Galunisertib monohydrate
Based on 75 publication(s) in Google Scholar
Galunisertib monohydrate 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.: 924898-09-9
- Formula: C22H21N5O2
- Molecular Weight:387.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) Galunisertib monohydrate
More- Signal Transduct Target Ther. 2025 Oct 7;10(1):332. [Abstract]
- Cancer Cell. 2026 May 21:S1535-6108(26)00220-5.
- Immunity. 2026 Apr 27:S1074-7613(26)00141-X. [Abstract]
- Cancer Discov. 2024 Oct 4;14(10):1964-1989. [Abstract]
- Nat Commun. 2024 Feb 14;15(1):1348. [Abstract]
- Cell Discov. 2025 Mar 11;11(1):22. [Abstract]
- Redox Biol. 2026 Mar:90:104047. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Clin Invest. 2026 Jul 21.
- J Exp Clin Cancer Res. 2023 Oct 3;42(1):258. [Abstract]
- J Exp Clin Cancer Res. 2023 Aug 9;42(1):200. [Abstract]
- J Control Release. 2024 Mar:367:768-778. [Abstract]
- Cancer Lett. 2023 Aug 28:570:216330. [Abstract]
- Cancer Lett. 2022 Sep 1:543:215795. [Abstract]
- J Immunother Cancer. 2025 Dec 5;13(12):e012988. [Abstract]
- Int J Biol Sci. 2023 Jan 1;19(1):204-224. [Abstract]
- Int J Biol Macromol. 2023 Oct 1:250:126147. [Abstract]
- Mol Ther Oncol. 2024 Aug 8;32(3):200858. [Abstract]
- Antioxidants (Basel). 2024 Jul 29;13(8):914. [Abstract]
- Br J Cancer. 2025 Dec 13. [Abstract]
- Stem Cell Res Ther. 2025 Aug 20;16(1):443. [Abstract]
- World J Gastroenterol. 2026 Feb 7;32(5):115301. [Abstract]
- Cell Rep. 2022 Aug 30;40(9):111253. [Abstract]
- JCI Insight. 2026 Feb 23;11(4):e198810. [Abstract]
- Biochem Pharmacol. 2026 Mar 10:249:117889. [Abstract]
- Cell Mol Life Sci. 2024 Apr 21;81(1):189. [Abstract]
- Liver Int. 2021 Aug;41(8):1956-1968. [Abstract]
- OncoImmunology. 2020 Sep 22;9(1):1824631. [Abstract]
- Breast Cancer Res. 2019 Nov 21;21(1):123. [Abstract]
- Cells. 2022 Jan 11;11(2):237. [Abstract]
- Int Immunopharmacol. 2025 Dec 10:167:115663. [Abstract]
- Int Immunopharmacol. 2023 Jun:119:110180. [Abstract]
- Int J Mol Sci. 2022 Jun 15;23(12):6689. [Abstract]
- Cell Oncol (Dordr). 2021 Feb;44(1):193-204. [Abstract]
- Am J Physiol Cell Physiol. 2026 Feb 1;330(2):C467-C481. [Abstract]
- Am J Physiol Cell Physiol. 2023 Jul 1;325(1):C344-C361. [Abstract]
- Front Pharmacol. 2021 Apr 30:12:644886. [Abstract]
- J Nutr Biochem. 2021 Jan:87:108518. [Abstract]
- Tissue Eng Regen Med. 2021 Dec;18(6):963-973. [Abstract]
- Bioorg Chem. 2021 Sep:114:105222. [Abstract]
- Sci Rep. 2025 Apr 24;15(1):14277. [Abstract]
- Int J Cancer. 2024 May 15;154(10):1814-1827. [Abstract]
- J Cell Mol Med. 2020 Mar;24(6):3656-3668. [Abstract]
- FASEB J. 2025 Nov 30;39(22):e71239. [Abstract]
- J Endocrinol Invest. 2026 Jul 6.
- Cancer Res Commun. 2024 Feb 15;4(2):418-430. [Abstract]
- J Cell Physiol. 2019 Jul;234(7):10554-10565. [Abstract]
- Cytokine. 2026 Aug:204:157169. [Abstract]
- Exp Cell Res. 2022 Dec 1;421(1):113376. [Abstract]
- Brain Sci. 2019 Dec 30;10(1):20. [Abstract]
- Int J Parasitol. 2018 Nov;48(13):1023-1033. [Abstract]
- Biol Reprod. 2025 Jul 25:ioaf168. [Abstract]
- J Immunol Res. 2018 Sep 3:2018:6248590. [Abstract]
- Pathol Oncol Res. 2021 Nov 19;27:1609997. [Abstract]
- Int J Clin Exp Med. 2020;13(2):396-406.
- Biomed Pharmacother. 2026 Sep:202:119803.
- SSRN. 2026 May 12.
