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LY2409881 hydrochloride
产品别名
LY2409881 hydrochloride
2-{5-Chloro-2-[3-(4-methylpiperazin-1-yl)propylamino]-pyrimidin-4-yl}benzo[b]thiophene-4-carboxylic acid cyclopropylamide hydrochloride
N-Cyclopropyl-2-[5-Chloro-2-[[3-(4-methylpiperazin-1-yl)propyl]amino]pyrimidin-4-yl]benzo[b]thiophene-4-carboxamide hydrochloride
LY-2409881 hydrochloride
LY 2409881 hydrochloride
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C24H29ClN6OS · xHCl |
| Molecular weight | 485.04 (free base basis) |
| MDL number | MFCD28900675 |
| Biochem/physiol Actions【生化/生理作用】 | LY2409881 is a potent IκΒ kinase β (IKK2, IKKβ, IKKbeta) inhibitor (IC50 = 30 nM) that effectively inhibits 10 ng/mL TNFα-induced IκB phosphorylation in LY10 DLBCL cells (by >95%; 10 μM) and exhibits good selectivity by kinase profiling among more than 300 kinases (>10-fold selectivity). LY2409881 enhances TNFα cytotoxicity in SKOV3 ovarian cancer cultures (~20% survival with 316 nM LY2409881 & 10 ng/mL TNFα in 72 hrs; 100% survival with LY2409881 or TNFα alone) by blocking NF-κB antiapoptotic signal activation without affecting TRADD & FADD proapoptotic pathway induction. When administered in vivo, LY2409881 is shown to suppress LY10 xenograft-derived tumor growth in mice (50-200 mg/kg, twice weekly ip.). |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| storage condition【储存条件】 | desiccated |
| color【颜色】 | white to beige |
| solubility【溶解性】 | H2O: 2 mg/mL, clear |
| storage temp.【储存温度】 | −20℃ |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
