Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Bentamapimod (AS 602801) 是一种ATP 竞争性的JNK 抑制剂,对JNK1、JNK2和JNK3的IC50分别为 80、90 和 230 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 216 | 现货 | ||
2 mg | ¥ 298 | 现货 | ||
5 mg | ¥ 549 | 现货 | ||
10 mg | ¥ 963 | 现货 | ||
25 mg | ¥ 1,490 | 现货 | ||
50 mg | ¥ 1,980 | 现货 | ||
100 mg | ¥ 3,680 | 现货 | ||
500 mg | ¥ 7,880 | 现货 | ||
1 g | ¥ 10,800 | 现货 |
产品描述 | Bentamapimod (AS 602801) is a novel, orally active inhibitor of JNK. |
靶点活性 | JNK3:230 nM, JNK1:80 nM, JNK2:90 nM |
体外活性 | 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[2]. |
体内活性 | 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[3]. |
细胞实验 | AS 602801 (AS602801) is dissolved in DMSO (10 mM) and stored, and then diluted with appropriate media before use[2]. PANC-1, A2780, and A549 human cancer cells and IMR90 human normal fibroblasts are treated without (control) or with the indicated concentrations of AS 602801 (2.5, 5, and 7.5 μM) for 3 days. The number of viable cells (left panels) and the percentage of dead cells (right panels) are determined using trypan blue as a vital dye[2]. |
别名 | AS 602801 |
分子量 | 457.55 |
分子式 | C25H23N5O2S |
CAS No. | 848344-36-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4.57 mg/mL (9.98 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1856 mL | 10.9278 mL | 21.8555 mL | 54.6388 mL |
5 mM | 0.4371 mL | 2.1856 mL | 4.3711 mL | 10.9278 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Bentamapimod 848344-36-5 MAPK JNK inhibit AS602801 Inhibitor AS 602801 AS-602801 inhibitor