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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3 Customer Reviews

  • Treatment of HLE and HLF cells with TGFβRI inhibitor LY2157299 led to dose-dependent loss of GLI2 levels.

    Cancer Research, 2014, 74(21): 5963-77 . Galunisertib (LY2157299) purchased from Selleck.

    Cells were treated in both formats with 10 uM of SB525334 (TGFβR1), SJN 2511 (TGFβR1), LY2157299 (TGFβR2, TGFβR1), Dorsomorphin (AMPK, ALK2, ALK3, ALK6), DMH-1 (ALK2), or GW5074 (c-raf), or 50 ng/ml of TGF-β. Microtissue or tissue-culture well fluorescence for each condition are shown after 3 days of culture for 393T5 cells, which proliferate slower in control conditions, so that the two cell lines undergo the same number of population doublings during each assay.

    Lab Chip 2013 13(10), 1969-78. Galunisertib (LY2157299) purchased from Selleck.

  • Immunofluorescence of SMα (Red) and VE-cadherin (Red) combined with DAPI (blue) revealed that VM markers were elevated in DMSO-treated NHA/A172 cells but not in galunisertib-treated NHA/A172 cells.

    Sci Rep, 2016, 6:23056.. Galunisertib (LY2157299) purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 M4fV[WZ2dmO2aX;uJGF{e2G7 M2mzNlExKM7:TR?= M3fIdFQ5KGh? MonDSG1UVw>? MUnzeIlufWyjdHXzJJRp\SClZXzsJIlvfmG|aX;uJIlvfG9idHjlJINwdGyjZ3XuJIdmdCCjbnSgeIhmKE2jdILp[4VtNWOxYYTl[EBkd2yuYXflckBo\Wx? NXT2dVBXOjR5OEC4NlE>

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02981342 Recruiting Pancreatic Ductal Adenocarcinoma Eli Lilly and Company January 2017 Phase 2
NCT02906397 Not yet recruiting ADVANCED HEPATOCELLULAR CARCINOMA (HCC) Abramson Cancer Center of the University of Pennsylvania November 2016 Phase 1
NCT02734160 Recruiting Metastatic Pancreatic Cancer Eli Lilly and Company|AstraZeneca June 2016 Phase 1
NCT02688712 Not yet recruiting Rectal Adenocarcinoma Providence Health & Services|Eli Lilly and Company June 2016 Phase 2
NCT02752919 Completed Healthy Eli Lilly and Company April 2016 Phase 1
NCT02452008 Recruiting Prostate Cancer Sidney Kimmel Comprehensive Cancer Center April 2016 Phase 2

Tech Support

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID