Galunisertib monohydrate
Based on 72 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 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]
- 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.
- 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
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 (72)
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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 -
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 -
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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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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