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化学情報
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Synonyms | MDV3100 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C21H16F4N4O2S |
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| 分子量 | 464.44 | CAS No. | 915087-33-1 | |
| Solubility (25°C)* | 体外 | DMSO | 93 mg/mL (200.24 mM) | |
| Ethanol | 4 mg/mL (8.61 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | エンザルタミド (Enzalutamide (MDV3100)) は、アンドロゲン受容体 (androgen receptor, AR) アンタゴニストで LNCaP 細胞における IC50 は36 nM です。エンザルミドはオートファジー (autophagy) を増加させることが示されています。 |
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| in vitro | Enzalutamide has greater affinity to AR than Bicalutamide 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 could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys). [1] Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. [2] |
| in vivo | Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. [1] |
プロトコル(参考用のみ)
| キナーゼアッセイ | AR reporter assay | |
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| Enzalutamide is evaluated by an artificial AR response reporter system in a hormone refractory prostate cancer cell line. In this system, the prostate cancer LNCaP cells are engineered to stably express about 5-fold higher level of AR than endogenous level. The exogenous AR has similar properties to endogenous AR in that both are stabilized by a synthetic androgen R1881. The AR-over expressed cells are also engineered to stably incorporate an AR response reporter and the reporter activity of these cells shows features of hormone refractory prostate cancer. The antagonistic activity of Enzalutamide is tested in the presence of 100 pM of R1881. Engineered LNCaP cells are maintained in Iscove's medium containing 10% fetal bovine serum (FBS). Two days prior to Enzalutamide treatment, the cells are grown in Iscove's medium containing 10% charcoal-stripped FBS (CS-FBS) to deprive of androgens. The cells are split and grown in Iscove's medium containing 10% CS-FBS with 100 pM of R1881 and increasing concentrations of Enzalutamide. After two days of incubation, reporter activities are assayed. | ||
| 細胞アッセイ | 細胞株 | LNCaP or LNCaP/AR cells |
| 濃度 | 0-10 μM | |
| 反応時間 | 1-4 days | |
| 実験の流れ | Enzalutamide is diluted in DMSO. LNCaP or LNCaP/AR cells (104 cells/well) are androgen-starved by growth in media containing 5-10% charcoal-stripped serum for 3-5 days. Then the cells are challenged with various concentrations of Enzalutamide in media containing 5-10% charcoal-stripped serum. | |
| 動物実験 | 動物モデル | Castration-resistant LNCaP/HR xenografts in male SCID mice |
| 投薬量 | 10 mg/kg | |
| 投与方法 | Administered via gavage daily | |
参考
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カスタマーフィードバック
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Data from [Cancer Sci, 2013, 104(8), 1027-32]
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Data from [PLoS One, 2013, 8, e53701]
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Data from [PLoS One, 2013, 8, e53701]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| Cholinergic signaling via muscarinic M1 receptor confers resistance to docetaxel in prostate cancer [ Cell Rep Med, 2024, 5(2):101388] | PubMed: 38262412 |
| PROX1 drives neuroendocrine plasticity and liver metastases in prostate cancer [ Cancer Lett, 2024, 597:217068] | PubMed: 38901665 |
| Combined inhibition of CDK4/6 and AKT is highly effective against the luminal androgen receptor (LAR) subtype of triple negative breast cancer [ Cancer Lett, 2024, 604:217219] | PubMed: 39244005 |
| Understanding the function of Pax5 in development of docetaxel-resistant neuroendocrine-like prostate cancers [ Cell Death Dis, 2024, 15(8):617] | PubMed: 39183332 |
| RNA-sequencing predicts a role of androgen receptor and aldehyde dehydrogenase 1A1 in osteosarcoma lung metastases [ Oncogene, 2024, 43(14):1007-1018] | PubMed: 38361046 |
| Oxidative stress in peroxisomes induced by androgen receptor inhibition through peroxisome proliferator-activated receptor promotes enzalutamide resistance in prostate cancer [ Free Radic Biol Med, 2024, 221:81-88] | PubMed: 38762061 |
| Upregulation of key factors of viral entry of corona- and influenza viruses upon TLR3-signaling in cells from the respiratory tract and clinical treatment options by 1,8-Cineol [ Phytother Res, 2024, 10.1002/ptr.8280] | PubMed: 39020450 |
| Manzamine A reduces androgen receptor transcription and synthesis by blocking E2F8-DNA interactions and effectively inhibits prostate tumor growth in mice [ Mol Oncol, 2024, 10.1002/1878-0261.13637] | PubMed: 38605607 |
| ST3 beta-galactoside alpha-2,3-sialyltransferase 1 (ST3Gal1) synthesis of Siglec ligands mediates anti-tumour immunity in prostate cancer [ Commun Biol, 2024, 7(1):276] | PubMed: 38448753 |
| Cancer-associated fibroblasts promote enzalutamide resistance and PD-L1 expression in prostate cancer through CCL5-CCR5 paracrine axis [ iScience, 2024, 27(5):109674] | PubMed: 38646169 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。