- Res Sq. 2026 Mar 11.
- Heidelberg University. 2025.
- bioRxiv. 2025 Sep 21.
- Biomed Pharmacother. 2025 Sep 18:192:118565. [Abstract]
- patent. US20250215017A1.
- bioRxiv. 2025 Jun 24.
- bioRxiv. 2025 May 4:2025.04.29.651320. [Abstract]
- bioRxiv. 2024 November 11.
- bioRxiv. 2024 Nov 25:2024.11.22.624939. [Abstract]
- Patent. US20240197712A1.
- Patent. US20240139331A1.
- bioRxiv. 2024 May 15.
- bioRxiv. 2023 Aug 15.
- Patent. US20220378739A1.
- Evid Based Complement Alternat Med. 2022 Apr 11;2022:9823258. [Abstract]
- Evid Based Complement Alternat Med. 2021 Feb 12:2021:6671282. [Abstract]
- Universidad de Granada. 2020 Sep.
- bioRxiv. 2020 Apr.
Customer Validation & Images
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Flow Cytometry
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RT-PCR
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Cell Imaging/Staining
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In Vivo Imaging
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IF
Biological Activity
Description
IC50 & Target
IC50: 56 nM (TGF-βRI)[4]
Chemical Information
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CAS No. 924898-09-9
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Molecular Weight 387.43
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Formula C22H21N5O2
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SMILES
O=C(C1=CC=C2N=CC=C(C3=C(CCC4)N4N=C3C5=NC(C)=CC=C5)C2=C1)N.O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (75)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
2025 Oct 7;10(1):332. PMID: 41053000
Galunisertib monohydrate 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 monohydrate 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 monohydrate 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.
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Immunity
An SPP1-SOCS1 pathway constrains interferon responses in tumor-associated macrophages and shapes an immunosuppressive tumor microenvironment. [Abstract]2026 Apr 27:S1074-7613(26)00141-X. PMID: 42049035 -
Cancer Discov
Oncogenic KRAS-dependent stromal interleukin-33 directs the pancreatic microenvironment to promote tumor growth. [Abstract]2024 Oct 4;14(10):1964-1989. PMID: 38958646 -
Nat Commun
TGF-β blockade drives a transitional effector phenotype in T cells reversing SIV latency and decreasing SIV reservoirs in vivo. [Abstract]2024 Feb 14;15(1):1348. PMID: 38355731 -
Cell Discov
2025 Mar 11;11(1):22. PMID: 40064862 -
Redox Biol
CRISPR-based chemogenomic profiling reveals redox vulnerabilities to epigallocatechin-3-gallate and green tea polyphenol extract. [Abstract]2026 Mar:90:104047. PMID: 41581373 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
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J Exp Clin Cancer Res
Gastric cancer-derived LBP promotes liver metastasis by driving intrahepatic fibrotic pre-metastatic niche formation. [Abstract]2023 Oct 3;42(1):258. PMID: 37789385
Galunisertib monohydrate 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 monohydrate 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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J Exp Clin Cancer Res
An amino acid transporter subunit as an antibody-drug conjugate target in colorectal cancer. [Abstract]2023 Aug 9;42(1):200. PMID: 37559159 -
J Control Release
Nano-chemical priming strategy to enhance TGF-β resistance and anti-tumor activity of natural killer cells. [Abstract]2024 Mar:367:768-778. PMID: 38341178 -
Cancer Lett
Inducible nitric oxide synthase (iNOS)-activated Cxcr2 signaling in myeloid cells promotes TGFβ-dependent squamous cell carcinoma lung metastasis. [Abstract]2023 Aug 28:570:216330. PMID: 37524225 -
Cancer Lett
Dual inhibition of TGFβ signaling and CSF1/CSF1R reprograms tumor-infiltrating macrophages and improves response to chemotherapy via suppressing PD-L1. [Abstract]2022 Sep 1:543:215795. PMID: 35718267 -
J Immunother Cancer
Colorectal cancer organoids drive hypoxia, TGF-β, and patient-specific diversification of NK cell activation programs. [Abstract]2025 Dec 5;13(12):e012988. PMID: 41360426 -
Int J Biol Sci
TGFβ Governs the Pleiotropic Activity of NDRG1 in Triple-Negative Breast Cancer Progression. [Abstract]2023 Jan 1;19(1):204-224. PMID: 36594086 -
