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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。

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 | 
Enzalutamide 相关产品
| 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), LNCaP cells:12 μM (LD50), Androgen receptor:36 nM (LNCaP cells), PC3 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。  | 
| 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。  | 
| 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 | 
| 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 | 
| 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: 257 mg/mL (553.35 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 
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