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Enzalutamide (Synonyms: 恩杂鲁胺; MDV3100) 纯度: 99.96%
Enzalutamide (MDV3100) 是一种雄激素受体 (androgen receptor (AR)) 拮抗剂,在 LNCaP 前列腺细胞中抑制 AR 的 IC50 值为 36 nM。Enzalutamide 是一种自噬 (autophagy) 激活剂。
Enzalutamide Chemical Structure
CAS No. : 915087-33-1
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10 mM * 1 mL in DMSO | ¥990 | In-stock | |
5 mg | ¥900 | In-stock | |
10 mg | ¥1392 | In-stock | |
50 mg | ¥3550 | In-stock | |
100 mg | ¥5200 | In-stock | |
200 mg | ¥7500 | In-stock | |
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Enzalutamide 相关产品
•相关化合物库:
- Drug Repurposing Compound Library Plus
- FDA-Approved Drug Library Plus
- FDA-Approved Drug Library Mini
- Bioactive Compound Library Plus
- FDA-Approved Drug Library
- Anti-Cancer Compound Library
- Autophagy Compound Library
- Drug Repurposing Compound Library
- Orally Active Compound Library
- FDA Approved & Pharmacopeial Drug Library
- Targeted Therapy Drug Library
- Transcription Factor Targeted Library
生物活性 |
Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator[1][2]. |
IC50 & Target |
IC50: 36 nM (androgen-receptor, in LNCaP cells)[1] |
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体外研究 (In Vitro) |
Enzalutamide (MDV3100) has greater affinity to AR than ICI 176334 does in a competition assay with 16β-[18F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide inhibits the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys)[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Enzalutamide (MDV3100) induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
464.44 |
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Formula |
C21H16F4N4O2S |
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CAS 号 |
915087-33-1 |
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中文名称 |
恩杂鲁胺;恩扎鲁胺 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 50 mg/mL (107.66 mM) H2O : ≥ 0.1 mg/mL (0.22 mM) * “≥” means soluble, but saturation unknown. 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [1] |
LNCaP cells (107 cells/condition) are grown in RPMI media supplemented with 5% charcoalstripped serum for 22 days, then treated with DMSO or 1 nM R1881, combined with an antiandrogen (DMSO, 1 μM ICI 176334, 10 μM ICI 176334, 1 μM RD162, 10 μM RD162, 1 μM MDV3100, or 10 μM MDV3100) for 8 hours. An aliquot of cells are harvested for qRT-PCR of PSA and TMPRSS2 mRNA. The remaining cells are cross-linked using 1% paraformaldehyde for 10 minutes, then glycine is added and samples centrifuged (4°C, 4000 rpm, 5 minutes) to stop further crosslinking. Chromatin immunoprecipitation is performed using a chromatin immunoprecipitation assay kit. Immunoprecipitated DNA is amplified by real-time PCR. Primers are PSA enhancer forward-ATGTTCACATTAGTACACCTTGCC and reverse-TCTCAGATCCAGGCTTGCTTACTGTC and TMPRSS2 enhancer forward-TGGTCCTGGATGATAAAAAAAGTTT and reverse-GACATACGCCCCACAACAGA[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [3][4] |
Mice[3] 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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