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LY2835219

Abemaciclib methanesulfonate

LY2835219对CDK4和CDK6的IC50分别为2 nM和10 nM。

目录号
EY1264
EY1264
EY1264
EY1264
纯度
99.24%
99.24%
99.24%
99.24%
规格
5 mg
10 mg
50 mg
100 mg
原价
580
850
900
1350
售价
580
850
900
1350
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

    LY2835219 is an orally available inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM, respectively.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 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] Sanchez-Martinez et al. Mol Cancer Ther, 2011,10(11 Suppl), Abstract nr B234.

    分子式
    C28H36F2N8O3S
    分子量
    602.7
    CAS号
    1231930-82-7
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    80 mg/mL
    Water
    100 mg/mL
    Ethanol
    20 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
    NCT02014129 Neoplasm Metastasis|Lymphoma Drug: LY2835219 Eli Lilly and Company Phase 1 2013-12-01 2017-02-14
    NCT02327143 Healthy Volunteers Drug: LY2835219|Drug: ^13C-LY2835219 Eli Lilly and Company Phase 1 2015-01-01 2015-02-24
    NCT02059148 Healthy Volunteers Drug: LY2835219 Eli Lilly and Company Phase 1 2014-02-01 2014-11-19
    NCT02117648 Neoplasm|Neoplasm Metastasis Drug: LY2835219|Drug: Clarithromycin Eli Lilly and Company Phase 1 2014-04-01 2015-09-17
    NCT01913314 Healthy Volunteers Drug: [^14C]-LY2835219 Eli Lilly and Company Phase 1 2013-08-01 2014-11-19
    NCT02256267 Healthy Volunteers Drug: LY2835219|Drug: Rifampin Eli Lilly and Company Phase 1 2014-10-01 2014-12-17
    NCT01739309 Mantle Cell Lymphoma Drug: LY2835219 Eli Lilly and Company Phase 2 2013-03-01 2017-03-08
    NCT01394016 Advanced Cancer Drug: LY2835219|Drug: Fulvestrant Eli Lilly and Company Phase 1 2009-12-07 2017-03-20
    NCT02102490 Metastatic Breast Cancer Drug: Abemaciclib Eli Lilly and Company Phase 2 2014-06-01 2016-08-13
    NCT02450539 Non-Small Cell Lung Cancer Stage IV Drug: Abemaciclib|Drug: Docetaxel Eli Lilly and Company Phase 2 2015-08-01 2017-03-06
    NCT02246621 Breast Cancer Drug: Abemaciclib|Drug: Anastrozole|Drug: Letrozole|Drug: Placebo Eli Lilly and Company Phase 3 2014-11-01 2017-01-09
    NCT02441946 Breast Cancer|Hormone Receptor Positive Tumor|Early-Stage Breast Carcinoma Drug: Abemaciclib|Drug: Loperamide|Drug: Anastrozole Eli Lilly and Company Phase 2 2015-08-01 2017-01-24
    NCT02846987 Sarcoma|Dedifferentiated Liposarcoma Drug: Abemaciclib Memorial Sloan Kettering Cancer Center|Eli Lilly and Company Phase 2 2016-07-01 2016-12-22
    NCT02079636 Carcinoma, Non-small Cell Lung Drug: Abemaciclib|Drug: Pemetrexed|Drug: Gemcitabine|Drug: Ramucirumab|Drug: LY3023414|Drug: Pembrolizumab Eli Lilly and Company|Merck Sharp & Dohme Corp. Phase 1 2014-03-01 2017-03-21
    NCT02057133 Breast Neoplasms Drug: LY2835219|Drug: Letrozole|Drug: Anastrozole|Drug: Tamoxifen|Drug: Exemestane|Drug: Everolimus|Drug: Trastuzumab|Drug: LY3023414|Drug: Fulvestrant Eli Lilly and Company Phase 1 2014-03-01 2017-03-17
    NCT02763566 Breast Cancer Drug: Abemaciclib|Drug: Anastrozole|Drug: Letrozole|Drug: Placebo|Drug: Fulvestrant Eli Lilly and Company Phase 3 2016-12-01 2017-03-22
    NCT02482935 Healthy Drug: Abemaciclib Eli Lilly and Company Phase 1 2015-06-01 2015-10-16
    NCT02779751 Non Small Cell Lung Cancer|Breast Cancer Drug: Abemaciclib|Drug: Pembrolizumab Eli Lilly and Company|Merck Sharp & Dohme Corp. Phase 1 2016-11-14 2017-03-21
    NCT02152631 Non Small Cell Lung Cancer Drug: Abemaciclib|Drug: Erlotinib Eli Lilly and Company Phase 3 2014-09-01 2017-03-06
    NCT02675231 Hormone Receptor Positive Tumor|HER-2 Positive Breast Cancer Drug: Abemaciclib|Drug: Trastuzumab|Drug: Fulvestrant|Drug: Standard of Care Single Agent Chemotherapy Eli Lilly and Company Phase 2 2016-03-01 2017-03-22
    NCT02919696 Advanced Cancer|Metastatic Cancer Drug: Abemaciclib Eli Lilly and Company Phase 1 2017-04-17 2017-02-24
    NCT02747004 Metastatic Breast Cancer Drug: Abemaciclib|Drug: Tamoxifen|Drug: Prophylactic Loperamide Eli Lilly and Company Phase 2 2016-09-01 2017-03-21
    NCT02792725 Metastatic Breast Cancer Drug: Abemaciclib Eli Lilly and Company null 2017-03-23
    NCT02107703 Breast Neoplasms Drug: Abemaciclib|Drug: Fulvestrant|Drug: Placebo Eli Lilly and Company Phase 3 2014-07-01 2017-03-02
    NCT02308020 Breast Cancer|Non-small Cell Lung Cancer|Melanoma|Brain Metastases Drug: Abemaciclib Eli Lilly and Company Phase 2 2015-04-01 2017-03-03
    NCT02387814 Hepatic Insufficiency|Healthy Drug: Abemaciclib Eli Lilly and Company Phase 1 2015-03-01 2015-09-10

    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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