Bentamapimod (AS-602801) 是一种ATP竞争性的 JNK 抑制剂,作用于 JNK1,JNK2 和 JNK3的IC50 分别为 80 nM,90 nM 和 230 nM。
别名:AS-602801
Bentamapimod (别名:AS-602801) 是一种ATP竞争性的 JNK 抑制剂,作用于 JNK1,JNK2 和 JNK3的IC50 分别为 80 nM,90 nM 和 230 nM。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: Bentamapimod (30 mg/kg) on nude mice bearing xenografts biopsied from women with endometriosis (BWE) causes 29% regression of lesion. 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%). Bentamapimod reduces inflammatory cytokines in endometriotic lesions, while levels of cytokines in ipsilateral horns are unaffected.
体外实验* | |
---|---|
细胞系 | PANC-1, A2780, and A549 human cancer cells |
方法 | Bentamapimod (AS602801) is dissolved in DMSO (10 mM) and stored, and then diluted with appropriate media before use. 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. |
浓度 | 2.5, 5, and 7.5 μM |
处理时间 | 3 days |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
体内实验* | |
---|---|
动物模型 | 5-week-old athymic (ncr/nude) ovariectomized mice |
配制 | dissolved in in DMSO (10 mM) and diluted with PBS |
剂量 | 10 mg/kg and 30 mg/kg/animal for 30 days |
给药处理 | gavage |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
分子量 | 457.55 |
分子式 | C25H23N5O2S |
CAS号 | 848344-36-5 |
溶解性(25°C) | DMSO 10 mM |
储存条件 |
粉末型式 -20°C 3年;4°C 2年 溶于溶剂 -80°C 6个月;-20°C 1个月 |
运输方式 | 冰袋运输,根据产品的不同,可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.1856 mL | 10.9278 mL | 21.8555 mL |
5 mM | 0.4371 mL | 2.1856 mL | 4.3711 mL |
10 mM | 0.2186 mL | 1.0928 mL | 2.1856 mL |
小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
其他相关的JNK产品 |
---|
JIP-1(153-163)
JIP-1(153-163) (TI-JIP) 是 c-JNK 的肽类抑制剂,该序列是基于 JIP-1 的153-163肽段修饰的 (Modifications: Phe-11 = C-terminal amide)。 |
JNK3 inhibitor-5
JNK3 inhibitor-5 是一种有效的、选择性的 JNK3 抑制剂,其 IC50 为 0.379 nM。 |
JNK-1-IN-1
JNK-1-IN-1 是一种 JNK-1 抑制剂。 |
JNK2-IN-1
JNK2-IN-1 是一种 JNK2 抑制剂 (Kds: 79.2 Μm)。 |
JNK-1-IN-2
JNK-1-IN-2 是一种 JNK-1 抑制剂 (IC50: 33.5 nM)。 |
产品仅供科学研究或药证申报的用途使用,不为任何个人或者非科研性质的其他用途提供服务。
Copyright © 2010-2022 AbMole版权所有 沪ICP备16047849号 沪公网安备 31011502012228号