Galunisertib
Based on 71 publication(s) in Google Scholar
Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.90%
- CAS No.: 700874-72-2
- Formule: C22H19N5O
- Masse moléculaire:369.42
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) Galunisertib
More- Signal Transduct Target Ther. 2025 Oct 7;10(1):332. [Abstract]
- Cancer Cell. 2026 May 21:S1535-6108(26)00220-5.
- Cancer Discov. 2024 Oct 4;14(10):1964-1989. [Abstract]
- Nat Commun. 2024 Feb 14;15(1):1348. [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]
- Cell Discov. 2025 Mar 11;11(1):22. [Abstract]
- Redox Biol. 2026 Mar:90:104047. [Abstract]
- J Control Release. 2024 Mar:367:768-778. [Abstract]
- J Immunother Cancer. 2025 Dec 5;13(12):e012988. [Abstract]
- Cancer Lett. 2023 Aug 28:570:216330. [Abstract]
- Cancer Lett. 2022 Sep 1:543:215795. [Abstract]
- Int J Biol Sci. 2023 Jan 1;19(1):204-224. [Abstract]
- Int J Biol Macromol. 2023 Oct 1:250:126147. [Abstract]
- Biomed Pharmacother. 2025 Sep 18:192:118565. [Abstract]
- Stem Cell Res Ther. 2025 Aug 20;16(1):443. [Abstract]
- Cell Rep. 2022 Aug 30;40(9):111253. [Abstract]
- Br J Cancer. 2025 Dec 13. [Abstract]
- Antioxidants (Basel). 2024 Jul 29;13(8):914. [Abstract]
- OncoImmunology. 2020 Sep 22;9(1):1824631. [Abstract]
- Cell Mol Life Sci. 2024 Apr 21;81(1):189. [Abstract]
- JCI Insight. 2026 Feb 23;11(4):e198810. [Abstract]
- Biochem Pharmacol. 2026 Mar 10:249:117889. [Abstract]
- Breast Cancer Res. 2019 Nov 21;21(1):123. [Abstract]
- World J Gastroenterol. 2026 Feb 7;32(5):115301. [Abstract]
- Mol Ther Oncol. 2024 Aug 8;32(3):200858. [Abstract]
- Cells. 2022 Jan 11;11(2):237. [Abstract]
- Liver Int. 2021 Aug;41(8):1956-1968. [Abstract]
- Int J Mol Sci. 2022 Jun 15;23(12):6689. [Abstract]
- J Nutr Biochem. 2021 Jan;87:108518. [Abstract]
- Front Pharmacol. 2021 Apr 30:12:644886. [Abstract]
- Cell Oncol (Dordr). 2021 Feb;44(1):193-204. [Abstract]
- Am J Physiol Cell Physiol. 2026 Feb 1;330(2):C467-C481. [Abstract]
- Int Immunopharmacol. 2025 Oct 11:167:115663. [Abstract]
- Int J Cancer. 2024 May 15;154(10):1814-1827. [Abstract]
- Am J Physiol Cell Physiol. 2023 Jul 1;325(1):C344-C361. [Abstract]
- Int Immunopharmacol. 2023 Jun:119:110180. [Abstract]
- Bioorg Chem. 2021 Sep:114:105222. [Abstract]
- FASEB J. 2025 Nov 30;39(22):e71239. [Abstract]
- J Cell Mol Med. 2020 Mar;24(6):3656-3668. [Abstract]
- Tissue Eng Regen Med. 2021 Dec;18(6):963-973. [Abstract]
- J Cell Physiol. 2019 Jul;234(7):10554-10565. [Abstract]
- Sci Rep. 2025 Apr 24;15(1):14277. [Abstract]
- Cytokine. 2026 Aug:204:157169. [Abstract]
- J Immunol Res. 2018 Sep 3:2018:6248590. [Abstract]
- Exp Cell Res. 2022 Dec 1;421(1):113376. [Abstract]
- Cancer Res Commun. 2024 Feb 15;4(2):418-430. [Abstract]
- Int J Parasitol. 2018 Nov;48(13):1023-1033. [Abstract]
- Biol Reprod. 2025 Jul 25:ioaf168. [Abstract]
- Brain Sci. 2019 Dec 30;10(1):20. [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.
