LY2835219对CDK4和CDK6的IC50分别为2 nM和10 nM。
LY2835219 is an orally available inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM, respectively.
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。
[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
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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