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LY2109761

Chemical Structure : LY2109761

CAS No.: 700874-71-1

LY2109761 (LY 2109761;LY-2109761)

Catalog No.: PC-42887Not For Human Use, Lab Use Only.

LY2109761 is a potent, selective and orally active TGF-β RI/II dual inhibitor with Ki of 38/300 nM, respectively.

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Biological Activity

LY2109761 is a potent, selective and orally active TGF-β RI/II dual inhibitor with Ki of 38/300 nM, respectively.
LY2109761 completely inhibits TGF-β-induced Sma2 phosphorylation on tumor cells or the liver microenviroment, inhibits the L3.6pl/GLT soft agar growth。
LY2109761 suppresses both basal and TGF-β1-induced cell migration and invasion, and stimulates anoikis in vitro。
LY2109761 significantly reduces the tumor burden as well as spontaneous abdominal metastases, and prolongs survival combined with gemicitabine in vivo model of pancreatic cancer.

Physicochemical Properties

M.Wt 441.5249
Formula C26H27N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Quinoline, 4-[5,6-dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]-

References

1. Mazzocca A, et al. Hepatology. 2009 Oct;50(4):1140-51.

2. Zhang M, et al. Cancer Res, 2011, 71(23), 7155-7167.

3. Melisi D, et al. Mol Cancer Ther, 2008, 7(4), 829-840.

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