Home > others & > CB-839

CB-839

CB839,CB 839

CB-839是Glutaminase(KGA和GAC)高效选择性、具口服活力抑制剂,对重组GAC的IC50值小于15nM。

目录号
EY1773
EY1773
EY1773
EY1773
纯度
99.65%
99.65%
99.65%
99.65%
规格
5 mg
10 mg
50 mg
100 mg
原价
885
1415
4412
6422
售价
885
1415
4412
6422
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    CB-839 is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. Phase 1.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    1 mM

  • 动物实验

    200 mg/kgp.o.

  • 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 AKm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] Gross MI, et al. Mol Cancer Ther. 2014, 13(4):890-901.

    分子式
    C26H24F3N7O3S
    分子量
    571.57
    CAS号
    1439399-58-2
    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
    NCT02071927 Acute Myeloid Leukemia (AML)|Acute Lymphocytic Leukemia (ALL) Drug: CB-839|Drug: CB-Aza Calithera Biosciences, Inc Phase 1 2014-03-01 2017-02-07
    NCT03047993 Myelodysplastic Syndrome|Other Diseases of Blood and Blood-forming Organs Drug: CB-839|Drug: Azacitidine M.D. Anderson Cancer Center|National Cancer Institute (NCI)|Calithera Biosciences, Inc Phase 1|Phase 2 2017-04-01 2017-02-06
    NCT02944435 Healthy Volunteers Drug: CB-839 Capsules|Drug: CB-839 Tablets Calithera Biosciences, Inc Phase 1 2016-10-01 2017-01-03
    NCT02071888 Non-Hodgkin's Lymphoma (NHL)|Multiple Myeloma|Waldenstrom's Macroglobulinemia (WM)|Diffuse Large B-cell Lymphoma (DLBCL),|Other B-cell NHL Subtypes, Including WM|T-cell NHL Drug: CB-839|Drug: CB-839 and low dose dexamethasone|Drug: CB-839, pomalidomide, and low dose dexamethasone Calithera Biosciences, Inc Phase 1 2014-02-01 2016-04-29
    NCT02861300 Colorectal Cancer|Colon Cancer|Rectal Cancer|Solid Tumor Drug: CB-839|Drug: Capecitabine Case Comprehensive Cancer Center Phase 1|Phase 2 2016-08-01 2016-09-28
    NCT02771626 Clear Cell Renal Cell Carcinoma|Melanoma|Non-small Cell Lung Cancer Drug: CB-839|Drug: Nivolumab Calithera Biosciences, Inc Phase 1|Phase 2 2016-08-01 2017-01-19
    NCT02071862 Solid Tumors|Triple-Negative Breast Cancer|Non Small Cell Lung Cancer|Renal Cell Carcinoma|Mesothelioma|Fumarate Hydratase (FH)-Deficient Tumors|Succinate Dehydrogenase (SDH)-Deficient Gastrointestinal Stromal Tumors (GIST)|Succinate Dehydrogenase (SDH)-Deficient Non-gastrointestinal Stromal Tumors|Tumors Harboring Isocitrate Dehydrogenase-1 (IDH1) and IDH2 Mutations|Tumors Harboring Amplifications in the cMyc Gene Drug: CB-839|Drug: Pac-CB|Drug: CBE|Drug: CB-Erl|Drug: CBD|Drug: CB-Cabo Calithera Biosciences, Inc Phase 1 2014-02-01 2016-08-18
    NCT03057600 Triple Negative Breast Cancer|TNBC - Triple-Negative Breast Cancer Drug: Pac-CB Calithera Biosciences, Inc Phase 2 2017-05-01 2017-02-17

    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。

  • 相关化合物库

  • 使用AMQUAR产品发表文献后请联系我们

相关推荐

X
  • 联系人 :
  • 收件地址 :
  • 电话号码 :
  • 单位名称 :
  • 产品货号 :
  • 产品规格 :
  • 发票抬头以及单位税号 :