Home > TGF-betaR1(ALK5) & > Galunisertib

Galunisertib

LY2157299

Galunisertib是有效的TGFβ receptor I (TβRI)抑制剂,IC50为56 nM。

目录号
EY1774
EY1774
EY1774
EY1774
EY1774
纯度
99.69%
99.69%
99.69%
99.69%
99.69%
规格
2 mg
5 mg
10 mg
50 mg
100 mg
原价
400
650
880
3420
6105
售价
400
650
880
3420
6105
库存
现货
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    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.

  • 体外研究

  • 体内研究

    溶解于DMSO中并稀释于生理盐水

  • 激酶实验

  • 细胞实验

  • 动物实验

    75 mg/kg/day 口服

  • 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] 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

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

    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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