2. TGF-beta/Smad
  3. TGF-β Receptor
  4. Galunisertib

Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.

For research use only. We do not sell to patients.

CAS No. : 700874-72-2

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Customer Review

Based on 68 publication(s) in Google Scholar

Other Forms of Galunisertib:

Galunisertib Related Antibodies

Top Publications Citing Use of Products

68 Publications Citing Use of MCE Galunisertib

Flow Cytometry
In Vivo Imaging
RT-PCR
IF
Cell Imaging/Staining

    Galunisertib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Oct 7;10(1):332.  [Abstract]

    LY2157299 (100 mg/kg; oral gavage). The frequencies of CD31+VE-Cadherin+ECs within CD45-Ter119- BM cells from mice subjected to the specified treatments were assessed through flow cytometry.

    Galunisertib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Oct 7;10(1):332.  [Abstract]

    LY2157299 (100 μM; 24 h). The mRNA level of PTN in BM ECs treated with TGF-β1 alone or in combination with LY2157299 (LY) was assessed via qPCR.

    Galunisertib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Oct 7;10(1):332.  [Abstract]

    LY2157299 (100 μM; 24 h). Representative images of double-positive BM ECs (yellow) co-stained with DiI-AcLDL (red) and FITC-UEA I (green) following the indicated treatments.

    Galunisertib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2023 Oct 3;42(1):258.  [Abstract]

    Galunisertib (75 mg/kg; oral gavage). Representative bioluminescent images and BLI analysis of mice with intrasplenic injection of MKN45 cells showed the inhibitory effect of the anti-LBP antibody and galunisertib on LM in vivo.

    Galunisertib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2023 Oct 3;42(1):258.  [Abstract]

    Galunisertib (75 mg/kg; oral gavage). IF was applied to confirm that galunisertib inhibit the actin remodeling of MKN45 cells.

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    ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.

    IC50 & Target

    IC50: 56 nM (TGF-βRI)[4]
    Cellular Effect
    Cell Line Type Value Description References
    4T1 CC50
    > 20 μM
    Compound: LY-2157299
    Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 38626523]
    4T1 IC50
    > 0.1 μM
    Compound: 5, LY-2157299
    Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay
    Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay
    		[PMID: 24786585]
    BEAS-2B CC50
    12.96 μM
    Compound: LY-2157299
    Cytotoxicity against human BEAS-2B cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Cytotoxicity against human BEAS-2B cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 38626523]
    HEK-293T CC50
    > 20 μM
    Compound: LY-2157299
    Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 38626523]
    HaCaT IC50
    > 0.1 μM
    Compound: 5, LY-2157299
    Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay
    Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay
    		[PMID: 24786585]
    HepG2 CC50
    5.46 μM
    Compound: LY-2157299
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 38626523]
    Kasumi 1 CC50
    3.12 μM
    Compound: LY-2157299
    Antiproliferative activity against human Kasumi 1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human Kasumi 1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 38626523]
    L02 CC50
    17.38 μM
    Compound: LY-2157299
    Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 38626523]
    MCF-10A CC50
    19.88 μM
    Compound: LY-2157299
    Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 38626523]
    MDA-MB-231 CC50
    > 20 μM
    Compound: LY-2157299
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 38626523]
    MV4-11 CC50
    > 20 μM
    Compound: LY-2157299
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 38626523]
    PANC-1 CC50
    > 20 μM
    Compound: LY-2157299
    Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 38626523]
    Panc02 CC50
    > 20 μM
    Compound: LY-2157299
    Antiproliferative activity against mouse Panc02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against mouse Panc02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 38626523]
    Sf9 IC50
    0.119 μM
    Compound: 3; LY-2157299
    Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay
    Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay
    		[PMID: 31299584]
    Sf9 IC50
    0.119 μM
    Compound: 4; LY-2157299
    Inhibition of recombinant GST-tagged human ALK5 expressed in baculovirus infected Sf9 insect cells
    Inhibition of recombinant GST-tagged human ALK5 expressed in baculovirus infected Sf9 insect cells
    		[PMID: 31810777]
    Sf9 IC50
    0.129 μM
    Compound: 3; LY-2157299
    Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method
    Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method
    		[PMID: 31303386]
    Sf9 IC50
    69.4 nM
    Compound: 4; LY-2157299
    Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay
    Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay
    		[PMID: 26483198]
    U-251 CC50
    16.96 μM
    Compound: LY-2157299
    Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 38626523]
    In Vitro