Int J Biol Macromol
CL4-modified exosomes deliver lncRNA DARS-AS1 siRNA to suppress triple-negative breast cancer progression and attenuate doxorubicin resistance by inhibiting autophagy. [Abstract]2023 Oct 1:250:126147. PMID: 37544559 -
Mol Ther Oncol
Galunisertib promotes bevacizumab-induced vascular normalization in nasopharyngeal carcinoma: Multi-parameter MRI evaluation. [Abstract]2024 Aug 8;32(3):200858. PMID: 39280586 -
Antioxidants (Basel)
2024 Jul 29;13(8):914. PMID: 39199160 -
Br J Cancer
Fibroblast growth factor signals drive the metastatic behavior in small cell lung cancer. [Abstract]2025 Dec 13. PMID: 41390896 -
Stem Cell Res Ther
Harnessing TGF-β signaling to improve testicular organoid development from dissociated testicular cells. [Abstract]2025 Aug 20;16(1):443. PMID: 40830519 -
World J Gastroenterol
ICAM2 loss drives 5-fluorouracil resistance via TGF-β/Smad/SP1/PTN-dependent apoptosis evasion and macrophage remodeling in gastric cancer. [Abstract]2026 Feb 7;32(5):115301. PMID: 41693979 -
Cell Rep
2022 Aug 30;40(9):111253. PMID: 36044839 -
JCI Insight
Single-cell capture of on-ART SIV transcription reveals TGF-β-mediated metabolic control of viral latency. [Abstract]2026 Feb 23;11(4):e198810. PMID: 41729081 -
Biochem Pharmacol
PMEPA1 promotes mTOR inhibitor resistance in triple-negative breast cancer: Targeting the TGF-β/PMEPA1 axis as a therapeutic strategy to overcome resistance. [Abstract]2026 Mar 10:249:117889. PMID: 41819443 -
Cell Mol Life Sci
Adipose-derived stem cells promote glycolysis and peritoneal metastasis via TGF-β1/SMAD3/ANGPTL4 axis in colorectal cancer. [Abstract]2024 Apr 21;81(1):189. PMID: 38643448 -
Liver Int
The MSP-RON pathway regulates liver fibrosis through transforming growth factor beta-dependent epithelial-mesenchymal transition. [Abstract]2021 Aug;41(8):1956-1968. PMID: 33786995 -
OncoImmunology
Pirfenidone facilitates immune infiltration and enhances the antitumor efficacy of PD-L1 blockade in mice. [Abstract]2020 Sep 22;9(1):1824631. PMID: 33457101 -
Breast Cancer Res
WDR5 inhibition halts metastasis dissemination by repressing the mesenchymal phenotype of breast cancer cells. [Abstract]2019 Nov 21;21(1):123. PMID: 31752957 -
Cells
Wnt5A and TGFβ1 Converges through YAP1 Activity and Integrin Alpha v Up-Regulation Promoting Epithelial to Mesenchymal Transition in Ovarian Cancer Cells and Mesothelial Cell Activation. [Abstract]2022 Jan 11;11(2):237. PMID: 35053353 -
Int Immunopharmacol
GPRC5A+ myCAFs promote ESCC progression via TGF-β-induced fibroblast activation and ANXA1-mediated M2 macrophage polarization. [Abstract]2025 Dec 10:167:115663. PMID: 41082840 -
Int Immunopharmacol
A polysaccharide from Codonopsis pilosula roots attenuates carbon tetrachloride-induced liver fibrosis via modulation of TLR4/NF-κB and TGF-β1/Smad3 signaling pathway. [Abstract]2023 Jun:119:110180. PMID: 37068337 -
Int J Mol Sci
Galunisertib Exerts Antifibrotic Effects on TGF-β-Induced Fibroproliferative Dermal Fibroblasts. [Abstract]2022 Jun 15;23(12):6689. PMID: 35743131 -
Cell Oncol (Dordr)
1p/19q co-deletion status is associated with distinct tumor-associated macrophage infiltration in IDH mutated lower-grade gliomas. [Abstract]2021 Feb;44(1):193-204. PMID: 32915415 -
Am J Physiol Cell Physiol
Ablation of tumor-derived IGFBP-3 attenuates cancer-associated skeletal muscle wasting in murine pancreatic cancer. [Abstract]2026 Feb 1;330(2):C467-C481. PMID: 41525104 -
Am J Physiol Cell Physiol
Sel1-like Proteins and Peptides are the Major Oxalobacter formigenes-derived Factors Stimulating Oxalate Transport by Human Intestinal Epithelial Cells. [Abstract]2023 Jul 1;325(1):C344-C361. PMID: 37125773 -
Front Pharmacol
Bellidifolin Ameliorates Isoprenaline-Induced Myocardial Fibrosis by Regulating TGF-β1/Smads and p38 Signaling and Preventing NR4A1 Cytoplasmic Localization. [Abstract]2021 Apr 30:12:644886. PMID: 33995055 -
J Nutr Biochem
Functional targeting of the TGF-βR1 kinase domain and downstream signaling: A role for the galloyl moiety of green tea-derived catechins in ES-2 ovarian clear cell carcinoma. [Abstract]2021 Jan:87:108518. PMID: 33017609 -
Tissue Eng Regen Med
