Bicalutamide

製品コードS1190 バッチS119005

化学情報

	Synonyms	ICI-176334	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₈H₁₄F₄N₂O₄S
	分子量	430.37	CAS No.	90357-06-5
Solubility (25°C)*	体外	DMSO	87 mg/mL (202.15 mM)
		Ethanol	7 mg/mL (16.26 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
in vitro	Bicalutamide undergoes an antagonist-to-agonist switch, stimulating AR activity. Bicalutamide treatment of LNCaP/AR(cs) cells in absence of the synthetic androgen R1881 results in altered gene expression consistent with its well-documented agonist activity in context of AR overexpression. Bicalutamide induces cell proliferation in a dose-dependent manner, and only partially antagonized the effects of R1881. Bicalutamide treatment also results in a significant amount of nuclear AR, although less than that observed with R1881. Bicalutamide exhibits partial agonist activity as evidenced by induction of DNA binding at AR target genes and incomplete antagonism of the effects of R1881. In absence of R1881, Bicalutamide partially activates VP16-AR–mediated transcription, indicative of AR binding to DNA. In LNCaP/AR-luc cells with a stably integrates AR-driven luciferase reporter construct. In the presence of R1881, Bicalutamide shows only weak partial antagonism of VP16-AR–mediated transcription with an IC50 of 0.35 μM. ^[1] Micromolar bicalutamide causes a significant dose-dependent reduction in clonogenicity. ^[2] Dual inhibition of the AR and mTOR signaling pathways provides further benefit with the ridaforolimus-bicalutamide combination producing syner -gistic antiproliferative effects in prostate cancer cells in vitro when compared with each agent alone. ^[3]
in vivo	Single bicalutamide reduces tumor growth by 79%, at defined submaximal doses. The ridaforolimus-bicalutamide combination exhibits improved and potent antitumor activity, almost completely abrogating tumor growth. The combination is also well tolerated, as evidenced by no significant changes in body weight over the course of treatment. Plasma PSA levels are again tightly linked to tumor growth in the combination-treated mice. ^[3]

プロトコル(参考用のみ)

キナーゼアッセイ	Whole-cell competitive binding assays
キナーゼアッセイ	Whole-cell competitive binding assays are performed in LNCaP/AR(codon-switch) (LNCaP/AR(cs)) (harbors a mixture of exogenous wild-type AR and endogenous mutant AR (T877A)) and cells propagated in Iscove's or RPMI media supplemented with 10% fetal bovine serum, or during the assay with 10% charcoal-stripped, dextran-treated fetal bovine serum (CSS). Cells are pre-incubated with ¹⁸F-FDHT, increasing concentrations (1pM to 1μM) of cold Bicalutamide are added, and the assay is performed to measure specific uptake of ¹⁸F-FDHT (4). IC50 values are determined using a one site binding model with least squares curve fitting and R² > 0.99.
細胞アッセイ	細胞株	C4-2 cell
	濃度	0-1 μM
	反応時間	72 hours
	実験の流れ	Exponentially growing C4-2 cells are plated into two 96-well plates and incubated overnight at 37 ˚C. Twenty-four hours later one plate is aspirated and stored at -80 ˚C and the other treated with 10-fold serial concentrations of ridaforolimus (1000 nM to 0.0001 nM) or vehicle (ethanol). Following 72 hours culture at 37 ˚C, the plates are assessed simultaneously for cell growth using the Cy qUANT Cell Proliferation Assay kit. Bicalutamide and Ridaforolimus combination proliferation assays are performed similarly except cell growth is determined as the change in cell number between vehicle control and compound treated cells after 72 hours in culture.
動物実験	動物モデル	Male nude mice bearing C4-2 cells
	投薬量	10 mg/kg
	投与方法	Administered via p.o.

参考

カスタマーフィードバック

: Data from [Oncogene, 2014, 10.1038/onc.2014.302]

: Data from [Cancer Sci, 2013, 104(8), 1027-32]

: , , World J Urol, 2017, 35(8):1213-1221

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

GL-V9 inhibits the activation of AR-AKT-HK2 signaling networks and induces prostate cancer cell apoptosis through mitochondria-mediated mechanism [ iScience, 2024, 27(3):109246]	PubMed: 38439974
Gαi2 Protein Inhibition Blocks Chemotherapy- and Anti-Androgen-Induced Prostate Cancer Cell Migration [ Cancers (Basel), 2024, 16(2)296]	PubMed: 38254786
Therapeutic Potential of Bipolar Androgen Therapy for Castration-Resistant Prostate Cancer: In Vitro and In Vivo Studies [ Biomedicines, 2024, 12(1)181]	PubMed: 38255286
AR antagonists develop drug resistance through TOMM20 autophagic degradation-promoted transformation to neuroendocrine prostate cancer [ J Exp Clin Cancer Res, 2023, 42(1):204]	PubMed: 37563661
Ferroptosis heterogeneity in triple-negative breast cancer reveals an innovative immunotherapy combination strategy [ Cell Metab, 2022, S1550-4131-2200411-9]	PubMed: 36257316
Docetaxel remodels prostate cancer immune microenvironment and enhances checkpoint inhibitor-based immunotherapy [ Theranostics, 2022, 12(11):4965-4979]	PubMed: 35836810
The ERα-NRF2 signalling axis promotes bicalutamide resistance in prostate cancer [ Cell Commun Signal, 2022, 20(1):178]	PubMed: 36376959
CYP1B1-catalyzed 4-OHE2 promotes the castration resistance of prostate cancer stem cells by estrogen receptor α-mediated IL6 activation [ Cell Commun Signal, 2022, 20(1):31]	PubMed: 35292057
α-Terthienyl induces prostate cancer cell death through inhibiting androgen receptor expression [ Biomed Pharmacother, 2022, 152:113266]	PubMed: 35691152
TLK1-mediated MK5-S354 phosphorylation drives prostate cancer cell motility and may signify distinct pathologies [ Mol Oncol, 2022, 16(13):2537-2557]	PubMed: 35064619

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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