|S1250||Enzalutamide (MDV3100)||<1 mg/mL||92 mg/mL||<1 mg/mL|
|S1190||Bicalutamide||<1 mg/mL||86 mg/mL||5 mg/mL|
|S1174||MK-2866 (GTx-024)||<1 mg/mL||78 mg/mL||78 mg/mL|
|S2840||Apalutamide (ARN-509)||<1 mg/mL||18 mg/mL||5 mg/mL|
|S1140||Andarine||<1 mg/mL||88 mg/mL||88 mg/mL|
|S5285||RU58841||<1 mg/mL||73 mg/mL||73 mg/mL|
|S5275||RAD140||-1 mg/mL||78 mg/mL||-1 mg/mL|
|S5023||Nadolol||-1 mg/mL||61 mg/mL||-1 mg/mL|
|S4836||Nilutamide||<1 mg/mL||63 mg/mL||63 mg/mL|
|S4794||Drostanolone Propionate||-1 mg/mL||18 mg/mL||-1 mg/mL|
|S4795||Trenbolone acetate||-1 mg/mL||62 mg/mL||-1 mg/mL|
|S4797||Nicergoline||-1 mg/mL||22 mg/mL||-1 mg/mL|
|S3946||Mesterolone||-1 mg/mL||13 mg/mL||-1 mg/mL|
|S3717||Testosterone Enanthate||9 mg/mL||80 mg/mL||80 mg/mL|
|S4757||Dihydrotestosterone(DHT)||<1 mg/mL||58 mg/mL||58 mg/mL|
|S2803||Galeterone||<1 mg/mL||24 mg/mL||40 mg/mL|
|S1908||Flutamide||<1 mg/mL||55 mg/mL||55 mg/mL|
|S2604||Dehydroepiandrosterone (DHEA)||<1 mg/mL||57 mg/mL||57 mg/mL|
|S2042||Cyproterone Acetate||<1 mg/mL||83 mg/mL||10 mg/mL|
|S1304||Megestrol Acetate||<1 mg/mL||33 mg/mL||15 mg/mL|
|S2832||Epiandrosterone||<1 mg/mL||29 mg/mL||58 mg/mL|
|S7040||AZD3514||<1 mg/mL||100 mg/mL||100 mg/mL|
|S4054||Spironolactone||<1 mg/mL||83 mg/mL||20 mg/mL|
|S4593||Chlormadinone acetate||<1 mg/mL||27 mg/mL||1 mg/mL|
|S7559||ODM-201||<1 mg/mL||80 mg/mL||38 mg/mL|
|S7955||EPI-001||<1 mg/mL||79 mg/mL||79 mg/mL|
- Androgen Receptor阻害剤(28)
- 新Androgen Receptor製品
Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.
Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line.
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.
MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.
Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.
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).
Andarine is a selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Phase 3.
Drostanolone Propionate is an anabolic androgenic steroid with strong anti-estrogenic properties.
Trenbolone acetate, a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.
Protodioscin, 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.
Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. It has a selective alpha-1A adrenergic receptor blocking property and also other additional mechanisms of actions.
Mesterolone is a synthetic steroid with anabolic and androgenic activities.
Boldenone is an agonist of the androgen receptor (AR). Boldenone Undecylenate is a derivative of testosterone, which has strong anabolic effect and only moderately androgenic.
Testosterone Enanthate is an androgen and anabolic steroid used in androgen replacement therapy.
Dihydrotestosterone is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.
Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.
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.
Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.
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.
Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.
Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.
(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
Megestrol acetate is a synthetic progestogen, used to treat breast cancer and loss of appetite.
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.
Epiandrosterone is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.
AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.
Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.
(A, B) Indicated HIV-1 latency cells (A. J-LAT 10.6; B. CA5) were treated with levosimendan or spironolactone (5, 10, or 20 μM) in combination with TNFα (10 ng/ml). After 24 hr, mRNA was extracted, and reverse transcribed to cDNA for measurement of HIV-1 initiated or elongated (proximal [Pro], intermediate [Int], and distal [Dis]) transcripts by qPCR. Results were normalized to DMSO control. Values represent the mean ± s.d. (n = 4-6).
Chlormadinone acetate is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours.
Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.
EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.