氨鲁米特 T1103

Product Introduction
Bioactivity


英文名: Aminoglutethimide

描述: Aminoglutethimide (BA-16038) 是一种芳香酶抑制剂，IC50=10 μM，用于治疗晚期 BREAST Y。

细胞实验: The NCI-h295 tumor cell line is maintained in RPMI 1640 medium supplemented with transferrin (0.1 mg/mL), insulin (5 μg/mL), selenium (5.2 μg/mL) and 2% FCS. The cells are incubated for 48 hours with Aminoglutethimide (3, 30, 300 μM). Then cells are examined by trypan blue staining for cell viability, counted with a coulter counter. For the assessment of ACTH-R mRNA, cells are harvested, and total RNA is extracted, electrophoresed, blotted and hybridized with a human ACTH-R cDNA probe.(Only for Reference)

激酶实验: Concentration–response and kinetic studies: The microsomal protein (30 μg), [1β-3H]androstenedione (6.6 × 105 dpm) and NADPH (270 μM) are used for the concentration–response experiment with an incubation time of 20 minutes. The Aminoglutethimide is initially tested at 10 μM and 100 μM concentrations, followed by a full concentration–response study with at least 8 concentrations ranging from 0.01 μM to 160 μM. For the initial velocity study the concentration of [1β-3H]androstenedione is varied from 7.5 to 100 nM and the incubation time is set to 5 minutes. The tritiated water formed during the conversion of the tritiated substrate, [1β-3H]androstenedione, to estrone is quantified by liquid scintillation counting. Each assay is performed three times in duplicate and the results are treated by nonlinear regression analysis allowing the determination of the half-maximal inhibitory concentration (IC50).

体内活性: Aminoglutethimide在1至2周的服用后，将其自身的代谢速率从基础值的2.6±0.3 (S.E.) liters/24小时提高到5.3±1.4 liters/24小时，并显著加快人工合成的糖皮质激素dexamethasone的代谢速率，从基础值的145±26.6 liters/24小时提升至568±127 liters/24小时（p < 0.02）。[3] Aminoglutethimide（150 mg/kg）能够在成年雌性小鼠的卵巢和未成熟雄性小鼠的睾丸中，抑制由人绒毛膜促性腺激素(hCG)诱导的鸟氨酸脱羧酶(ODC)的表达，并几乎耗尽了由hCG引起的生殖腺和血浆中的孕酮或睾酮，这与对cAMP依赖性蛋白激酶的抑制（IC50 287 μM）有关，而非阻断类固醇生成途径。[4]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 7 mg/mL (30.13 mM)
DMSO : 16 mg/mL (68.9 mM)


关键字: Aminoglutethimide | NSC330915 | BA16038 | inhibit | BA 16038 | NSC 330915 | Aromatase | Inhibitor

相关产品: Org30958 | Endoxifen | Exemestane | Vorozole | alpha-Naphthoflavone | 3-(3,4-Dimethoxyphenyl)propanoic acid | Fadrozole | Letrozole | Oleuropein | Fadrozole hydrochloride

相关库: Approved Drug Library | Anti-Breast Cancer Compound Library | Anti-Cancer Drug Library | CNS-Penetrant Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Chemotherapy Drug Library | Target-Focused Phenotypic Screening Library | High Solubility Fragment Library

氨鲁米特 T1103信息由TargetMol中国为您提供，如您想了解更多关于氨鲁米特 T1103报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途