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- LY2109761 | TGF-β receptor type I/II inhibitor
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- LY2109761 | TGF-β receptor type I/II inhibitor
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- Molecular Target
- Ser/Thr Kinase
- TKL Kinase
- LY2109761 | TGF-β receptor type I/II inhibitor
Product Description
LY-2109761 is an orally-bioavailable pyrrolopyrazole inhibitor of the TGF-b1/2 kinase subtypes in Phase I and II clinical studies for malignant malignancies. With Ki potencies of 38 nM and 300 nM, respectively, LY-2109761 has been studied in metastatic pancreatic cancer cells and completely inhibits basal and TGF-b1-stimulated migration and invasion of L3.6pl/GLT cells. [1] LY-2109761 treatment suppresses Smad2 phosphorylation and the Smad-dependent downstream pathway. [2]
LY-2109761 is synergistic with gemcitabine, significantly prolonging survival times and reducing tumor volume and metastatic events. [1] Additionally, LY2109761 enhances radiation response and prolongs survival in glioblastomas. Prolliferation assays displayed a reduction of NMA-23 cell viability and inhibited self-renewal of glioblastoma cancer stem-like cells (CSLC). [3]
Technical information:
| Chemical Formula: | C26H27N5O2 | |
| CAS #: | 700874-71-1 | |
| Molecular Weight: | 441.52 | |
| Purity: | > 98% | |
| Appearance: | Pale Brown | |
| Chemical Name: | 7-(2-morpholinoethoxy)-4-(2-(pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | LY-2109761, LY 2109761, LY2109761 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Melisi et al., LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. Mol. Cancer Ther. 2008, 7(4), 829-840. Pubmed ID: 1841379 |
| 2. | Connolly et al., Complexities of TGF-? targeted cancer therapy. Int. J. Biol. Sci. 2012, 8(7), 964-978. Pubmed ID: 22811618 |
| 3. | Zhang et al., Blockade of TGF-? signaling by the TGF?R-I kinase inhibitor LY2109761 enhances radiation response and prolongs survival in glioblastoma. Cancer Res. 2011, 71, 7155-7167. Pubmed ID: 22006998 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
