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Biological Activity:
Orally active transforming growth factor beta receptor (TGF-βR) kinase inhibitor under clinical development; IC50 values to be 86 nm (TβR1) and 2 nM (TβR2) respectively.
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. [online]
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. [online]
P Workman. New cancer drugs in the horizon. Fut. Oncology 2005, 1(3), 315-318. [online]
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
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