Name: Enzalutamide
Brand: TargetMol
SKU: T6002
Price: 233 CNY
Availability: InStock
Rating: 5 (10 reviews)

Enzalutamide

很棒

产品编号 T6002Cas号 915087-33-1

别名 恩杂鲁胺, MDV3100

Enzalutamide (MDV3100) 是一种雄激素受体 (AR) 拮抗剂 (IC50=36 nM in LNCaP)。Enzalutamide 可以激活自噬，具有抗肿瘤活性，常用于去势抵抗性前列腺癌的治疗。

规格

价格

库存

数量

1 mg

¥ 233

In stock

5 mg

¥ 535

In stock

10 mg

¥ 859

In stock

25 mg

¥ 1,550

In stock

50 mg

¥ 2,570

In stock

100 mg

¥ 3,720

In stock

200 mg

¥ 5,230

In stock

500 mg

¥ 7,590

In stock

1 mL x 10 mM (in DMSO)

¥ 645

In stock

产品介绍

生物活性

产品描述	Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP). Enzalutamide activates autophagy, has antitumor activity, and is commonly used in the treatment of desmoplasia-resistant prostate cancer.
靶点活性	SJSA-1:34.7 μM (LD50), PC3 cells:12 μM (LD50), Androgen receptor:36 nM (LNCaP cells), LNCaP cells:12 μM (LD50)
体外活性	方法：人前列腺癌细胞 LNCaP、PC3 和人骨肉瘤细胞 SJSA-1 用 Enzalutamide (0.01-100 μM) 处理 1 h，使用 MTT 检测细胞活力。结果：Enzalutamide 显示降低了所有细胞系的生存能力，对 LNCaP、PC3 和 SJSA-1 细胞系的 LD50 分别为 12 μM、23.4 μM 和 34.7 μM。[1] 方法：人前列腺癌细胞 VCaP 用 Enzalutamide (10 μM) 处理 1-3 天，使用 Western Blot 方法检测靶点蛋白表达水平。结果：Enzalutamide 上调 cleaved-PARP 表达，诱导细胞凋亡。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 Enzalutamide (1-50 mg/kg) 灌胃给药给携带人去势抵抗性肿瘤 (CRPC) LNCaP-AR-Lux 的 CB17SCID 小鼠，每天一次，持续二十八天。结果：Enzalutamide 在 CRPC 异种移植物模型中诱导肿瘤体积的消退，并在 AR 过度扩张的前列腺癌症细胞中诱导细胞凋亡。[3] 方法：为评估 AR 在性成熟后骨代谢和骨骼生长中的作用，将 Enzalutamide (10-100 mg/kg，1% carboxymethyl cellulose+0.5% Tween 80+5% dimethylsulfoxide) 口服给药给 C57BL/6N 小鼠，每天一次，持续二十一天。结果：Enzalutamide 降低了轴骨中的骨量，Enzalutamide 显著降低了轴心骨骼的机械强度。性成熟后，Enzalutamide 可减少雄性小鼠中轴骨骼的骨量，但不能减少阑尾骨骼的骨量。[4]
细胞实验	For in vitro experiments, LNCaP or LNCaP/AR cells (10^4 cells/well) were androgen-starved by growth in media containing 5-10% charcoal-stripped serum for 3-5 days. Then the cells were challenged with various concentrations of R1881, bicalutamide, RD162 or MDV3100 in media containing 5-10% charcoal-stripped serum [1].
动物实验	In vivo tumorigenicity experiments were done by subcutaneous injection of 10^6 cells (100 uL in 50% Matrigel and 50% growth media) into the flanks of castrated male SCID mice. Daily gavage treatment (using a formulation of 1% carboxymethyl cellulose, 0.1% Tween-80, 5% DMSO) was initiated when tumor size reached ~100 mm3. Tumor size was measured weekly in three dimensions (l x w x d) with calipers. For in vivo luciferase imaging, d-luciferin substrate (100 μL, 15 mg/mL) was injected intraperitoneally. After 5 minutes, mice were anesthetized using isofluorane and imaged using a cooled charged-coupled device IVIS camera. Data were analyzed using Living Image 2.30 software [1].
别名	恩杂鲁胺, MDV3100

化学信息

分子量	464.44
分子式	C₂₁H₁₆F₄N₄O₂S
CAS No.	915087-33-1
Smiles	S=C1N(C(C)(C)C(=O)N1C2=CC(C(F)(F)F)=C(C#N)C=C2)C3=CC(F)=C(C(NC)=O)C=C3
密度	1.49 g/cm3

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 260 mg/mL (559.81 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 8.5 mg/mL (18.3 mM), Suspension.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1531 mL	10.7657 mL	21.5313 mL	107.6565 mL
5 mM	0.4306 mL	2.1531 mL	4.3063 mL	21.5313 mL
10 mM	0.2153 mL	1.0766 mL	2.1531 mL	10.7657 mL
20 mM	0.1077 mL	0.5383 mL	1.0766 mL	5.3828 mL
50 mM	0.0431 mL	0.2153 mL	0.4306 mL	2.1531 mL
100 mM	0.0215 mL	0.1077 mL	0.2153 mL	1.0766 mL

体内实验配液计算器