Molecular Weight(MW): 369.42
Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3.
Cited by 31 Publications
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Choose Selective TGF-beta/Smad Inhibitors
|Description||Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3.|
LY2157299 potently inhibits the TGFβ receptor signaling. LY2157299 abolishes the TGFβ induced Smad2 phosphorylation in HUVEC cells. LY2157299 also shows dose dependent potentiation of VEGF or bFGF induced cell proliferation in HUVEC. LY2157299 also promotes VEGF induced HUVEC cell migration. LY2157299 potentiates angiogenesis in the in vitro VEGF-stimulated cord formation assay.  LY2157299 inhibits TGF-β-mediated SMAD2 activation and hematopoietic suppression in primary hematopoietic stem cells in a dose-dependent manner. LY2157199 treatment stimulates hematopoiesis from primary MDS bone marrow specimens.  In human glioblastoma (GBM) cells, LY2157299 treatment blocks signaling through the heteromeric TGFβ receptor complex to reduce levels of active, phosphorylated SMAD. 
|In vivo||Although anti-tumor activity has been observed in several pre-clinical models, LY2157299 fails to show significant in vivo angiogenic effects in the 4T1, Colo205, or A549 xenograft models.  Administration of LY2157299 ameliorates anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure.  Oral administration of LY2157299 at 75 mg/kg/day displays significant antitumor activity against both Calu6 and MX1 xenografts in mice.  In vivo, LY2157299 induces angiogenesis and enhances VEGF and basic-fibroblast-growth-factor-induced angiogenesis in a Matrigel-plug assay, whereas adding an alpha5-integrin-neutralizing antibody to the Matrigel selectively inhibits this enhanced response. |
-  Mundla SR, Patent, 2006, US7872020.
-  Yingling JM, et al. Proc Am Assoc Cancer Res. 2006, 47, abstract 250.
-  Zhou L, et al. Cancer Res, 2011, 71(3), 955-963.
|In vitro||DMSO||74 mg/mL (200.31 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04031872||Not yet recruiting||Drug: LY3200882||Colorectal Cancer Metastatic||The Netherlands Cancer Institute|Vall d''Hebron Institute of Oncology|Agendia|European Organisation for Research and Treatment of Cancer - EORTC|Azienda Ospedaliera Niguarda Cà Granda|Fundación para la Investigación del Hospital Clínico de Valencia|University of Campania Luigi Vanvitelli|University of Turin Italy|Eli Lilly and Company|Catalan Institute of Health|Universitaire Ziekenhuizen Leuven||February 2020||Phase 1|Phase 2|
|NCT03470350||Withdrawn||Drug: Galunisertib||Colorectal Cancer Metastatic||The Netherlands Cancer Institute|Vall d''Hebron Institute of Oncology|Agendia|European Organisation for Research and Treatment of Cancer - EORTC|Azienda Ospedaliera Niguarda Cà Granda|Fundación para la Investigación del Hospital Clínico de Valencia|University of Campania Luigi Vanvitelli|University of Turin Italy|Eli Lilly and Company|Catalan Institute of Health|Universitaire Ziekenhuizen Leuven||August 24 2018||Phase 1|Phase 2|
|NCT02734160||Completed||Drug: Galunisertib|Drug: Durvalumab||Metastatic Pancreatic Cancer||Eli Lilly and Company|AstraZeneca||June 15 2016||Phase 1|
|NCT02752919||Completed||Drug: Galunisertib||Healthy||Eli Lilly and Company||April 2016||Phase 1|
|NCT02452008||Recruiting||Drug: Enzalutamide|Drug: LY2157299||Prostate Cancer||Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Eli Lilly and Company||April 2016||Phase 2|
|NCT02538471||Terminated||Radiation: Radiation therapy|Drug: Study Drug||Metastatic Breast Cancer||Weill Medical College of Cornell University|University of California Los Angeles||August 10 2015||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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