LY2109761
Cat. No.:YN460011
CAS No. :700874-71-1
产品名称: | LY2109761 |
CAS No.: | 700874-71-1 |
Chemical Name: | 4-[5,6-dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]-quinoline |
Synonyms: | LY 2109761; LY2109761 |
分子量: | 441.52 |
分子式: | C₂₆H₂₇N₅O₂ |
SMILES: | N12N=C(C(C3=C4C=CC(OCCN5CCOCC5)=CC4=NC=C3)=C1CCC2)C6=NC=CC=C6 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | LY2109761是可口服,选择性的TGF-β receptor type I/II抑制剂,Ki分别为38 nM 和 300 nM。 |
IC50和靶点: | |
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Li, H.y., McMillen, W.T., Heap, C.R., et al.Optimization of a dihydropyrrolopyrazole series of transforming growth factor-β type I receptor kinase domain inhibitors: Discovery of an orally bioavailable transforming growth factor-β receptor type I inhibitor as antitumor agentJ. Med. Chem.51(7),2302-2306(2008)
Melisi, D., Ishiyama, S., Sclabas, G.M., et al.LY2109761, a novel transforming growth factorβreceptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasisMol. Cancer Ther.7(4),829-840(2008)
Flechsig, P., Dadrich, M., Bickelhaupt, S., et al.LY2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of TGF-β and BMP-associated proinflammatory and proangiogenic signalsClin. Cancer Res.18(13),3616-3627(2012)