| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| L408237-1ml |
1ml |
现货  |
|
| 英文别名 | 7-(2-morpholinoethoxy)-4-(2-(pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline |
|---|---|
| 规格或纯度 | Moligand™, 2mM in DMSO |
| 英文名称 | LY2109761 |
| 生化机理 | LY2109761 是一种新型选择性 TGF-β 受体 I/II 型（TβRI/II）双重抑制剂，在无细胞试验中的Ki值分别为 38 nM 和 300 nM；研究表明它对 Smad2 的磷酸化有负面影响。LY2109761 可阻止自噬并诱导细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 转化生长因子 beta 受体 1 抑制剂；转化生长因子 beta 受体 2 抑制剂 |
| 产品介绍 |
LY2109761是一种新型的，选择性的TGF-β receptor type I/II (TβRI/II)双重抑制剂，Ki分别为38 nM和300 nM，对Smad2的磷酸化产生负面影响。A small molecule inhibitor of the TGF-β receptor type 1/type II kinases. Information LY2109761 is a novel selectiveTGF-β receptor type I/II (TβRI/II)dual inhibitor withKiof 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. LY2109761 blocksautophagyand inducesapoptosis. LY2109761 treatment induces a dose-dependent low-anchorage growth inhibition of L3.6pl/GLT cells, leading to ~33% or 73% inhibition at 2 μM and 20 μM, respectively, which can be strongly enhanced when combined with gemcitabine in combination index value of 0.36581. Blocking TβRI/II kinase activity with LY2109761 (5 μM) completely suppresses both the basal and TGF-β1-stimulated migration and invasion of L3.6pl/GLT cells, significantly enhances the detachment-induced apoptosis by 26% at 8 hours treatment, and completely suppresses TGF-β–induced Smad2 phosphorylation. LY2109761 treatment at 1 nM is sufficient to significantly block the migration and invasion but not adhesion of hepatocellular carcinoma cells by increasing E-cadherin expression. LY2109761 pretreatment enhances radiosensitivity of glioblastoma cells via TGF-β signaling blockage. LY2109761 (10 μM) reduces the self-renewal and proliferation of GBM-derived cancer stem–like cells (CSLC), which can be significantly enhanced when combined with radiation. In vivo Administration of LY2109761 (50 mg/kg) alone or in combination with gemcitabine (25 mg/kg) significantly reduces the tumor volume by ~70% and ~90%, respectively, prolongs the survival with the median survival duration of 45.0 days and 77.5 days, respectively, and reduces spontaneous abdominal metastases in the L3.6pl/GLT Xenograft mice model. In consistent with the in vitro effect, administration of LY2109761 alone or in combination with radiation, markedly inhibits tumor growth in the orthotopical CSLC glioblastoma model by 43.4% and 76.3%, respectively, decreases tumor invasion and tumor microvessel density, and significantly enhances radiation-induced tumor growth delay in the U87MG xenograft mice model. cell lines： Concentrations：Dissolved in DMSO, final concentrations ~10 μM Incubation Time：48 hours Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | C1CC2=C(C(=NN2C1)C3=CC=CC=N3)C4=C5C=CC(=CC5=NC=C4)OCCN6CCOCC6 |
| 分子量 | 441.52 |
| Reaxy-Rn | 14275148 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14275148&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 48 mg/mL (201.47 mM); Ethanol: 3 mg/mL (12.59 mM); Water: Insoluble; |
|---|
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