 1 Follicular Lymphoma|Noncontiguous Stage II Grade 2 Follicular Lymphoma|Noncontiguous Stage II Grade 3 Follicular Lymphoma|Noncontiguous Stage II Mantle Cell Lymphoma|Noncontiguous Stage II Marginal Zone Lymphoma|Noncontiguous Stage II Small Lymphocytic Lymphoma|Peripheral T-cell Lymphoma|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Grade III Lymphomatoid Granulomatosis|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Small Lymphocytic Lymphoma|Splenic Marginal Zone Lymphoma|Stage I Adult Burkitt Lymphoma|Stage I Adult Diffuse Large Cell Lymphoma|Stage I Adult Diffuse Mixed Cell Lymphoma|Stage I Adult Diffuse Small Cleaved Cell Lymphoma|Stage I Adult Immunoblastic Large Cell Lymphoma|Stage I Adult Lymphoblastic Lymphoma|Stage I Grade 1 Follicular Lymphoma|Stage I Grade 2 Follicular Lymphoma|Stage I Grade 3 Follicular Lymphoma|Stage I Mantle Cell Lymphoma|Stage I Marginal Zone Lymphoma|Stage I Small Lymphocytic Lymphoma|Stage III Adult Burkitt Lymphoma|Stage III Adult Diffuse Large Cell Lymphoma|Stage III Adult Diffuse Mixed Cell Lymphoma|Stage III Adult Diffuse Small Cleaved Cell Lymphoma|Stage III Adult Immunoblastic Large Cell Lymphoma|Stage III Adult Lymphoblastic Lymphoma|Stage III Grade 1 Follicular Lymphoma|Stage III Grade 2 Follicular Lymphoma|Stage III Grade 3 Follicular Lymphoma|Stage III Mantle Cell Lymphoma|Stage III Marginal Zone Lymphoma|Stage III Small Lymphocytic Lymphoma|Stage IV Adult Burkitt Lymphoma|Stage IV Adult Diffuse Large Cell Lymphoma|Stage IV Adult Diffuse Mixed Cell Lymphoma|Stage IV Adult Diffuse Small Cleaved Cell Lymphoma|Stage IV Adult Immunoblastic Large Cell Lymphoma|Stage IV Adult Lymphoblastic Lymphoma|Stage IV Grade 1 Follicular Lymphoma|Stage IV Grade 2 Follicular Lymphoma|Stage IV Grade 3 Follicular Lymphoma|Stage IV Mantle Cell Lymphoma|Stage IV Marginal Zone Lymphoma|Stage IV Small Lymphocytic Lymphoma|Unspecified Adult Solid Tumor, Protocol Specific|Waldenstrm Macroglobulinemia Drug: R-(-)-gossypol acetic acid|Drug: paclitaxel|Drug: carboplatin|Other: pharmacological study National Cancer Institute (NCI) Phase 1 2009-07-01 2013-01-09
    NCT01977209 Non-small Cell Lung Cancer Drug: Gossypol|Drug: Placebo Third Military Medical University Phase 3 2013-09-01 2013-10-30

    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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