    Galunisertib (LY2157299) (0.1, 1, 10, and 100 μM) displays a slight dose-dependent potentiation of Bay 43-9006 in SK-Sora, HepG2, and Hep3B cell lines but not in JHH6, SK-HEP1, and HuH7 cell lines[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Galunisertib Related Antibodies
    In Vivo

    Human xenografts Calu6 (non-small cell lung cancer) and MX1 (breast cancer) are implanted subcutaneously in nude mice. After oral administration of 75 mg/kg, Galunisertib (LY2157299) induces a 70% decrease in pSmad for both types of cell lines. The time at which pSmad recovered 80% of baseline is approximately 6 h after administration[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    369.42

    Formula

    C22H19N5O
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    CC1=CC=CC(C2=NN3C(CCC3)=C2C4=CC=NC5=C4C=C(C=C5)C(N)=O)=N1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (270.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

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    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 5.75 mg/mL (15.56 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (5.63 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.95%

    SDS (396 KB)

    COA (252 KB) LCMS (121 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Cell survival is determined using the MTT assay. The conversion of yellow water-soluble tetrazolium MTT into purple insoluble formazan is catalyzed by mitochondrial dehydrogenases and used to estimate the number of viable cells. In brief, cells are seeded in 96-well tissue culture plates at a density of 2×103 cells/well. After drug exposure, cells are incubated with 0.4 mg/mL MTT for 4 hours at 37°C. After incubation, the supernatant is discarded, insoluble formazan precipitates are dissolved in 0.1 mL of DMSO, and the absorbance is measured at 560 nm by use of a microplate reader. Wells with untreated cells or with drug-containing medium without cells are used as positive and negative controls respectively. For proliferation assay, MTT assay is done daily to determine the number of viable cells in untreated control andGalunisertib (LY2157299) (0.1, 1, 10, and 10 μM)-treated group[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Mice[3]
    Charles River nude mice (weight 25 mg) are used. Galunisertib (LY2157299) is given orally as a single dose or in a multiple dosing design. The value of the dose levels given in a single dose manner is 10 (n=3), 30 (n=8), 50 (n=26), 75 (n=69), 100 (n=3), 150 (n=21) and 300 (n=3) mg/kg. Animals are sacrificed at the following times: 0.5, 1, 1.5, 2, 4, 8 and 16 h after administration, then the tumor is removed and blood is recovered. In the multiple dosing study, Galunisertib (LY2157299) is administered twice a day (bid) at the dose of 75 mg/kg every 12 h for 20 consecutive days to 31 mice. Animals are sacrificed at 2 h after the last administration at days 10, 15, 20 and 25, and the tumor is removed for pSmad determination and the blood is recovered for determination of drug levels in plasma.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7069 mL 13.5347 mL 27.0695 mL 67.6736 mL
    5 mM 0.5414 mL 2.7069 mL 5.4139 mL 13.5347 mL
    10 mM 0.2707 mL 1.3535 mL 2.7069 mL 6.7674 mL
    15 mM 0.1805 mL 0.9023 mL 1.8046 mL 4.5116 mL
    20 mM 0.1353 mL 0.6767 mL 1.3535 mL 3.3837 mL
    25 mM 0.1083 mL 0.5414 mL 1.0828 mL 2.7069 mL
    30 mM 0.0902 mL 0.4512 mL 0.9023 mL 2.2558 mL
    40 mM 0.0677 mL 0.3384 mL 0.6767 mL 1.6918 mL
    50 mM 0.0541 mL 0.2707 mL 0.5414 mL 1.3535 mL
    60 mM 0.0451 mL 0.2256 mL 0.4512 mL 1.1279 mL
    80 mM 0.0338 mL 0.1692 mL 0.3384 mL 0.8459 mL
    100 mM 0.0271 mL 0.1353 mL 0.2707 mL 0.6767 mL
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    Galunisertib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Galunisertib700874-72-2LY2157299LY 2157299LY-2157299TGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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