Art. -Nr.: HY-13226

Galunisertib

(Synonyms: LY2157299)

72 Cited Publications

Kundenbewertung

Based on 72 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.

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Reinheit: 99.90%
CAS. Nr.: 700874-72-2
Formel: C₂₂H₁₉N₅O
Molecular Weight:369.42

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Galunisertib Chemical Structure

CAS. Nr.: 700874-72-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (72)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen :

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]
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]
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]
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]
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]
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]
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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 700874-72-2
Appearance Solid
Molecular Weight 369.42
Formel C₂₂H₁₉N₅O
Color White to yellow
SMILES

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

LY2157299
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (72)

All Flow CytometryIn Vivo ImagingRT-PCRIFCell Imaging/Staining

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Journal Impact Factor

Signal Transduct Target Ther

TGF-β1-triggered maladaptive bone marrow endothelium impedes hematopoietic recovery. [Abstract]

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.
Cancer Cell

2026 May 21:S1535-6108(26)00220-5. PMID: 42167227
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

A positive feedback loop between SMAD3 and PINK1 in regulation of mitophagy. [Abstract]

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 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.
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)

Evidence for TGF-β1/Nrf2 Signaling Crosstalk in a Cuprizone Model of Multiple Sclerosis. [Abstract]

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

Arid1a mutation suppresses TGF-β signaling and induces cholangiocarcinoma. [Abstract]

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

Dual role of RACK1 in airway epithelial mesenchymal transition and apoptosis. [Abstract]

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

TGF-beta inhibitors influence leishmania infection outcome in a susceptible host. [Abstract]

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

TGF-β Promotes the Proliferation of Microglia In Vitro. [Abstract]

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

Uncovering a Key Role of ETS1 on Vascular Abnormality in Glioblastoma. [Abstract]

2021 Nov 19;27:1609997. PMID: 34867089
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

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
patent

US20250215017A1.
bioRxiv

2025 Jun 24.
bioRxiv

AI-assisted Drug Re-purposing for Human Liver Fibrosis. [Abstract]

2025 May 4:2025.04.29.651320. PMID: 40654780
bioRxiv

2024 November 11.
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
Patent

US20240197712A1.
Patent

US20240139331A1.
bioRxiv

2024 May 15.
bioRxiv

2023 Aug 15.
Patent

US20220378739A1.
Evid Based Complement Alternat Med

Pharmacological Activities of Natural Products through the TGF- β Signalling Pathway. [Abstract]

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
Universidad de Granada

2020 Sep.
bioRxiv

2020 Apr.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7069 mL

13.5347 mL

27.0695 mL

5 mM

0.5414 mL

2.7069 mL

5.4139 mL

10 mM

0.2707 mL

1.3535 mL

2.7069 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

Protocol 3

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.

Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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].

MedChemExpress (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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (396 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Galunisertib

72 Cited Publications

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Galunisertib

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Publications Citing Use of MedChemExpress (MCE) Galunisertib

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (72)

Lösungsmittel & Löslichkeit

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Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Galunisertib Related Classifications

HY-13226 Related Classifications