Enzalutamide D3 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells[1].
分子量
467.45
Formula
C21H13D3F4N4O2S
CAS 号
1443331-82-5
中文名称
恩杂鲁胺 d3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009 May 8;324(5928):787-90.
Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist[1].
体外研究 (In Vitro)
Enzalutamide is converted into its major metabolites, N-desmethyl enzalutamide and carboxylic acid enzalutamide, by cytochrome P450 (CYP) 3A4/5 and CYP2C8, respectively. N-desmethyl enzalutamide has clinically relevant anti-androgen capacities similar to enzalutamide, whereas carboxylic acid enzalutamide is inactive[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.
分子量
451.39
Formula
C20H13F4N3O3S
CAS 号
1242137-15-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. van Nuland M, et al. Exposure-Response Assessment of Enzalutamide and Its Major Metabolites in a Real-World Cohort of Patients with Metastatic Castration-Resistant Prostate Cancer. Pharmacotherapy. 2019 Dec;39(12):1137-1145.
N-desmethyl Enzalutamide D6 (N-desmethyl MDV 3100 D6) is a deuterium labeled N-desmethyl Enzalutamide. N-desmethyl Enzalutamide is an active metabolite of Enzalutamide. N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide[1].
IC50 & Target
Androgen-receptor[1]
分子量
456.45
Formula
C20H8D6F4N4O2S
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Gibbons JA, et al. Pharmacokinetic Drug Interaction Studies with Enzalutamide. Clin Pharmacokinet. 2015 Oct;54(10):1057-69.
N-desmethyl Enzalutamide D6 (N-desmethyl MDV 3100 D6) is a deuterium labeled N-desmethyl Enzalutamide. N-desmethyl Enzalutamide is an active metabolite of Enzalutamide. N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide[1].
IC50 & Target
Androgen-receptor[1]
分子量
456.45
Formula
C20H8D6F4N4O2S
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Gibbons JA, et al. Pharmacokinetic Drug Interaction Studies with Enzalutamide. Clin Pharmacokinet. 2015 Oct;54(10):1057-69.
N-desmethyl Enzalutamide D6 (N-desmethyl MDV 3100 D6) is a deuterium labeled N-desmethyl Enzalutamide. N-desmethyl Enzalutamide is an active metabolite of Enzalutamide. N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide[1].
IC50 & Target
Androgen-receptor[1]
分子量
456.45
Formula
C20H8D6F4N4O2S
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Gibbons JA, et al. Pharmacokinetic Drug Interaction Studies with Enzalutamide. Clin Pharmacokinet. 2015 Oct;54(10):1057-69.
Enzalutamide D3 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells[1].
分子量
470.47
Formula
C21H10D6F4N4O2S
CAS 号
1443331-94-9
中文名称
恩杂鲁胺 d6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009 May 8;324(5928):787-90.
Enzalutamide D3 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells[1].
分子量
470.47
Formula
C21H10D6F4N4O2S
CAS 号
1443331-94-9
中文名称
恩杂鲁胺 d6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009 May 8;324(5928):787-90.
Enzalutamide D3 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells[1].
分子量
470.47
Formula
C21H10D6F4N4O2S
CAS 号
1443331-94-9
中文名称
恩杂鲁胺 d6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009 May 8;324(5928):787-90.
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]
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]. Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex[2].
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.
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]. Enzalutamide shows dose-independent pharmacokinetics at intravenous and oral doses of 0.5-5 mg/kg[4].
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.
Clinical Trial
分子量
464.44
Formula
C21H16F4N4O2S
CAS 号
915087-33-1
中文名称
恩杂鲁胺;恩扎鲁胺
运输条件
Room temperature in continental US; may vary elsewhere.
Solubility: 2.5 mg/mL (5.38 mM); Suspended solution; Need ultrasonic
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
[1]. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science, 2009, 324 (5928), 787-790.
[2]. Scher HI, et al. Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study. Lancet, 2010, 375(9724), 1437-1446.
[3]. Guerrero J, et al. Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration-resistant prostate cancer. Prostate. 2013 Sep;73(12):1291-305.
[4]. Kim TH, et al. Pharmacokinetics of enzalutamide, an anti-prostate cancer drug, in rats. Arch Pharm Res. 2015 Nov;38(11):2076-82.
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.
Animal Administration [3][4]
Mice[3] Following a 5-day acclimation period, 5- to 9-week-old male CB17SCID mice are castrated and allowed to recover for an additional 5 days before inoculation with tumor cells. LNCaP cells co-expressing exogenous AR and the AR-dependent reporter construct ARR2-Pb-Luc (LNCaP-AR-Lux cells) are used to generate a xenograft model of human prostate cancer. Before implantation, LNCaP-AR-Lux cells are prepared by the addition of trypsin-EDTA, washed with complete medium, collected and resuspended at 20×106 cells/mL. Cell suspensions are diluted with Matrigel to 2×106 cells/0.2 mL and delivered subcutaneously in the suprascapular region. Tumor growth is monitored to the volume of 100 mm3 when treatment begins (80 days). The observed rate of tumor take with LNCaP-AR-Lux cells is between 70% and 80%. Body weight and tumor volumes (width2×length/2) are measured two to three times per week with a digital caliper, and the average tumor volumes are determined. Test drugs are diluted in Tween 80:PEG 400, and stored at 4°C until administration by oral gavage. Each group of mice (n=7) is treated daily for 28 consecutive days with 1, 10, or 50 mg/kg Enzalutamide, vehicle control, or 50 mg/kg ICI 176334. At the end of the treatment period or when tumor volume exceeded 1,000 mm3, animals are euthanized and blood and tissue samples are collected for analysis. Rats[4] Male SD rats (n=3) are administered Enzalutamide through the tail vein (intravenous) and by oral gavage at 1 mg/kg and are kept in metabolic cages after dosing. Urine and feces samples are collected over the following time intervals after dosing: 0-2, 2-4, 4-6, 6-10, 10-24, 24-48, and 48-72 h. The metabolic cages are rinsed with distilled water, and residues are added to the urine samples at 72 h. To extract the Enzalutamide present in the feces, samples are shaken vigorously for 12 h with 50 % methanol.
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
[1]. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science, 2009, 324 (5928), 787-790.
[2]. Scher HI, et al. Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study. Lancet, 2010, 375(9724), 1437-1446.
[3]. Guerrero J, et al. Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration-resistant prostate cancer. Prostate. 2013 Sep;73(12):1291-305.
[4]. Kim TH, et al. Pharmacokinetics of enzalutamide, an anti-prostate cancer drug, in rats. Arch Pharm Res. 2015 Nov;38(11):2076-82.
Enzalutamide carboxylic acid-d6 Chemical Structure
规格
价格
是否有货
数量
5 mg
¥9350
In-stock
10 mg
询价
50 mg
询价
* Please select Quantity before adding items.
生物活性
Enzalutamide carboxylic acid D6 is the deuterium labeled Enzalutamide carboxylic acid (MDV3100 carboxylic acid). Enzalutamide carboxylic acid is an inactive metabolite of Enzalutamide[1].
分子量
457.43
Formula
C20H7D6F4N3O3S
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
参考文献
[1]. van Nuland M, et al. Exposure-Response Assessment of Enzalutamide and Its Major Metabolites in a Real-World Cohort of Patients with Metastatic Castration-Resistant Prostate Cancer. Pharmacotherapy. 2019 Dec;39(12):1137-1145.
N-desmethyl Enzalutamide is the active metabolite of Enzalutamide.N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide[1].
IC50 & Target
Androgen-receptor[1]
体内研究 (In Vivo)
N-desmethyl Enzalutamide is an active metabolite that is thought to contribute to the clinical effects of Enzalutamide because it demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as Enzalutamide. The carboxylic acid metabolite is pharmacologically inactive and circulates at approximately 25 % lower plasma concentrations than Enzalutamide[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.
分子量
450.41
Formula
C20H14F4N4O2S
CAS 号
1242137-16-1
运输条件
Room temperature in continental US; may vary elsewhere.