LY2157299 、CAS号: 700874-72-2

LY2157299的产品信息
英文名称：LY2157299，请联系客服QQ：1443869017获知LY2157299的库存和报价。
  上海赛鑫生物技术有限公司 供应美国原装进口：LY2157299
所属分类：现货> -20摄氏度低温储备>TGF-beta / Smad YZ剂 >> LY2157299
 别名：N/A
分子式：C₂₂H₁₉N₅O
分子量：369.42
CAS号：700874-72-2
物质化学性质：
 LY2157299 的生物活性LY2157299 is a novel selective small molecule transforming growth factor beta receptor (TGF-βR) kinase inhibitor with IC50 of 86 nM and 2 nM for TβR1 and 2 nM, respectively. LY2157299 was well tolerated at both doses of 40 and 80 mg and no drug-related CTCAE Grade 3 or 4 toxicities were observed. Absorption of LY2157299 was rapid as determined by plasma concentrations at the first sampling time (0.5 hours). Daily oral administration of LY2157299 was safe and well tolerated at the two dose levels and the pharmacokinetic profile was consistent with the prediction derived from preclinical PK/PD model. As would be predicted for an inhibitor of TGF-β signaling, LY2157299 blocked the phsophorylation of Smad2 but had no effect on fibroblast growth factor (FGF) or platelet-derived growth factor (PDGF) signaling. However, another study reported that LY2157299 induced angiogenesis and enhanced VEGF- and basic-fibroblast-growth-factor- induced angiogenesis in a Matrigel-plug assay, whereas adding an alpha5-integrin -neutralizing antibody to the Matrigel selectively inhibited this enhanced response. ^[1][2][3][4]