- patent. US20250215017A1.
- bioRxiv. 2025 Jun 24.
- bioRxiv. 2025 May 4:2025.04.29.651320. [Abstract]
- bioRxiv. 2024 Nov 25:2024.11.22.624939. [Abstract]
- bioRxiv. 2024 November 11.
- 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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RT-PCR
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In Vivo Imaging
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IF
Activité biologique
IC50: 56 nM (TGF-βRI)[4]
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Cell Line
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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
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[PMID: 38626523] |
| 4T1 | IC50 |
>0.1 μM
Compound: 5, LY-2157299
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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
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[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
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[PMID: 38626523] |
| HaCaT | IC50 |
>0.1 μM
Compound: 5, LY-2157299
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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
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[PMID: 24786585] |
| 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
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[PMID: 38626523] |
| 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
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[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
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[PMID: 38626523] |
| L02 | CC50 |
17.38 μM
Compound: LY-2157299
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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
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[PMID: 38626523] |
| MCF-10A | CC50 |
19.88 μM
Compound: LY-2157299
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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
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[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
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[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
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[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
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[PMID: 38626523] |
| PANC-1 | CC50 |
>20 μM
Compound: LY-2157299
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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
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[PMID: 38626523] |
| Sf9 | IC50 |
0.119 μM
Compound: 3; LY-2157299
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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
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[PMID: 31299584] |
| Sf9 | IC50 |
0.119 μM
Compound: 4; LY-2157299
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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
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[PMID: 31810777] |
| Sf9 | IC50 |
0.129 μM
Compound: 3; LY-2157299
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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
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[PMID: 31303386] |
| Sf9 | IC50 |
69.4 nM
Compound: 4; LY-2157299
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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
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[PMID: 26483198] |
| U-251 | CC50 |
16.96 μM
Compound: LY-2157299
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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
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[PMID: 38626523] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 700874-72-2
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Appearance Solid
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Masse moléculaire 369.42
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Formule C22H19N5O
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Color White to yellow
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SMILES
CC1=CC=CC(C2=NN3C(CCC3)=C2C4=CC=NC5=C4C=C(C=C5)C(N)=O)=N1
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Synonyms
LY2157299
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (71)
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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 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.
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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 -
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 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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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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
Cell Rep
2022 Aug 30;40(9):111253. PMID: 36044839 -
Br J Cancer
Fibroblast growth factor signals drive the metastatic behavior in small cell lung cancer. [Abstract]2025 Dec 13. PMID: 41390896 -
Antioxidants (Basel)
2024 Jul 29;13(8):914. PMID: 39199160 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
Int J Mol Sci
Galunisertib Exerts Antifibrotic Effects on TGF-β-Induced Fibroproliferative Dermal Fibroblasts. [Abstract]2022 Jun 15;23(12):6689. PMID: 35743131 -
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 -
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 -
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 -
Int Immunopharmacol
GPRC5A+ myCAFs promote ESCC progression via TGF-β-induced fibroblast activation and ANXA1-mediated M2 macrophage polarization. [Abstract]2025 Oct 11:167:115663. PMID: 41082840 -
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 -
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 -
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 -
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 -
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 -
J Cell Mol Med
2020 Mar;24(6):3656-3668. PMID: 32064783 -
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 -
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 -
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 -
Cytokine
2026 Aug:204:157169. PMID: 42143915 -
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 -
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 -
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 -
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 -
Brain Sci
2019 Dec 30;10(1):20. PMID: 31905898 -
Pathol Oncol Res
2021 Nov 19;27:1609997. PMID: 34867089 -
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bioRxiv
2025 May 4:2025.04.29.651320. PMID: 40654780 -
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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Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. 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]
[2]. 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]
[3]. 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]
[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]
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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