Three-Dimensional Modeling of the Structural Microenvironment in Post-Traumatic War Wounds. [Abstract]2021 Dec;18(6):963-973. PMID: 34363599 -
Bioorg Chem
Presegetane diterpenoids from Euphorbia sieboldiana as a new type of anti-liver fibrosis agents that inhibit TGF-β/Smad signaling pathway. [Abstract]2021 Sep:114:105222. PMID: 34375196 -
Sci Rep
Preclinical validation of TGFβ inhibitors as a novel therapeutic strategy for post-traumatic heterotopic ossification. [Abstract]2025 Apr 24;15(1):14277. PMID: 40274953 -
Int J Cancer
TGFβ-induced EN1 promotes tumor budding of adenoid cystic carcinoma in patient-derived organoid model. [Abstract]2024 May 15;154(10):1814-1827. PMID: 38282121 -
J Cell Mol Med
2020 Mar;24(6):3656-3668. PMID: 32064783 -
FASEB J
SAA1 Induces TGF-β1 Secretion by Ovarian Cancer Cells, Leading to M2 Macrophage Polarization and Inhibition of NK Cell Activity. [Abstract]2025 Nov 30;39(22):e71239. PMID: 41269670 -
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Cancer Res Commun
Lingual Denervation Improves the Efficacy of Anti-PD-1 Immunotherapy in Oral Squamous Cell Carcinomas by Downregulating TGFβ Signaling. [Abstract]2024 Feb 15;4(2):418-430. PMID: 38324026 -
J Cell Physiol
TCEA3 promotes differentiation of C2C12 cells via an Annexin A1-mediated transforming growth factor-β signaling pathway. [Abstract]2019 Jul;234(7):10554-10565. PMID: 30623413 -
Cytokine
2026 Aug:204:157169. PMID: 42143915 -
Exp Cell Res
IRE1α-XBP1 regulates PDK1-dependent induction of epithelial-mesenchymal transition in non-small cell lung cancer cells. [Abstract]2022 Dec 1;421(1):113376. PMID: 36209899 -
Brain Sci
2019 Dec 30;10(1):20. PMID: 31905898 -
Int J Parasitol
A TGF-β type I receptor-like molecule with a key functional role in Haemonchus contortus development. [Abstract]2018 Nov;48(13):1023-1033. PMID: 30266591 -
Biol Reprod
PTEN status on gonadotropin-releasing hormone (GnRH) metabolite, GnRH-(1-5), effects in endometrial cancer cell lines migration, & transcriptomic analysis of basal cell line and tumor gene expressions†. [Abstract]2025 Jul 25:ioaf168. PMID: 40709821 -
J Immunol Res
Altered NKp30, NKp46, NKG2D, and DNAM-1 Expression on Circulating NK Cells Is Associated with Tumor Progression in Human Gastric Cancer. [Abstract]2018 Sep 3:2018:6248590. PMID: 30255106 -
Pathol Oncol Res
2021 Nov 19;27:1609997. PMID: 34867089 -
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Biomed Pharmacother
TME-responsive nanoparticles co-targeting VCP, NETs, and dual immune checkpoints for immune revitalization in EGFR/PD-L1/CTLA-4-driven colorectal cancer. [Abstract]2025 Sep 18:192:118565. PMID: 40972397 -
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bioRxiv
2025 May 4:2025.04.29.651320. PMID: 40654780 -
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bioRxiv
Key Regulatory Elements of the TGFβ-LRRC15 Axis Predict Disease Progression and Immunotherapy Resistance Across Cancer Types. [Abstract]2024 Nov 25:2024.11.22.624939. PMID: 39651139 -
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Evid Based Complement Alternat Med
2022 Apr 11;2022:9823258. PMID: 35449819 -
Evid Based Complement Alternat Med
Punicalin Alleviates OGD/R-Triggered Cell Injury via TGF- β-Mediated Oxidative Stress and Cell Cycle in Neuroblastoma Cells SH-SY5Y. [Abstract]2021 Feb 12:2021:6671282. PMID: 33628309 -
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Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[1]. Bueno L, et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice. Eur J Cancer. 2008 Jan;44(1):142-50. [Content Brief]
[2]. Cong L, et al. Targeting the TGF-β receptor with kinase inhibitors for scleroderma therapy. Arch Pharm (Weinheim). 2014 Sep;347(9):609-15. [Content Brief]
[3]. Serova M, et al. Effects of TGF-beta signalling inhibition with galunisertib (LY2157299) in hepatocellular carcinoma models and in ex vivo whole tumor tissue samples from patients. Oncotarget. 2015 Aug 28;6(25):21614-27 [Content Brief]
[4]. Herbertz S, et al. Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway. Drug Des Devel Ther. 2015 Aug 10;9:4479-99. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Galunisertib monohydrate Related Classifications
HY-13226A Related Classifications
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