Galunisertib是有效的TGFβ receptor I (TβRI)抑制剂,IC50为56 nM。
LY2157299 is a potent small-molecule antagonist that specifically inhibits Transforming Growth Factor-β receptor I (TβRI). LY2157299 is now under phase II clinical evaluation of its anti-carcinoma activity against hepatocellular carcinoma and glioblastoma1.
溶解于DMSO中并稀释于生理盐水
75 mg/kg/day 口服
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] Mundla SR, Patent, 2006, US7872020.
分子式 C22H19N5O |
分子量 369.42 |
CAS号 700874-72-2 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 75 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02752919 | Healthy | Drug: Galunisertib | Eli Lilly and Company | Phase 1 | 2016-04-01 | 2016-06-30 |
NCT02304419 | Neoplasm | Drug: Galunisertib | Eli Lilly and Company | Phase 1 | 2015-05-01 | 2016-10-04 |
NCT02734160 | Metastatic Pancreatic Cancer | Drug: Galunisertib|Drug: Durvalumab | Eli Lilly and Company|AstraZeneca | Phase 1 | 2016-06-01 | 2016-12-06 |
NCT03081377 | Hepatocellular Carcinoma | Drug: Galunisertib 150mg by mouth twice a day|Radiation: SBRT | University of Pennsylvania | Phase 1 | 2017-04-01 | 2017-03-10 |
NCT02423343 | Solid Tumor|Non-Small Cell Lung Cancer Recurrent|Hepatocellular Carcinoma Recurrent|Glioblastoma | Drug: Galunisertib|Drug: Nivolumab | Eli Lilly and Company|Bristol-Myers Squibb | Phase 1|Phase 2 | 2015-10-01 | 2017-03-22 |
NCT02672475 | Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma | Drug: Galunisertib|Other: Laboratory Biomarker Analysis|Drug: Paclitaxel | Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) | Phase 1 | 2016-03-01 | 2016-10-14 |
NCT02240433 | Hepatocellular Carcinoma | Drug: LY2157299|Drug: Sorafenib | Eli Lilly and Company | Phase 1 | 2014-11-01 | 2017-02-01 |
NCT02688712 | Rectal Adenocarcinoma | Drug: LY2157299|Drug: Capecitabine|Drug: Fluorouracil|Procedure: Tumor specific mesorectal excision | Providence Health & Services|Eli Lilly and Company | Phase 2 | 2016-06-01 | 2016-06-23 |
NCT02154646 | Pancreatic Neoplasms | Drug: LY2157299|Drug: Gemcitabine | Eli Lilly and Company | Phase 1 | 2014-05-01 | 2016-02-09 |
NCT01965808 | Healthy Volunteers | Drug: LY2157299 | Eli Lilly and Company | Phase 1 | 2013-10-01 | 2013-12-03 |
NCT01722825 | Neoplasms|Neoplasm Metastasis | Drug: LY2157299 | Eli Lilly and Company | Phase 1 | 2012-11-01 | 2014-06-30 |
NCT02906397 | ADVANCED HEPATOCELLULAR CARCINOMA (HCC) | Drug: Galunisertib (LY2157299) | Abramson Cancer Center of the University of Pennsylvania | Phase 1 | 2016-11-01 | 2016-09-15 |
NCT02452008 | Prostate Cancer | Drug: Enzalutamide|Drug: LY2157299 | Sidney Kimmel Comprehensive Cancer Center | Phase 2 | 2016-04-01 | 2016-08-22 |
NCT02008318 | Myelodysplastic Syndromes | Drug: LY2157299|Drug: Placebo | Eli Lilly and Company | Phase 2|Phase 3 | 2014-03-01 | 2016-08-13 |
NCT02178358 | Hepatocellular Carcinoma | Drug: LY2157299|Drug: Sorafenib|Drug: Placebo | Eli Lilly and Company | Phase 2 | 2014-08-01 | 2016-08-18 |
NCT01582269 | Glioblastoma | Drug: LY2157299 monohydrate|Drug: Lomustine|Drug: Placebo | Eli Lilly and Company | Phase 2 | 2012-04-01 | 2016-07-05 |
NCT01220271 | Glioma | Drug: LY2157299|Drug: Radiation|Drug: Temozolomide | Eli Lilly and Company | Phase 1|Phase 2 | 2011-04-01 | 2017-02-15 |
NCT01246986 | Carcinoma, Hepatocellular | Drug: LY2157299|Drug: Sorafenib|Drug: Ramucirumab | Eli Lilly and Company | Phase 2 | 2011-03-01 | 2017-03-01 |
NCT02538471 | Metastatic Breast Cancer | Radiation: Radiation therapy|Drug: Study Drug | Weill Medical College of Cornell University|University of California, Los Angeles | Phase 2 | 2015-08-01 | 2017-03-20 |
NCT01682187 | Glioma | Drug: LY2157299|Drug: Lomustine | Eli Lilly and Company | Phase 1 | 2005-12-01 | 2017-01-06 |
NCT01373164 | Neoplasms|Neoplasm Metastasis|Pancreatic Cancer | Drug: LY2157299|Drug: Gemcitabine|Drug: Placebo | Eli Lilly and Company | Phase 1|Phase 2 | 2011-06-01 | 2017-01-16 |
NCT02981342 | Pancreatic Ductal Adenocarcinoma | Drug: Abemaciclib|Drug: LY3023414|Drug: Galunisertib|Drug: Gemcitabine|Drug: Capecitabine | Eli Lilly and Company | Phase 2 | 2017-01-01 | 2017-03-23 |
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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