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Formula | C21H16F4N4O2S |
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Molecular Weight | 464.44 | CAS No. | 915087-33-1 | |
Solubility (25°C)* | In vitro | DMSO | 92 mg/mL (198.08 mM) | |
Water | Insoluble | |||
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy. | ||
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Targets |
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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] |
Kinase Assay:[3] |
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Cell Assay:[1] |
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Animal Study:[1] |
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Data from [Cancer Sci, 2013, 104(8), 1027-32]
Data from [PLoS One, 2013, 8, e53701]
Data from [PLoS One, 2013, 8, e53701]
Data from [Data independently produced by , , Nat Med, 2018, 24(2):239-246]
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 |
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