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Bentamapimod
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Bentamapimod图片
CAS NO:848344-36-5
包装:5mg, 10mg
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品名称
AS-602801
产品介绍

生物活性

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.


化学数据

分子量457.55
分子式C25H23N5O2S
CAS号848344-36-5
纯度>98%
溶解性(25°C)DMSO 10 mM
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
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

动物实验
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

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
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。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM2.1856 mL10.9278 mL21.8555 mL
5 mM0.4371 mL2.1856 mL4.3711 mL
10 mM0.2186 mL1.0928 mL2.1856 mL