LY2157299

Grouped product items
SizePrice Qty
5mg
$175.00
50mg
$755.00
Catalog Number : 7007224

description

LY2157299 is a potent inhibitor of Transforming Growth factor-Beta Receptor I (TGF-BetaR). TGF-Beta1 is involved in the control of cell growth, proliferation, differentiation, and apoptosis. LY2157299 is reported to disrupt Smad-2 phosphorylation in Human Umbilical Vein Endothelial Cells (HUVEC) and inhibit the growth and migration of tumor cells.
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Additional Information

Applications:
FA
Synonyms:
LY 2157299, LY-2157299, Galunisertib
Formulation:
Crystalline solid
Chemical Name:
4-[2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]quinoline-6-carboxamide
Molecular Formula:

C22H19N5O

Molecular Weight:
369.4
CAS Number
700874-72-2
Purity:
≥98%
Storage Conditions:
Product should be kept at -20°C.
References:

Bueno, L., de Alwis, D. P., Pitou, C., Yingling, J., Lahn, M., Glatt, S., & Trocóniz, I. F. (2008). Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-β kinase antagonist, in mice. European journal of cancer44(1), 142-150.

Herbertz, S., Sawyer, J. S., Stauber, A. J., Gueorguieva, I., Driscoll, K. E., Estrem, S. T., ... & Slapak, C. A. (2015). Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway. Drug design, development and therapy9, 4479.

Maier, A., Peille, A. L., Vuaroqueaux, V., & Lahn, M. (2015). Anti-tumor activity of the TGF-β receptor kinase inhibitor galunisertib (LY2157299 monohydrate) in patient-derived tumor xenografts. Cellular Oncology38(2), 131-144.

Yingling, J. M., Shou, J., Xia, X., Chen, Y., Yan, L., Evans, W., ... & Law, K. (2006). A small molecule inhibitor of TGFβ RI kinase potentiates VEGF dependent angiogenesis in vitro. Cancer Research66(8 Supplement), 59-59.

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