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| 品牌 | absin | CAS | 848344-36-5 |
|---|---|---|---|
| 分子式 | C25H23N5O2S | 纯度 | 98% |
| 分子量 | 457.55 | 货号 | abs47028128 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a novel, orally active inhibitor of J | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
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,JNK3 |
| In 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. |
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| 研究领域 | |
| 研究领域 | CancerSignal transductionProtein phosphorylationSerine/threonine kinasesMAPK pathway ImmunologyInnate ImmunityTLR Signaling NeuroscienceDevelopment Signal TransductionProtein PhosphorylationSer / Thr KinasesMAPK Pathway Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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