产品说明
应用
LY2109761 has been used as an inhibitor of type I and II transforming growth factor-beta (TGFβ) receptors to reduce the phosphorylation of SMAD2 (mothers against decapentaplegic homolog) in HepG2 cells.
生化/生理作用
LY2109761 suppresses transforming growth factor (TGF)-β1-induced fibroblasts proliferation and collagen synthesis in hypertrophic scar fibroblasts. Therefore, it is used in treating hypertrophic scars.
LY2109761 is a potent and orally active TGF-β receptor (TGFβR) type I & II dual inhibitor (IC50 = 70 and 322 nM against TGFβRI/ALK5 and TGFβRII autophosphorylation, respectively, with 4 μM ATP), inhibiting Fyn/JNK3/Lck/MKK6/SAPK2α only at much higher concentrations (58-89% inhibition at 20 μM) and exhibiting little or no potency against 37 other kinases (IC50 >20 μM). LY2109761 inhibits 0.25 ng/mL TGFβ-induced NIH/3T3 proliferation in cultures (IC50 = 210 nM; 2-hr pretreatment prior to TGFβ for 24 hrs) and suppresses human MX1 breast carcinoma xenograft tumor growth in mice in vivo (by ∼80% on day 37; 75 mg/kg p.o. bid from day 7 to 20). When administered in combination with gemcitabine (25 mg/kg/day i.p.), LY2109761 (50 mg/kg p.o. bid) is shown to significantly reduce tumor burden and spontaneous abdominal metastases in a murine model of metastatic pancreatic cancer.
基本信息
经验(实验)分子式 | C26H27N5O2 |
分子量 | 441.52 |
MDL编号 | MFCD12923354 |
产品性质
测定 | ≥98% (HPLC) |
形式 | powder |
颜色 | white to beige |
溶解性 | DMSO: 2 mg/mL, clear |
储存温度 | −20℃ |
安全信息
储存分类代码 | 13 - Non Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |