Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Enzalutamide [915087-33-1]
Référence T6002-1mL
Conditionnement : 1mL
Marque : TargetMol
Contactez votre distributeur local :
Téléphone : +1 850 650 7790
Enzalutamide
Catalog No. T6002 CAS 915087-33-1
Synonyms: MDV3100
Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP). Enzalutamide activates autophagy, has antitumor activity, and is commonly used in the treatment of desmoplasia-resistant prostate cancer.
All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Enzalutamide, CAS 915087-33-1
| Description | Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP). Enzalutamide activates autophagy, has antitumor activity, and is commonly used in the treatment of desmoplasia-resistant prostate cancer. |
| Targets&IC50 | Androgen receptor:36 nM (LNCaP cells) |
| In vitro | METHODS: Human prostate cancer cells LNCaP, PC3 and human osteosarcoma cells SJSA-1 were treated with Enzalutamide (0.01-100 μM) for 1 h. Cell viability was measured using MTT. RESULTS: Enzalutamide was shown to decrease the viability of all cell lines, with LD50s of 12 μM, 23.4 μM, and 34.7 μM for LNCaP, PC3, and SJSA-1 cell lines, respectively. [1] METHODS: Human prostate cancer cells VCaP were treated with Enzalutamide (10 μM) for 1-3 days, and the expression levels of target proteins were detected by Western Blot. RESULTS: Enzalutamide up-regulated cleaved-PARP expression and induced apoptosis in human prostate cancer cells. [2] |
| In vivo | METHODS: To assay antitumor activity in vivo, Enzalutamide (1-50 mg/kg) was administered by gavage once daily for twenty-eight days to CB17SCID mice bearing human desmoplastic resistance tumor (CRPC) LNCaP-AR-Lux. RESULTS: Enzalutamide induced regression of tumor volume in a CRPC xenograft model and apoptosis in AR overexpanded prostate cancer cells. [3] METHODS: To assess the role of AR in bone metabolism and bone growth after sexual maturation, Enzalutamide (10-100 mg/kg, 1% carboxymethyl cellulose+0.5% Tween 80+5% dimethylsulfoxide) was administered orally to C57BL/6N mice once daily for twenty-one days. RESULTS: Enzalutamide decreased the amount of bone in the axial skeleton, and Enzalutamide significantly reduced the mechanical strength of the axial skeleton. After sexual maturity, Enzalutamide reduced bone mass in the axial skeleton but not in the appendicular skeleton of male mice. [4] |
| Cell Research | For in vitro experiments, LNCaP or LNCaP/AR cells (10^4 cells/well) were androgen-starved by growth in media containing 5-10% charcoal-stripped serum for 3-5 days. Then the cells were challenged with various concentrations of R1881, bicalutamide, RD162 or MDV3100 in media containing 5-10% charcoal-stripped serum [1]. |
| Animal Research | In vivo tumorigenicity experiments were done by subcutaneous injection of 10^6 cells (100 uL in 50% Matrigel and 50% growth media) into the flanks of castrated male SCID mice. Daily gavage treatment (using a formulation of 1% carboxymethyl cellulose, 0.1% Tween-80, 5% DMSO) was initiated when tumor size reached ~100 mm3. Tumor size was measured weekly in three dimensions (l x w x d) with calipers. For in vivo luciferase imaging, d-luciferin substrate (100 μL, 15 mg/mL) was injected intraperitoneally. After 5 minutes, mice were anesthetized using isofluorane and imaged using a cooled charged-coupled device IVIS camera. Data were analyzed using Living Image 2.30 software [1]. |
| Synonyms | MDV3100 |
| Molecular Weight | 464.44 |
| Formula | C21H16F4N4O2S |
| CAS No. | 915087-33-1 |
Storage
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 85 mg/mL (183 mM)
References and Literature
1. Wright TC, et al. Abiraterone In Vitro Is Superior to Enzalutamide in Response to Ionizing Radiation. Front Oncol. 2021 Jul 21;11:700543. 2. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009 May 8;324(5928):787-90. 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. Wu J, et al. Enzalutamide Reduces the Bone Mass in the Axial But Not the Appendicular Skeleton in Male Mice. Endocrinology. 2016 Feb;157(2):969-77.
Citations
1. Sun R, Yan B, Li H, et al.Androgen receptor variants confer castration resistance in prostate cancer by counteracting antiandrogen-induced ferroptosis.Cancer Research.2023 2. Shi F, Wu L, Cui D, et al.LncFALEC recruits ART5/PARP1 and promotes castration-resistant prostate cancer through enhancing PARP1-meditated self PARylation.Cellular Oncology.2023: 1-16. 3. Ren L, Luo H, Zhao J, et al.An integrated in vitro/in silico approach to assess the anti-androgenic potency of isobavachin.Food and Chemical Toxicology.2023: 113764. 4. Zhao J, Sun Y, Ren L, et al.Antagonism of androgen receptor signaling by aloe-emodin.Food and Chemical Toxicology.2023: 114092. 5. Ekiciler A, Chen W L K, Bo Y, et al.Quantitative Cytochrome P450 3A4 Induction Risk Assessment Using Human Hepatocytes Complemented with Pregnane X Receptor-Activating Profiles.Drug Metabolism and Disposition.2023, 51(3): 276-284. 6. Pan W, Zhang Z, Kimball H, et al. Abiraterone acetate induces CREB1 phosphorylation and enhances the function of the CBP-p300 complex, leading to resistance in prostate cancer cells. Clinical Cancer Research. 2021, 27(7): 2087-2099. 7. Ghoochani A, Hsu E C, Aslan M, et al. Ferroptosis inducers are a novel therapeutic approach for advanced prostate cancer. Cancer research. 2021 Mar 15;81(6):1583-1594. doi: 10.1158/0008-5472.CAN-20-3477. Epub 2021 Jan 22. 8. Liu S, Tao Y, Wu S, et al.Sanguinarine chloride induces ferroptosis by regulating ROS/BACH1/HMOX1 signaling pathway in prostate cancer.Chinese Medicine.2024, 19(1): 1-18. 9. Tao Y, Lu J, Li L, et al.Raltitrexed induces apoptosis through activating ROS-mediated ER stress by impeding HSPA8 expression in prostate cancer cells.Biochimica et Biophysica Acta (BBA)-Molecular Cell Research.2024: 119684.