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- AS 602801 848344-36-5

- AS 602801 848344-36-5
AS 602801 848344-36-5
产品描述 描述 AS 602801(Bentamapimod) is a novel, orally active inhibitor of JNK.
纯度 98%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 Bentamapimod外观 powder可溶性/溶解性 DMSO : 14.29 mg/mL (31.23 mM; Need ultrasonic)生物活性 靶点 JNK1,JNK2,JNK3In vitro(体外研究) AS 602801 (AS602801) treatment induces cell death and accordingly decreased the number of viable cells in all three cell lines in a dose-dependent manner, suggesting that AS 602801 may have selective cytotoxic activity against neoplastic cells. AS 602801 exhibits cytotoxicity against both serum-cultured non-stem cancer cells and cancer stem cells derived from human pancreatic cancer, non-small cell lung cancer, ovarian cancer and glioblastoma at concentrations that did not decrease the viability of normal human fibroblasts. AS 602801 also inhibits the self-renewal and tumor-initiating capacity of cancer stem cells surviving AS 602801 treatment.In vivo(体内研究) Treatment of nude mice bearing xenografts biopsied from women with endometriosis (BWE) with 30 mg/kg AS 602801 (AS602801) causes 29% regression of lesion. Medroxyprogesterone acetate (MPA) or progesterone (PR) alone did not cause regression of BWE lesions, but combining 10 mg/kg AS 602801 with MPA caused 38% lesion regression. In human endometrial organ cultures (from healthy women), treatment with AS 602801 or MPA reduced matrix metalloproteinase-3 (MMP-3) release into culture medium. In organ cultures established with BWE, PR or MPA failed to inhibit MMP-3 secretion, whereas AS 602801 alone or MPA + AS 602801 suppresses MMP-3 production. In an autologous rat endometriosis model, AS 602801 causes 48% regression of lesions compared to GnRH antagonist Antide (84%). AS 602801 reduces inflammatory cytokines in endometriotic lesions, while levels of cytokines in ipsilateral horns are unaffected. Furthermore, AS 602801 enhances natural killer cell activity, without apparent negative effects on uterus.参考文献 参考文献 1. Ferrandi C, et al. Mult Scler. 2011 Jan;17(1):43-56.
研究领域 研究领域 CancerSignal transductionProtein phosphorylationSerine/threonine kinasesMAPK pathwayImmunologyInnate ImmunityTLR SignalingNeuroscienceDevelopmentSignal TransductionProtein PhosphorylationSer / Thr KinasesMAPK PathwayDrug DiscoverySmall Molecule DrugLead Compound DiscoveryAS 602801 848344-36-5温馨提示:本产品仅作科研实验使用,不支持临床等研究
