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LY2109761
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产品编号 | 包装单位 | 单价(元) | 国内现货 | 国外库存 | 询价单 |
4086236 | 5 MG | 1120 | |||
4086236 | 25 MG | 3920 |
产品别名
700874-71-1
LY2109761
LY-2109761
4-[5,6-Dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]-quinoline
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C26H27N5O2 |
Molecular weight | 441.52 |
MDL number | MFCD12923354 |
Application【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. |
Biochem/physiol Actions【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. |
产品性质
Assay【测定】 | ≥98% (HPLC) |
form【形式】 | powder |
color【颜色】 | white to beige |
solubility【溶解性】 | DMSO: 2 mg/mL, clear |
storage temp.【储存温度】 | −20℃ |
安全信息
Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
WGK | WGK 3 |