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Products are for research use only. Not for human use. We do not sell to patients.
(Galunisertib; LY-2157299; LY 2157299)
LY2157299 Chemical Structure
|Product name: LY2157299|
|Cat. No.: HY-13226|
LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM.
IC50 value: 56 nM 
Target: TGFβ receptor I
in vitro: 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 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 .
|M.Wt||369.42||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≥ 47 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||2.7069 mL||13.5347 mL||27.0695 mL|
|5 mM||0.5414 mL||2.7069 mL||5.4139 mL|
|10 mM||0.2707 mL||1.3535 mL||2.7069 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|LY2157299||Eli Lilly & Co||31-OCT-13||30-NOV-13||Phase 1||25-NOV-13|
|Eli Lilly & Co||Advanced solid tumor||30-NOV-12||30-APR-14||Phase 1||20-NOV-13|
|Eli Lilly & Co||31-JAN-13||28-FEB-13||Phase 1||18-FEB-13|
|Eli Lilly & Co||Glioma||30-APR-11||31-JAN-15||Phase 2||11-NOV-13|
|Eli Lilly & Co||Hepatocellular carcinoma||31-MAR-11||31-MAY-15||Phase 2||15-NOV-13|
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