Molecular structure of LY2157299, CAS Number: 700874-72-2
LY2157299 (CAS 700874-72-2)
See product citations (3)
Alternate Names:
Galunisertib; 4-(2-(6-Methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide
Application:
LY2157299 is a potent TGF β RI inhibitor
CAS Number:
700874-72-2
Molecular Weight:
369.42
Molecular Formula:
C22H19N5O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
LY2157299, also known as galunisertib, is an investigational molecule that has been the subject of extensive research due to its mechanism of selectively inhibiting the TGF-β receptor I kinase. This specificity makes it a compound of interest in the study of cellular signaling pathways influenced by the transforming growth factor-beta (TGF-β) superfamily, which are known to play a role in the regulation of cell proliferation, differentiation, and apoptosis. In oncology research, LY2157299′s potential to modulate the TGF-β pathway is studied for its impact on tumor microenvironment and cancer cell growth, particularly in the context of stromal interaction and immune response modulation. Researchers also investigate the compound′s effects on fibrosis, as TGF-β signaling is critically involved in the fibrotic process.
LY2157299 (CAS 700874-72-2) References
- Differential Inhibition of the TGF-β Signaling Pathway in HCC Cells Using the Small Molecule Inhibitor LY2157299 and the D10 Monoclonal Antibody against TGF-β Receptor Type II. | Dituri, F., et al. 2013. PLoS One. 8: e67109. PMID: 23826206
- Defining a therapeutic window for the novel TGF-β inhibitor LY2157299 monohydrate based on a pharmacokinetic/pharmacodynamic model. | Gueorguieva, I., et al. 2014. Br J Clin Pharmacol. 77: 796-807. PMID: 24868575
- Effects of TGF-beta signalling inhibition with galunisertib (LY2157299) in hepatocellular carcinoma models and in ex vivo whole tumor tissue samples from patients. | Serova, M., et al. 2015. Oncotarget. 6: 21614-27. PMID: 26057634
- Brain perfusion and permeability in patients with advanced, refractory glioblastoma treated with lomustine and the transforming growth factor-β receptor I kinase inhibitor LY2157299 monohydrate. | Sepulveda-Sanchez, J., et al. 2015. Oncol Lett. 9: 2442-2448. PMID: 26137087
- Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway. | Herbertz, S., et al. 2015. Drug Des Devel Ther. 9: 4479-99. PMID: 26309397
- Galunisertib (LY2157299), a transforming growth factor-β receptor I kinase inhibitor, attenuates acute pancreatitis in rats. | Liu, X., et al. 2016. Braz J Med Biol Res. 49: e5388. PMID: 27509307
- TGFβR1 Blockade with Galunisertib (LY2157299) Enhances Anti-Neuroblastoma Activity of the Anti-GD2 Antibody Dinutuximab (ch14.18) with Natural Killer Cells. | Tran, HC., et al. 2017. Clin Cancer Res. 23: 804-813. PMID: 27756784
- Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor. | Yingling, JM., et al. 2018. Oncotarget. 9: 6659-6677. PMID: 29467918
- Polymeric Nano-Micelles as Novel Cargo-Carriers for LY2157299 Liver Cancer Cells Delivery. | Hanafy, NAN., et al. 2018. Int J Mol Sci. 19: PMID: 29509706
- LY2157299 Monohydrate, a TGF-βR1 Inhibitor, Suppresses Tumor Growth and Ascites Development in Ovarian Cancer. | Zhang, Q., et al. 2018. Cancers (Basel). 10: PMID: 30087253
- Targeting FOXA1-mediated repression of TGF-β signaling suppresses castration-resistant prostate cancer progression. | Song, B., et al. 2019. J Clin Invest. 129: 569-582. PMID: 30511964
- Brain-targeting biomimetic nanoparticles for codelivery of celastrol and LY2157299 for reversing glioma immunosuppression. | Zhu, S., et al. 2022. Int J Pharm. 619: 121709. PMID: 35364220
- Therapeutic Effect of Polymeric Nanomicelles Formulation of LY2157299-Galunisertib on CCl4-Induced Liver Fibrosis in Rats. | Panzarini, E., et al. 2022. J Pers Med. 12: PMID: 36579532
Inhibitor of:
β ig-h3, β-defensin 137, β-defensin 15, β-defensin 32, β-defensin 7, ACTR-IA, ACTR-IIB, AHNAK, ALK-1, Ang-2, Asporin, bFGF, BMP-5, BMP-6, BMPR-IB, BMPR-II, Cadherin (CDH), CHAD, COL13A1, COL1A2, COL4A2, CRIM1, Cryptic, DAF-1, Dlx-5, dsg1α, EG625591, EMILIN-1, FAST-1/2, FGF-BP3, FGL1, FHL-2, FIR, FLRG, Fussel-18, GDF-11, GDF-9, GDF-9B, gremlin-1, gremlin-2, GRIP-1, Hic-5, IDAS, IL-10Rβ, Inhibin β-A, Inhibin β-E, Integrin β8, Layilin, LOC645781, LOC728896, LOXL4, LRG1, LRRC70, LRRC72, Lumican, LYZL6, MAWDBP1, N-cadherin, netrin-1, Nodal, NOMO, NOMO1, NOMO2, NPN, Olfr372, Olfr47, Olfr538, OTTMUSG00000012042, PLAGL2, PMEPA1, PTGF-β, Reg lllγ, RGMb, SARA, Ski, Sm B/B′, Smad2, Smad3, Smad4, Smad5, Smad7, Smuc, SSEA-3, Tβ-b, TBCK, TBX22, TGF B-1, TGF beta, TGF beta 1, TGF beta RI, TGFα, TGFβ RII, TGFβ RIII, TGFβ2, TGFβ3, TGIF2LX1, TGIF2LX2, TIAF-1, TIMAP, Trichohyalin, Vasorin, and VWC1.Activator of:
ADMP, C030030A07Rik, C030039L03Rik, CD109, CD77 synthase (A4GALT), chordin, Cnpy1, COL2A1, Cripto, Cytokeratin 12, DAF-3, DAF-7, DAND5, Ear7, EG625424, FAM170B, FGF-5, fibrillin-3, Fibulin-2, IPCEF1, Lefty-2, MAWDBP1, PRDM13, Smad6, SnoN_SnoN2_SnoA, TBC1D30, TGF B-1, TGIF, TGIF2LX, TGIF2LY, TMEM100, TSC-22 D2, TSC-36, UHRF1BP1, Wnt-14b, and ZNF512.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
LY2157299, 5 mg | sc-391123 | 5 mg | $213.00 | |||
LY2157299, 10 mg | sc-391123A | 10 mg | $359.00 |