Galunisertib (LY2157299)

Catalog No.S2230

For research use only.

Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3.

Galunisertib (LY2157299) Chemical Structure

CAS No. 700874-72-2

Selleck's Galunisertib (LY2157299) has been cited by 150 publications

Purity & Quality Control

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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 MUPGeY5kfGmxbjDBd5NigQ>? M{XUZlExKM7:TR?= NGjnR|M1QCCq NYDWUpBZTE2VTx?= M1;4bpN1cW23bHH0[ZMhfGinIHPlcIwhcW64YYPpc44hcW62bzD0bIUh[2:ubHHn[Y4h\2WuIHHu[EB1cGViTXH0dolo\WxvY3;heIVlKGOxbHzh[4VvKGenbB?= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd6MEiyNUc,OjR5OEC4NlE9N2F-
Sf9 MVjGeY5kfGmxbjDhd5NigQ>? MmHYTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCJU2St[pV{\WRiQVzLOUBmgHC{ZYPz[YQhcW5iU3[5JIlve2WldDDj[YxteyC3c3nu[{Bk[XOnaX6gZZMhe3Wkc4TyZZRmKGK7IIDyc5BzcWW2YYL5JJJi\GmxaYPveI9xcWNicILveIVqdiCtaX7hd4Uh[XO|YYmsJGlEPTBiPTCwMlA3QTRizszNMi=> NX\Lb4w5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0PFMyQThpPkK2OFg{OTl6PD;hQi=>
Sf9 NH3oVnpHfW6ldHnvckBie3OjeR?= NFLucYJKdmirYnn0bY9vKG:oIHj1cYFvKEGOS{Wg[ZhxemW|c3XkJIlvKFOoOTDpcpNm[3RiY3XscJMhfXOrbnegZ4F{\WmwIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDb[4FudWFvM{PQYWFVWCxiSVO1NEA:KDBwMEWxJO69VS5? NX3leYF{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixN|U3QDVpPkK4NVM2Pjh3PD;hQi=>
Sf9 NHPY[3NHfW6ldHnvckBie3OjeR?= MWWxJIhz MnL6TY5pcWKrdHnvckBw\iCqdX3hckBJcXNvdHHn[4VlKFSJRnLleIFTOSCWMkC0SEBufXSjboSg[ZhxemW|c3XkJIlvKFOoOTDpcpNm[3RiY3XscJMh[W[2ZYKgNUBpeiCkeTDIWHJHKGG|c3H5MEBKSzVyIE2gNE4xODRzIN88UU4> NGn0Npk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSyNlM{Oid-Mkm0NlI{OzJ:L3G+
B16 NVnkfI5uSW62aYT1cY9zKGG|c3H5 MUO3OUBu\y:tZx?= M4f2dmFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFKxOkBk\WyuczDpckBud3W|ZTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIIT1cY9zKGe{b4f0bEBifCB5NTDt[{9s\yxicH:gZollKHKnbHH0bZZmKHSxII\lbIlkdGVvdILlZZRm\CClb370do9t NFrrTGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe4OlU5PSd-MkS3PFY2QDV:L3G+
B16 MkD2RY51cXS3bX;yJIF{e2G7 M3vSelc2KG2pL3vn Ml7oRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViQkG2JINmdGy|IHnuJI1wfXOnIHHzd4V{e2WmIHHzJJN2eHC{ZYPzbY9vKG:oIIT1cY9zKH[xbIXt[UBifCB5NTDt[{9s\yxicH:gZollKHKnbHH0bZZmKHSxII\lbIlkdGVvdILlZZRm\CClb370do9t Moi4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5OE[1PFUoRjJ2N{i2OVg2RC:jPh?=
B16 NWThbYo4SW62aYT1cY9zKGG|c3H5 M2L1Zlc2KG2pL3vn NWHWZnRPSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhdW:3c3WgRlE3KGOnbHzzJIlvKG2xdYPlJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gcJlueGhibn;k[UBu\XSjc4Thd4l{KGG2IEe1JI1oN2upLDDwc{BjcWRicnXsZZRqfmVidH:geoVpcWOuZT30doVifGWmIHPvcpRzd2x? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd6NkW4OUc,OjR5OE[1PFU9N2F-
Assay
Methods Test Index PMID
Western blot TGF-βR1 / p-ERK ; Periostin / Fibronectin / Snail / Twist / pSmad2 / pERK / pAkt / pFAK 30881035 29774119
Growth inhibition assay Cell viability 28873435
Immunofluorescence E-cadherin 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 (from reference)

Animal Research:[5]
  • Animal Models: Nude mice implanted subcutaneously with Calu6 or MX1 cells
  • Dosages: 75 mg/kg/day
  • Administration: Orally

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 369.42
Formula

C22H19N5O

CAS No. 700874-72-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NC(=CC=C1)C2=NN3CCCC3=C2C4=C5C=C(C=CC5=NC=C4)C(=O)N

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04031872 Unknown status 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
NCT02452008 Recruiting Drug: Enzalutamide|Drug: LY2157299 Prostate Cancer Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Eli Lilly and Company May 3 2016 Phase 2
NCT02752919 Completed Drug: Galunisertib Healthy Eli Lilly and Company April 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

Handling Instructions

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