Galunisertib (LY2157299)

Catalog No.S2230

Galunisertib (LY2157299) Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 272 In stock
USD 170 In stock
USD 270 In stock
USD 770 In stock
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Cited by 32 Publications

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Biological Activity

Description Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3.
Targets
TβRI [1]
(Cell-free assay)
56 nM
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. [2] 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. [3] In human glioblastoma (GBM) cells, LY2157299 treatment blocks signaling through the heteromeric TGFβ receptor complex to reduce levels of active, phosphorylated SMAD. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Panc-1 M{nqfWZ2dmO2aX;uJGF{e2G7 M4Dz[FExKM7:TR?= MmKwOFghcA>? M4X1TWROW09? M2PwV5N1cW23bHH0[ZMhfGinIHPlcIwhcW64YYPpc44hcW62bzD0bIUh[2:ubHHn[Y4h\2WuIHHu[EB1cGViTXH0dolo\WxvY3;heIVlKGOxbHzh[4VvKGenbB?= M{P1SlI1PzhyOEKx

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Periostin / Fibronectin / Snail / Twist / pSmad2 / pERK / pAkt / pFAK; 

PubMed: 29774119     


U-87 MG cells were serum-starved for 24 h, then incubated in serum-free medium containing (or lacking) 10 μM Galunisertib (LY2157299) and 10 ng/mL of TGF-β for 48 h. Cells were lysed and expression levels of EMT markers periostin, fibronectin, Snail and twist, or the phosphorylation status of Smad2, Erk, Akt and Fak proteins were monitored by immunoblotting.

TGF-βR1 / p-ERK; 

PubMed: 30881035     


Western blot was performed to analyze the expression level of TGF-βR1, p-smad2 and p-ERK1/2. VECTOR, cells transduced with VECTOR lentivirus; VECTOR+ LY2157299, cells transduced with VECTOR lentivirus and treated with LY2157299; USP4, cells transduced with USP4 lentivirus; USP4+ LY2157299, cells transduced with USP4 lentivirus and treated with LY2157299.

29774119 30881035
Growth inhibition assay
Cell viability; 

PubMed: 28873435     


Primary cell cultures were treated with LY2157299. MTS was performed at 72 hrs. TGF-ΒR1 inhibition by LY2157299 did not influence cell viability in any type of primary cell culture. 

28873435
Immunofluorescence
E-cadherin; 

PubMed: 29467918     


KPC-M09 cells were treated with control, TGFβ or TGFβ plus galunisertib (2 μM or 10 μM). Bright field images are shown in the top panel and were imaged at 20X. The bottom panel shows fluorescent IHC using anti-E-cadherin (red) as well as DAPI (blue) as a counter stain. Cells were imaged at 40X.

29467918
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. [2] Administration of LY2157299 ameliorates anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure. [3] Oral administration of LY2157299 at 75 mg/kg/day displays significant antitumor activity against both Calu6 and MX1 xenografts in mice. [5] 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. [6]

Protocol

Animal Research:[5]
- Collapse
  • Animal Models: Nude mice implanted subcutaneously with Calu6 or MX1 cells
  • Formulation: Dissolved in DMSO and diluted in saline
  • Dosages: 75 mg/kg/day
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL (200.31 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1%CMC-Na
For best results, use promptly after mixing.
30mg/mlmg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 369.42
Formula

C22H19N5O

CAS No. 700874-72-2
Storage powder
in solvent
Synonyms N/A

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID