Androgen Receptor

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研究领域

抑制剂选择性比较

Androgen Receptor产品

所有产品(48) Androgen Receptor抑制剂(11) Androgen Receptor拮抗剂(19) Androgen Receptor激动剂(12) Androgen Receptor调节剂(6)

目录号	产品描述	文献引用	实验数据
S1123	Abiraterone (CB-7598) Abiraterone (CB-7598) 是一种有效CYP17抑制剂，无细胞试验中IC50为2 nM。Abiraterone (CB-7598) 是一种雄性激素 androgen 生物合成抑制剂。	Cancer Cell, 2021, S1535-6108(21)00659-0 Cancers (Basel), 2021, 13(16)3959 Sci Rep, 2021, 11(1):10765	Inhibition study of expressed orendogenous 5α-reductase-3 enzymeintheabsenceandpresence of 100 and150 nM abiraterone at pH7.4 using 1.0 μM testosterone as substrate.
S2246	Abiraterone Acetate (CB7630) Abiraterone Acetate (CB7630)是Abiraterone的醋酸盐形式，是一种甾体类细胞色素CYP17抑制剂，无细胞试验中IC50为72 nM。Abiraterone acetateis 是一种口服的雄性激素 androgen 生物合成抑制剂。	Clin Cancer Res, 2021, clincanres.4391.2020 Neoplasia, 2021, 23(12):1261-1274 J Biol Chem, 2021, 297(2):100969	BCaPT10 and BPH-1 cells were treated with vehicle (NTC, white bars), 10 uM abiraterone (ABI, gray bars), or abiraterone plus steroid hormones (black bars, 100 nM DHT, 10 nM estradiol, and 10 nM progestin). Minimum of 200 cells per condition was used from each of at least 3 independent experiments. Each result is shown as the average 盨EM from at least 3 independent experiments. One-way ANOVA. , P < .05; , P < .01; , P < .005; **, P < .001.
S6965^New	Bavdegalutamide (ARV-110) Bavdegalutamide (ARV-110)是一种口服生物可利用的特异性 androgen receptor (AR) PROTAC 降解剂，可导致AR的泛素化和降解。ARV-110 可完全降解 androgen receptor (AR)，在所有测试的细胞系中的DC50值均 < 1 nM。ARV-110 可用于前列腺癌的研究。
S2840	Apalutamide (ARN-509) Apalutamide (ARN-509)是一种选择性的，竞争性androgen receptor抑制剂，无细胞试验中IC50为16 nM，对前列腺癌的治疗有效。Phase 3。	Prostate, 2022, 82(3):314-322 J Pathol, 2021, 10.1002/path.5652 Nat Commun, 2020, 19;11(1):2508	ONC1-0013B inhibits AR activity in vitro. A. ONC1-0013B structure. B. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 1 day. PSA expression plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). Ki values: 20.0±5.5nM (ONC1-13B), 30.8±7.7nM (MDV3100), 38.4nM (ARN-509). Mean±SEM from 5 replicate experiments (except ARN-509). C. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 5 days. Viable cells plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). IC50 values: 30nM (ONC1-13B), 148nM (MDV3100), 240nM (ARN-509). D. Competitive-binding assay vs AR ligand Fluormone™ (PolarScreen™ Androgen Receptor Competitor Assay). IC50 values: 19nM (DHT), 7.9uM (ONC1-13B), 16.3uM (MDV3100).
S1353	Ketoconazole (R 41400) Ketoconazole (R 41400)能抑制cyclosporine oxidase（环孢素氧化酶）和testosterone 6 beta-hydroxylase（睾丸素6β-羟化酶），IC50分别为0.19 mM和0.22 mM。Ketoconazole 是一种雄性激素 androgen 生物合成抑制剂。	Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4 Nat Commun, 2021, 12(1):652 Pharmacol Res, 2021, 169:105648
S1195	TAK-700 (Orteronel) TAK-700 (Orteronel) 是一种有效的，高度选择性的，人17，20-lyase抑制剂，IC50为38 nM，比作用于其他CYPs(例如11-羟化酶和CYP3A4)选择性高1000倍以上。TAK-700 (Orteronel) 是一种雄性激素 androgen 生物合成抑制剂。Phase 3。	Drug Metab Dispos, 2017, 45(6):635-645 Biochem Biophys Res Commun, 2016, 477(4):1005-10
S1304	Megestrol Acetate Megestrol acetate (BDH1298, SC10363)是一种人工合成的孕酮，抑制HegG2，IC50为260μM。	Hum Cell, 2022, 10.1007/s13577-022-00671-y Hum Cell, 2021, 34(6):1911-1918 Hum Cell, 2021, 10.1007/s13577-021-00639-4	HEC-1A cells were treated with pterostilbene (75 μM), megestrol acetate (75 μM) or the combination for 24 h. Whole cell lysates were collected and measured for the change of cell cycle and apoptosis pathways by Western blot. Results are representative of 3 or more preparations.
S7040	AZD3514 AZD3514是一种口服的有效androgen receptor（雄激素受体）抑制剂，K_i为2.2 μM，且降低AR蛋白表达。Phase 1。
S0097	(S,R,S)-AHPC (MDK7526) (S,R,S)-AHPC (MDK7526, VH032-NH2, VHL ligand 1)是一种 VH032-based VHL ligand，可用于募集 von Hippel-Lindau (VHL)蛋白。(S,R,S)-AHPC 可能对 androgen receptor 的靶向降解有用。(S,R,S)-AHPC 可以通过接头与蛋白质的配体例如BCR-ABL1连接，以形成PROTAC例如GMB-475。GMB-475 可在 Ba/F3 细胞中诱导BCR-ABL1降解，IC50值为1.11 μM。
S6885	Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone) 是一种来自臭椿Ailanthus altissima的天然通过抗肝癌(HCC)成分，可通过降低 cyclins 和 CDKs 的表达、提高 p21 和 p27 的表达来诱导G0/G1期细胞周期阻滞。Ailanthone 可触发DNA损伤，其特征为 ATM/ATR 通路的激活。Ailanthone 可在Huh7细胞中诱导线粒体介导、涉及 PI3K/AKT 信号通路的细胞凋亡。Ailanthone 也是全长 Androgen Receptor (AR-FL)和组成型活性截断AR剪接变体(AR-Vs, AR_1-651)的抑制剂，对应的IC50值分别为69 nM和309 nM。
S9667	Inobrodib (CCS-1477) Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4）是一种有效的和选择性的 p300/CBP bromodomain 的抑制剂。CCS1477 通过抑制 androgen receptor (AR) 的表达和功能以及抑制 c-Myc 起作用。
S1250	Enzalutamide (MDV3100) Enzalutamide (MDV3100)是一种androgen-receptor (AR)拮抗剂，在 LNCaP细胞中IC50为36 nM。研究证明 Enzalutamide 可促进自噬。	Cancer Res, 2022, canres.1807.2021 Proc Natl Acad Sci U S A, 2022, 119(4)e2025710119 Oncogene, 2022, 10.1038/s41388-021-02157-x
S1190	Bicalutamide (ICI-176334) Bicalutamide (ICI-176334) 是一种androgen receptor (AR)拮抗剂，在LNCaP/AR(cs)细胞系中IC50为0.16 μM。Bicalutamide 可诱导自噬。	Cell Commun Signal, 2022, 20(1):31 Sci Adv, 2021, 7(27)eabg2564 Cell Rep, 2021, 36(10):109625	Immunohistochemical staining of Ki67 was performed to determine cell proliferation in the tumors. Each tissue section was counted manually in three different areas to assess the Ki67-positive cell index. Data were then presented as number of Ki67-positive cells per x 400 microscope field. Results are presented as the means s.d. **P < 0.001 by Student 's t-test, compared with control.
S9898^New	Proxalutamide (GT0918) Proxalutamide (GT0918) 是第二代androgen receptor拮抗剂，在 AR 竞争性结合试验中以 32 nM 的 IC50 与 AR 的配体结合域结合。
S9900^New	JNJ-63576253 (TRC-253) JNJ-63576253 (TRC-253)是一种有效且具有选择性的下一代 androgen receptor (AR) 拮抗剂，IC50 为 6.9 nM。JNJ-63576253 在 WT 和 LBD 突变、enzalutamide耐药的前列腺癌模型中显示出强大的抑制作用。
S2803	Galeterone Galeterone (TOK-001)是一种选择性CYP17抑制剂，也是androgen receptor (AR)（雄激素受体）拮抗剂，IC50分别为300 nM和384 nM，也有效抑制人类前列腺肿瘤生长。Phase 2。	ChemMedChem, 2022, e202200043 Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w Steroids, 2020, 153:108534	C. Impact of CYP17A1 inhibitors on genes involved in androgen biosynthesis. H295R cells were treated with control (DMSO) or 1 μM orteronel and galeterone for 72 h and then RNA was isolated and transcribed to cDNA. Results of qRT-PCR validation of HSD3B2, CYP17A1 and AKR1C3 genes relative to the housekeeping gene cyclophilin A. Expression of the genes was analyzed by SYBR Green real-time PCR. Analysis of relative gene expression was determined by the 2−ΔΔCt method. *p < 0.05.
S1908	Flutamide Flutamide (SCH-13521)是一种抗雄激素药物，与雄激素受体有结合活性，K_i为55 nM，主要用于治疗前列腺癌。	Hum Cell, 2022, 10.1007/s13577-022-00671-y Cell Chem Biol, 2021, 28(6):788-801.e5 Hum Cell, 2021, 10.1007/s13577-021-00639-4	Active Stat5a/b increases nuclear levels of antiandrogen-liganded AR in PC-3 cells. PC-3 cells were infected with AdAR, AdPrlR and AdWTStat5a, serum-starved for 12 h, and pretreated with 1 nM DHT, 10 μM Bicalutamide (Bic), 10 μM Flutamide (Flu) or 10 μM MDV3100 (MDV) for 1 h before stimulation with 10 nM Prl for 30 min, where indicated. Immunostaining depicts DAPI, Stat5a/b, AR and merged imaging of Stat5a/b and AR.
S2604	Dehydroepiandrosterone (DHEA) Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone)是一种重要的内源性类固醇激素，作为androgen receptor拮抗剂以及 estrogen receptor 激动剂。	Stem Cell Rev Rep, 2021, 10.1007/s12015-021-10239-2 J Chromatogr B Analyt Technol Biomed Life Sci, 2021, 1186:123002 SSRN, 2021, 10.2139/ssrn.3886996
S2042	Cyproterone Acetate Cyproterone Acetate是雄激素受体拮抗剂，IC50为7.1 nM，也是微弱的孕激素受体激动剂，具有微弱的孕激素和糖皮质激素活性。	Sci Rep, 2021, 11(1):5457 Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332	(C) Effect of AR antagonist cyproterone acetate (0–5 nM) on androgen-induced ADTRP transactivation in HeLa cells. (D) Effect of AR antagonist cyproterone acetate (0–0.5 nM) on androgen-induced ADTRP transactivation in HeLa cells
S4054	Spironolactone Spironolactone是一种强有效的雄激素受体拮抗剂， IC50为77 nM.	Int J Mol Sci, 2021, 22(4)1638 J Biol Chem, 2021, S0021-9258(21)00252-0 J Environ Sci Health B, 2020, 55(2):91-102	(h and i) Triptolide inhibits transcription. After exposure to triptolide (1 μm), spironolactone (10 μm), actinomycin D (2 μm, transcription inhibitor used as a positive control) or DMSO for 6 h, the global RNA synthesis was evaluated by the measurement of 5-EU incorporation. The figure shows representative merged pictures of DAPI and 5-EU signal. The intensity of the signal was evaluated through fluorescence microscopy (h) and quantified with the CellProfiler Software. Triptolide but not spironolactone inhibits global transcription.
S4836	Nilutamide Nilutamide (RU23908)是一种非甾体类抗雄性激素药物，对androgen receptors具有亲和力。用于治疗前列腺癌。
S4593	Chlormadinone acetate Chlormadinone acetate (Gestafortin) 是一种甾族的黄体酮，具有抗雄激素和抗促性腺激素的作用。其半衰期约为34-38小时。
S7559	Darolutamide (ODM-201) Darolutamide (ODM-201, BAY-1841788)是一种新型androgen receptor (AR)拮抗剂，能够阻断AR核转运，其K_i为f 11 nM。Phase 3。	Proc Natl Acad Sci U S A, 2020, 202021450 Mol Cancer Ther, 2020, molcanther.0417.2020 Mol Cancer Ther, 2020, 19;molcanther00152020	Growth suppression effect of different antiandrogens and Chk1 inhibitors on MDA-MB-453 and SUM185PE cells. The effects of a range of concentrations of three antiandrogens (enzalutamide, ENZA; darolutamide, ODM-201; and abiraterone acetate, AA) and two Chk1 inhibitors (GDC-0575 and AZD7762) were assessed by MTT. Histograms represent the respective IC50s (mean of n = 3–4 experiments; error bars show the 95% confidence interval).
S8885	UT-34 UT-34 是一种有效的、选择性的、可口服的第二代 androgen receptor (AR) 泛拮抗剂和降解剂，其对于野生型 AR、T877A AR和W741L AR的IC50值分别为203.46 nM、80.78 nM和94.17 nM。UT-34 是一种恩杂鲁胺抗性的前列腺癌的潜在的下一代治疗剂。
S5285	RU58841 RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
S7955	EPI-001 EPI-001是androgen receptor N-端结构域的拮抗剂，也是一种选择性PPAR-gamma调节剂。	Prostate, 2019, 79(2):206-214
S9045	Triptophenolide Triptophenolide (Hypolide), derived from Tripterygium wilfordii, is a pan-antagonist for wild-type and mutant androgen receptors with the IC50 values of 260 nM for AR-WT, 480 nM for AR-F876L, 388 nM for AR-T877A, and 437 nM for W741C+T877A.
S6896	Clascoterone Clascoterone (Winlevi, Cortexolone 17 alpha-propionate, Cortexolone 17α-propionate, CB-03-01) 是一种局部的和外周选择性的 androgen receptor (AR) 的拮抗剂。
S4728	3,3'-Diindolylmethane 3,3'-Diindolylmethane(DIM) 是indole-3-carbinol的主要消化产物，而indole-3-carbinol是十字花科蔬菜中一种潜在的抗癌物质。3,3'-Diindolylmethane(DIM) 是一种纯粹的 androgen receptor (AR) 的强拮抗剂。	FASEB J, 2021, 35(5):e21502 Cell Death Dis, 2019, 10(2):38
S5437	4,4'-DDE 4,4'-DDE (DDE, p,p'-DDE, p,p'-dichlorodiphenyldichloroethylene), a breakdown product of DDT, is an organochlorine pesticide and may behave as a potent androgen receptor antagonist.
S1140	Andarine Andarine (GTx-007, S-4)是一种选择性的非甾体类androgen receptor (AR)（雄激素受体）激动剂，K_i为4 nM，对合成代谢器官具有组织选择性。Phase 3.	Anal Chem, 2021, 10.1021/acs.analchem.1c01083 Drug Test Anal, 2020, 10.1002/dta.2917 J Am Soc Mass Spectrom, 2020, 31(11):2243-2249
S2832	Epiandrosterone Epiandrosterone (3β-androsterone, EpiA) 是一种类固醇激素，具有微弱的雄激素活性，是DHEA的一种天然代谢产物。
S3830	Protodioscin Protodioscin (Furostanol I), a steroidal saponin compound found in a number of plant species, is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.
S6352	Androsterone Androsterone (5alpha-Androsterone)是源于性激素的类固醇代谢产物，具有较弱的雄激素属性。	Mediators Inflamm, 2019, 2019:7162976
S5508	Dehydroepiandrosterone acetate Dehydroepiandrosterone acetate (DHEA, Androstenolone) is a kind of dehydroepiandrosterone derivatives. DHEA is an endogenous steroid hormone, which is considered to be a natural product/dietary supplement with many proposed benefits to humans.	Br J Cancer, 2020, 10.1038/s41416-020-1007-3 Cancer Lett, 2016, 382(2):195-202
S3946	Mesterolone Mesterolone (Androviron, Mesteranum, Proviron) is a synthetic steroid with anabolic and androgenic activities.
S6407	Tulobuterol hydrochloride Tulobuterol是长效的β2-adrenergic receptor激动剂，具有支气管扩张、消炎和抗病毒活性。
S4794	Drostanolone Propionate Drostanolone Propionate (Dromostanolone propionate, NSC-12198, Drostanolone 17β-propionate) is an anabolic androgenic steroid with strong anti-estrogenic properties.
S4795	Trenbolone acetate Trenbolone acetate (RU-1697, Trenbolone 17β), a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.
S3717	Testosterone Enanthate Testosterone Enanthate (Testosterone heptanoate, NSC-17591)是一种雄激素和合成代谢类固醇，用于治疗雄性素补疗。	Cancers (Basel), 2021, 13(19)4937 Onco Targets Ther, 2020, 8;13:2987-2995
S3715	Boldenone Undecylenate Boldenone是androgen receptor (AR)的激动剂。Boldenone Undecylenate是睾酮的衍生物，具有强效合成作用，但仅具有中等适度的雄激素活性。
S4757	Dihydrotestosterone (DHT) Dihydrotestosterone (DHT, androstanolone, stanolone, 5α-DHT)是一种内源性的雄激素性类固醇和激素，是雄激素受体的激动剂，其亲和力比睾酮高2-3倍，诱导雄激素受体信号的效力比睾酮高3倍。	J Med Chem, 2022, 65(3):2507-2521 Life Sci Alliance, 2022, 5(4)e202101116 J Oncol, 2022, 2022:6085948
S1174	Ostarine (GTx-024) Ostarine (GTx-024, MK-2866) 是一种selective androgen receptor modulator (SARM)（选择性雄激素受体调节剂）， K_i为3.8 nM，作用于合成代谢器官具有组织选择性。Phase 3。	Int J Mol Sci, 2022, 23(8)4404 J Clin Invest, 2021, 131(10)146777 Anal Chem, 2021, 10.1021/acs.analchem.1c01083
S5275	Testolone (RAD140) Testolone (RAD140) is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.	J Clin Invest, 2021, 131(10)146777 Anal Chem, 2021, 10.1021/acs.analchem.1c01083
S0276	GSK-2881078 GSK 2881078 是一种非甾体选择性的 androgen receptor 的调节剂，有潜力应用于治疗恶病质。
S8822	Ligandrol (LGD-4033) Ligandrol (LGD-4033, VK-5211)是一种新型非类固醇的、具有口服选择性的androgen receptor调节剂，对雄激素受体具有高亲和力（Kd约为1 nM）和高选择性。	J Clin Invest, 2021, 131(10)146777 Anal Chem, 2021, 10.1021/acs.analchem.1c01083 Anal Bioanal Chem, 2021, 10.1007/s00216-021-03740-7
S0839	ACP-105 ACP-105 是一种口服有效的 selective androgen receptor modulator (SARM)，对AR野生型和AR突变T877A的pEC50值分别为9.0和9.4。	Drug Test Anal, 2020, 10.1002/dta.2917
S6630	Dimethylcurcumin (ASC-J9) Dimethylcurcumin (ASC-J9, Dimethyl curcumin, GO-Y025)是一种 androgen receptor (AR) 降解促进剂，可通过降解全长和剪接变异体的雄激素受体来抑制去势抵抗性前列腺癌的生长。

目录号	产品描述	文献引用	实验数据
S1123	Abiraterone (CB-7598) Abiraterone (CB-7598) 是一种有效CYP17抑制剂，无细胞试验中IC50为2 nM。Abiraterone (CB-7598) 是一种雄性激素 androgen 生物合成抑制剂。	Cancer Cell,2021, S1535-6108(21)00659-0 Cancers (Basel),2021, 13(16)3959 Sci Rep,2021, 11(1):10765	Inhibition study of expressed orendogenous 5α-reductase-3 enzymeintheabsenceandpresence of 100 and150 nM abiraterone at pH7.4 using 1.0 μM testosterone as substrate.
S2246	Abiraterone Acetate (CB7630) Abiraterone Acetate (CB7630)是Abiraterone的醋酸盐形式，是一种甾体类细胞色素CYP17抑制剂，无细胞试验中IC50为72 nM。Abiraterone acetateis 是一种口服的雄性激素 androgen 生物合成抑制剂。	Clin Cancer Res,2021, clincanres.4391.2020 Neoplasia,2021, 23(12):1261-1274 J Biol Chem,2021, 297(2):100969	BCaPT10 and BPH-1 cells were treated with vehicle (NTC, white bars), 10 uM abiraterone (ABI, gray bars), or abiraterone plus steroid hormones (black bars, 100 nM DHT, 10 nM estradiol, and 10 nM progestin). Minimum of 200 cells per condition was used from each of at least 3 independent experiments. Each result is shown as the average 盨EM from at least 3 independent experiments. One-way ANOVA. , P < .05; , P < .01; , P < .005; **, P < .001.
S6965^New	Bavdegalutamide (ARV-110) Bavdegalutamide (ARV-110)是一种口服生物可利用的特异性 androgen receptor (AR) PROTAC 降解剂，可导致AR的泛素化和降解。ARV-110 可完全降解 androgen receptor (AR)，在所有测试的细胞系中的DC50值均 < 1 nM。ARV-110 可用于前列腺癌的研究。
S2840	Apalutamide (ARN-509) Apalutamide (ARN-509)是一种选择性的，竞争性androgen receptor抑制剂，无细胞试验中IC50为16 nM，对前列腺癌的治疗有效。Phase 3。	Prostate,2022, 82(3):314-322 J Pathol,2021, 10.1002/path.5652 Nat Commun,2020, 19;11(1):2508	ONC1-0013B inhibits AR activity in vitro. A. ONC1-0013B structure. B. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 1 day. PSA expression plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). Ki values: 20.0±5.5nM (ONC1-13B), 30.8±7.7nM (MDV3100), 38.4nM (ARN-509). Mean±SEM from 5 replicate experiments (except ARN-509). C. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 5 days. Viable cells plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). IC50 values: 30nM (ONC1-13B), 148nM (MDV3100), 240nM (ARN-509). D. Competitive-binding assay vs AR ligand Fluormone™ (PolarScreen™ Androgen Receptor Competitor Assay). IC50 values: 19nM (DHT), 7.9uM (ONC1-13B), 16.3uM (MDV3100).
S1353	Ketoconazole (R 41400) Ketoconazole (R 41400)能抑制cyclosporine oxidase（环孢素氧化酶）和testosterone 6 beta-hydroxylase（睾丸素6β-羟化酶），IC50分别为0.19 mM和0.22 mM。Ketoconazole 是一种雄性激素 androgen 生物合成抑制剂。	Nat Biotechnol,2021, 10.1038/s41587-021-00860-4 Nat Commun,2021, 12(1):652 Pharmacol Res,2021, 169:105648
S1195	TAK-700 (Orteronel) TAK-700 (Orteronel) 是一种有效的，高度选择性的，人17，20-lyase抑制剂，IC50为38 nM，比作用于其他CYPs(例如11-羟化酶和CYP3A4)选择性高1000倍以上。TAK-700 (Orteronel) 是一种雄性激素 androgen 生物合成抑制剂。Phase 3。	Drug Metab Dispos,2017, 45(6):635-645 Biochem Biophys Res Commun,2016, 477(4):1005-10
S1304	Megestrol Acetate Megestrol acetate (BDH1298, SC10363)是一种人工合成的孕酮，抑制HegG2，IC50为260μM。	Hum Cell,2022, 10.1007/s13577-022-00671-y Hum Cell,2021, 34(6):1911-1918 Hum Cell,2021, 10.1007/s13577-021-00639-4	HEC-1A cells were treated with pterostilbene (75 μM), megestrol acetate (75 μM) or the combination for 24 h. Whole cell lysates were collected and measured for the change of cell cycle and apoptosis pathways by Western blot. Results are representative of 3 or more preparations.
S7040	AZD3514 AZD3514是一种口服的有效androgen receptor（雄激素受体）抑制剂，K_i为2.2 μM，且降低AR蛋白表达。Phase 1。
S0097	(S,R,S)-AHPC (MDK7526) (S,R,S)-AHPC (MDK7526, VH032-NH2, VHL ligand 1)是一种 VH032-based VHL ligand，可用于募集 von Hippel-Lindau (VHL)蛋白。(S,R,S)-AHPC 可能对 androgen receptor 的靶向降解有用。(S,R,S)-AHPC 可以通过接头与蛋白质的配体例如BCR-ABL1连接，以形成PROTAC例如GMB-475。GMB-475 可在 Ba/F3 细胞中诱导BCR-ABL1降解，IC50值为1.11 μM。
S6885	Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone) 是一种来自臭椿Ailanthus altissima的天然通过抗肝癌(HCC)成分，可通过降低 cyclins 和 CDKs 的表达、提高 p21 和 p27 的表达来诱导G0/G1期细胞周期阻滞。Ailanthone 可触发DNA损伤，其特征为 ATM/ATR 通路的激活。Ailanthone 可在Huh7细胞中诱导线粒体介导、涉及 PI3K/AKT 信号通路的细胞凋亡。Ailanthone 也是全长 Androgen Receptor (AR-FL)和组成型活性截断AR剪接变体(AR-Vs, AR_1-651)的抑制剂，对应的IC50值分别为69 nM和309 nM。
S9667	Inobrodib (CCS-1477) Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4）是一种有效的和选择性的 p300/CBP bromodomain 的抑制剂。CCS1477 通过抑制 androgen receptor (AR) 的表达和功能以及抑制 c-Myc 起作用。

目录号	产品描述	文献引用	实验数据
S1250	Enzalutamide (MDV3100) Enzalutamide (MDV3100)是一种androgen-receptor (AR)拮抗剂，在 LNCaP细胞中IC50为36 nM。研究证明 Enzalutamide 可促进自噬。	Cancer Res, 2022, canres.1807.2021 Proc Natl Acad Sci U S A, 2022, 119(4)e2025710119 Oncogene, 2022, 10.1038/s41388-021-02157-x
S1190	Bicalutamide (ICI-176334) Bicalutamide (ICI-176334) 是一种androgen receptor (AR)拮抗剂，在LNCaP/AR(cs)细胞系中IC50为0.16 μM。Bicalutamide 可诱导自噬。	Cell Commun Signal, 2022, 20(1):31 Sci Adv, 2021, 7(27)eabg2564 Cell Rep, 2021, 36(10):109625	Immunohistochemical staining of Ki67 was performed to determine cell proliferation in the tumors. Each tissue section was counted manually in three different areas to assess the Ki67-positive cell index. Data were then presented as number of Ki67-positive cells per x 400 microscope field. Results are presented as the means s.d. **P < 0.001 by Student 's t-test, compared with control.
S9898^New	Proxalutamide (GT0918) Proxalutamide (GT0918) 是第二代androgen receptor拮抗剂，在 AR 竞争性结合试验中以 32 nM 的 IC50 与 AR 的配体结合域结合。
S9900^New	JNJ-63576253 (TRC-253) JNJ-63576253 (TRC-253)是一种有效且具有选择性的下一代 androgen receptor (AR) 拮抗剂，IC50 为 6.9 nM。JNJ-63576253 在 WT 和 LBD 突变、enzalutamide耐药的前列腺癌模型中显示出强大的抑制作用。
S2803	Galeterone Galeterone (TOK-001)是一种选择性CYP17抑制剂，也是androgen receptor (AR)（雄激素受体）拮抗剂，IC50分别为300 nM和384 nM，也有效抑制人类前列腺肿瘤生长。Phase 2。	ChemMedChem, 2022, e202200043 Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w Steroids, 2020, 153:108534	C. Impact of CYP17A1 inhibitors on genes involved in androgen biosynthesis. H295R cells were treated with control (DMSO) or 1 μM orteronel and galeterone for 72 h and then RNA was isolated and transcribed to cDNA. Results of qRT-PCR validation of HSD3B2, CYP17A1 and AKR1C3 genes relative to the housekeeping gene cyclophilin A. Expression of the genes was analyzed by SYBR Green real-time PCR. Analysis of relative gene expression was determined by the 2−ΔΔCt method. *p < 0.05.
S1908	Flutamide Flutamide (SCH-13521)是一种抗雄激素药物，与雄激素受体有结合活性，K_i为55 nM，主要用于治疗前列腺癌。	Hum Cell, 2022, 10.1007/s13577-022-00671-y Cell Chem Biol, 2021, 28(6):788-801.e5 Hum Cell, 2021, 10.1007/s13577-021-00639-4	Active Stat5a/b increases nuclear levels of antiandrogen-liganded AR in PC-3 cells. PC-3 cells were infected with AdAR, AdPrlR and AdWTStat5a, serum-starved for 12 h, and pretreated with 1 nM DHT, 10 μM Bicalutamide (Bic), 10 μM Flutamide (Flu) or 10 μM MDV3100 (MDV) for 1 h before stimulation with 10 nM Prl for 30 min, where indicated. Immunostaining depicts DAPI, Stat5a/b, AR and merged imaging of Stat5a/b and AR.
S2604	Dehydroepiandrosterone (DHEA) Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone)是一种重要的内源性类固醇激素，作为androgen receptor拮抗剂以及 estrogen receptor 激动剂。	Stem Cell Rev Rep, 2021, 10.1007/s12015-021-10239-2 J Chromatogr B Analyt Technol Biomed Life Sci, 2021, 1186:123002 SSRN, 2021, 10.2139/ssrn.3886996
S2042	Cyproterone Acetate Cyproterone Acetate是雄激素受体拮抗剂，IC50为7.1 nM，也是微弱的孕激素受体激动剂，具有微弱的孕激素和糖皮质激素活性。	Sci Rep, 2021, 11(1):5457 Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332	(C) Effect of AR antagonist cyproterone acetate (0–5 nM) on androgen-induced ADTRP transactivation in HeLa cells. (D) Effect of AR antagonist cyproterone acetate (0–0.5 nM) on androgen-induced ADTRP transactivation in HeLa cells
S4054	Spironolactone Spironolactone是一种强有效的雄激素受体拮抗剂， IC50为77 nM.	Int J Mol Sci, 2021, 22(4)1638 J Biol Chem, 2021, S0021-9258(21)00252-0 J Environ Sci Health B, 2020, 55(2):91-102	(h and i) Triptolide inhibits transcription. After exposure to triptolide (1 μm), spironolactone (10 μm), actinomycin D (2 μm, transcription inhibitor used as a positive control) or DMSO for 6 h, the global RNA synthesis was evaluated by the measurement of 5-EU incorporation. The figure shows representative merged pictures of DAPI and 5-EU signal. The intensity of the signal was evaluated through fluorescence microscopy (h) and quantified with the CellProfiler Software. Triptolide but not spironolactone inhibits global transcription.
S4836	Nilutamide Nilutamide (RU23908)是一种非甾体类抗雄性激素药物，对androgen receptors具有亲和力。用于治疗前列腺癌。
S4593	Chlormadinone acetate Chlormadinone acetate (Gestafortin) 是一种甾族的黄体酮，具有抗雄激素和抗促性腺激素的作用。其半衰期约为34-38小时。
S7559	Darolutamide (ODM-201) Darolutamide (ODM-201, BAY-1841788)是一种新型androgen receptor (AR)拮抗剂，能够阻断AR核转运，其K_i为f 11 nM。Phase 3。	Proc Natl Acad Sci U S A, 2020, 202021450 Mol Cancer Ther, 2020, molcanther.0417.2020 Mol Cancer Ther, 2020, 19;molcanther00152020	Growth suppression effect of different antiandrogens and Chk1 inhibitors on MDA-MB-453 and SUM185PE cells. The effects of a range of concentrations of three antiandrogens (enzalutamide, ENZA; darolutamide, ODM-201; and abiraterone acetate, AA) and two Chk1 inhibitors (GDC-0575 and AZD7762) were assessed by MTT. Histograms represent the respective IC50s (mean of n = 3–4 experiments; error bars show the 95% confidence interval).
S8885	UT-34 UT-34 是一种有效的、选择性的、可口服的第二代 androgen receptor (AR) 泛拮抗剂和降解剂，其对于野生型 AR、T877A AR和W741L AR的IC50值分别为203.46 nM、80.78 nM和94.17 nM。UT-34 是一种恩杂鲁胺抗性的前列腺癌的潜在的下一代治疗剂。
S5285	RU58841 RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
S7955	EPI-001 EPI-001是androgen receptor N-端结构域的拮抗剂，也是一种选择性PPAR-gamma调节剂。	Prostate, 2019, 79(2):206-214
S9045	Triptophenolide Triptophenolide (Hypolide), derived from Tripterygium wilfordii, is a pan-antagonist for wild-type and mutant androgen receptors with the IC50 values of 260 nM for AR-WT, 480 nM for AR-F876L, 388 nM for AR-T877A, and 437 nM for W741C+T877A.
S6896	Clascoterone Clascoterone (Winlevi, Cortexolone 17 alpha-propionate, Cortexolone 17α-propionate, CB-03-01) 是一种局部的和外周选择性的 androgen receptor (AR) 的拮抗剂。
S4728	3,3'-Diindolylmethane 3,3'-Diindolylmethane(DIM) 是indole-3-carbinol的主要消化产物，而indole-3-carbinol是十字花科蔬菜中一种潜在的抗癌物质。3,3'-Diindolylmethane(DIM) 是一种纯粹的 androgen receptor (AR) 的强拮抗剂。	FASEB J, 2021, 35(5):e21502 Cell Death Dis, 2019, 10(2):38
S5437	4,4'-DDE 4,4'-DDE (DDE, p,p'-DDE, p,p'-dichlorodiphenyldichloroethylene), a breakdown product of DDT, is an organochlorine pesticide and may behave as a potent androgen receptor antagonist.

目录号	产品描述	文献引用
S1140	Andarine Andarine (GTx-007, S-4)是一种选择性的非甾体类androgen receptor (AR)（雄激素受体）激动剂，K_i为4 nM，对合成代谢器官具有组织选择性。Phase 3.	Anal Chem, 2021, 10.1021/acs.analchem.1c01083 Drug Test Anal, 2020, 10.1002/dta.2917 J Am Soc Mass Spectrom, 2020, 31(11):2243-2249
S2832	Epiandrosterone Epiandrosterone (3β-androsterone, EpiA) 是一种类固醇激素，具有微弱的雄激素活性，是DHEA的一种天然代谢产物。
S3830	Protodioscin Protodioscin (Furostanol I), a steroidal saponin compound found in a number of plant species, is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.
S6352	Androsterone Androsterone (5alpha-Androsterone)是源于性激素的类固醇代谢产物，具有较弱的雄激素属性。	Mediators Inflamm, 2019, 2019:7162976
S5508	Dehydroepiandrosterone acetate Dehydroepiandrosterone acetate (DHEA, Androstenolone) is a kind of dehydroepiandrosterone derivatives. DHEA is an endogenous steroid hormone, which is considered to be a natural product/dietary supplement with many proposed benefits to humans.	Br J Cancer, 2020, 10.1038/s41416-020-1007-3 Cancer Lett, 2016, 382(2):195-202
S3946	Mesterolone Mesterolone (Androviron, Mesteranum, Proviron) is a synthetic steroid with anabolic and androgenic activities.
S6407	Tulobuterol hydrochloride Tulobuterol是长效的β2-adrenergic receptor激动剂，具有支气管扩张、消炎和抗病毒活性。
S4794	Drostanolone Propionate Drostanolone Propionate (Dromostanolone propionate, NSC-12198, Drostanolone 17β-propionate) is an anabolic androgenic steroid with strong anti-estrogenic properties.
S4795	Trenbolone acetate Trenbolone acetate (RU-1697, Trenbolone 17β), a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.
S3717	Testosterone Enanthate Testosterone Enanthate (Testosterone heptanoate, NSC-17591)是一种雄激素和合成代谢类固醇，用于治疗雄性素补疗。	Cancers (Basel), 2021, 13(19)4937 Onco Targets Ther, 2020, 8;13:2987-2995
S3715	Boldenone Undecylenate Boldenone是androgen receptor (AR)的激动剂。Boldenone Undecylenate是睾酮的衍生物，具有强效合成作用，但仅具有中等适度的雄激素活性。
S4757	Dihydrotestosterone (DHT) Dihydrotestosterone (DHT, androstanolone, stanolone, 5α-DHT)是一种内源性的雄激素性类固醇和激素，是雄激素受体的激动剂，其亲和力比睾酮高2-3倍，诱导雄激素受体信号的效力比睾酮高3倍。	J Med Chem, 2022, 65(3):2507-2521 Life Sci Alliance, 2022, 5(4)e202101116 J Oncol, 2022, 2022:6085948

目录号	产品描述	文献引用
S1174	Ostarine (GTx-024) Ostarine (GTx-024, MK-2866) 是一种selective androgen receptor modulator (SARM)（选择性雄激素受体调节剂）， K_i为3.8 nM，作用于合成代谢器官具有组织选择性。Phase 3。	Int J Mol Sci, 2022, 23(8)4404 J Clin Invest, 2021, 131(10)146777 Anal Chem, 2021, 10.1021/acs.analchem.1c01083
S5275	Testolone (RAD140) Testolone (RAD140) is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.	J Clin Invest, 2021, 131(10)146777 Anal Chem, 2021, 10.1021/acs.analchem.1c01083
S0276	GSK-2881078 GSK 2881078 是一种非甾体选择性的 androgen receptor 的调节剂，有潜力应用于治疗恶病质。
S8822	Ligandrol (LGD-4033) Ligandrol (LGD-4033, VK-5211)是一种新型非类固醇的、具有口服选择性的androgen receptor调节剂，对雄激素受体具有高亲和力（Kd约为1 nM）和高选择性。	J Clin Invest, 2021, 131(10)146777 Anal Chem, 2021, 10.1021/acs.analchem.1c01083 Anal Bioanal Chem, 2021, 10.1007/s00216-021-03740-7
S0839	ACP-105 ACP-105 是一种口服有效的 selective androgen receptor modulator (SARM)，对AR野生型和AR突变T877A的pEC50值分别为9.0和9.4。	Drug Test Anal, 2020, 10.1002/dta.2917
S6630	Dimethylcurcumin (ASC-J9) Dimethylcurcumin (ASC-J9, Dimethyl curcumin, GO-Y025)是一种 androgen receptor (AR) 降解促进剂，可通过降解全长和剪接变异体的雄激素受体来抑制去势抵抗性前列腺癌的生长。

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