Bulk Inquiry
LY 2157299
- Galunisertib
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C22H19N5O
- MW: 369.42
Description
LY2157299 (Galunisertib) is an orally active transforming growth factor-β receptor (TGF-βR) kinase inhibitor under clinical development. LY2157299 inhibits TGF-β receptor type I (TβR1/ALK5) and TGF-β receptor type II (TβR2) with IC50 values of 86 nM and 2 nM, respectively, resulting in suppression of TGF-β-mediated signaling.
The TGF-β pathway regulates cell proliferation, differentiation, immune modulation, epithelial-to-mesenchymal transition (EMT), fibrosis, and tumor progression. LY2157299 is widely used as a research tool for investigating TGF-β signaling and has been evaluated in oncology and fibrosis-related therapeutic development.
Key Features
- Orally active TGF-β receptor kinase inhibitor
- IC50: 86 nM for TβR1 (ALK5)
- IC50: 2 nM for TβR2
- Inhibits TGF-β-mediated signaling pathways
- Clinically investigated compound (Galunisertib)
Applications
- TGF-β signaling research
- Fibrosis and tissue remodeling studies
- Cancer biology and tumor progression research
- EMT and metastasis investigations
- Smad signaling pathway studies
More Information
| Parent CAS No. | 700874-72-2 |
|---|---|
| Chemical Name | 4-[2-(6-Methyl-pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]-quinoline-6-carboxylic acid amide |
| SMILES | N1N2CCCC2=C(C2C3=CC(C(=O)N)=CC=C3N=CC=2)C=1C1C=CC=C(C)N=1 |
| MFCD | MFCD12923319 |
| InChi | InChI=1S/C22H19N5O/c1-13-4-2-5-18(25-13)21-20(19-6-3-11-27(19)26-21)15-9-10-24-17-8-7-14(22(23)28)12-16(15)17/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,23,28) |
| InChiKey | IVRXNBXKWIJUQB-UHFFFAOYSA-N |
| CID | 10090485 |
| Short Description | TGF-βR2 inhibitor |
References
- L Bueno et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-β kinase antagonist, in mice. Eur. J. Cancer. 2008, 44(1), 142-150.
- Z Liu et al. VEGF and inhibitors of TGFβ type-I receptor kinase synergistically promote blood-vessel formation by inducing 5-integrin expression. J. Cell Sci. 2009, 122, 3294-3302.
- P Workman. New cancer drugs in the horizon. Fut. Oncology 2005, 1(3), 315-318.
- D. Muñoz-Espín et al. Programmed cell senescence during mammalian embryonic development. Cell. 2013 Nov 21;155(5):1104-18. doi: 10.1016/j.cell.2013.10.019. Epub 2013 Nov 14.
- List of publications using LY 2157299 (Axon 1491) purchased from Axon Medchem
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