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MDV3100
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。
MDV3100图片
CAS NO:915087-33-1
包装:2mg, 5mg, 10mg, 50mg
包装与价格:
包装价格(元)
Free Sample (0.5-1 mg)电议
10mM*1mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议

产品名称
Enzalutamide, MDV-3100
产品介绍

生物活性

恩杂鲁胺 Enzalutamide (MDV3100)是一种雄激素受体(AR)拮抗剂,IC50为36 nM。Enzalutamide是雄激素受体(AR)拮抗剂,IC50为36 nM。在加入16β-[18F]氟-5α-DHT (18-FDHT)的竞争性实验中发现作用于AR时Enzalutamide比bicalutamide具有更高的亲和力。而Enzalutamide作用于LNCaP/AR(AR-过量表达)前列腺细胞时没有效果。


化学数据

分子量464.44
分子式C21H16F4N4O2S
CAS号915087-33-1
纯度100.0%
溶解性(25°C)DMSO 60 mg/mL
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VCaP cell line
方法Proliferation assays Trypsinized VCaP cells were adjusted to a concentration of 100,000 cells per mL in phenol-red-free RPMI 1640 (with 5% CSS), and dispensed in 16 μL aliquots into CellBIND 384 well plates (Corning, Lowell, MA). Cells were incubated for 48 hours, after which ligand was added in a 16 μL volume to the RPMI culture medium. For the antagonist mode assay, the ligands were diluted in culture medium also containing 30 pM R1881 (final [R1881] = 15 pM). After 7 days’ incubation, 16 μL of CellTiter-Glo Luminescent Cell Viability Assay (Promega, Madison, WI) was added and Relative Luminescence Units (RLUs) measured. In the agonist mode assay, percent viability of the samples was calculated as: % viability=[RLU sample-RLU medium without cells]/[RLU DMSO treated cells-RLU medium without cells]. In the antagonist mode assay, the percent viability of the samples was calculated as: % viability=[RLU sample-RLU VCaP without R1881]/[RLU R1881-treated cells - RLU VCaP without R1881].
浓度0~10μM
处理时间48h

动物实验
动物模型LNCaP/AR(cs) xenograft model in mice
配制prepared in 18% PEG-400, 1% Tween-80 and 1% povidone, and were formulated for dosing in 15% Vitamin E-TPGS and 65% of a 0.5% w/v CMC solution in 20 mM citrate buffer (pH 4.0).
剂量100mg/kg
给药处理oral 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 mM2.1531 mL10.7657 mL21.5313 mL
5 mM0.4306 mL2.1531 mL4.3063 mL
10 mM0.2153 mL1.0766 mL2.1531 mL