Exemestane

製品コードS1196 バッチS119602

印刷

化学情報

Chemical Structure Synonyms FCE24304, PNU155971,EXE Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H24O2
分子量 296.4 CAS No. 107868-30-4
Solubility (25°C)* 体外 DMSO 54 mg/mL (182.18 mM)
Ethanol 21 mg/mL (70.85 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 Exemestane is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.
in vitro

Exemestane competitively inhibits and time-dependently inactivates of human placental aromatase with Ki of 4.3 nM. Exemestane displaces [3H]DHT from rat prostate androgen receptor with IC50 of 0.9 μM. [1] Exemestane (1 μM) increases alkaline phosphatase activity in hFOB and Saos-2 cells and induces the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and glypican 2 in hFOB cells. [2] Exemestane causes aromatase degradation in a dose-responsive manner in MCF-7aro cells. [3]
in vivo

Exemestane increases lumbar spine BMD by 14.0% in OVX rats at dose of 100 mg/kg. Exemestane (100 mg/kg) and 17-hydroexemestane (20 mg/kg) significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin in rats and causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol inOVX rats. [4] Exemestane (20 mg/kg/day s.c.) induces 26% complete (CR) and 18% partial (PR) tumor regressions in rats with 7,12-dimethylbenzanthracene (DMBA)-induced mammary tumors. [5]
特徴 17-hydroexemestane is the principal metabolite of Exemestane.

プロトコル(参考用のみ)

キナーゼアッセイ Assays with human placental aromatase
Microsomes are prepared from human placenta and stored at -80℃. The rate of aromatization is determined by measuring the tritiated water released from [1β-3H]A. The assay is carried out in a final volume of 1 mL, in 10 mM phosphate buffer, pH 7.5, containing 100 mM KCl, 1 mM EDTA, 1 mM dithiothreitol, 100 μM NADPH, the enzyme preparation and the appropriate concentrations of Exemestane (in duplicate) and the substrate. After a 10 min incubation at 37 ℃, the assay is terminated by the addition of 4 mL cold chloroform. The acqueous phase is treated with a charcoal suspension, the supernatant is removed and counted for radioactivity by liquid scintillation in Rialuma. For the determination of the IC50 values, various concentrations of Exemestane are incubated with 20 μg of microsomal protein, in the presence of a fixed amount (50 nM) of [3H]A.
細胞アッセイ 細胞株 hFOB cells
濃度 1 μM
反応時間 24 hours
実験の流れ

hFOB is treated with steroids and Exemestane for 24 hours, when specimens are harvested and evaluated for cell proliferation using the WST-8 method. Optical densities (OD, 450 nm) are evaluated using a SpectraMax 190 microplate reader and Softmax Pro 4.3 microplate analysis software. The status of proliferation (%) is calculated according to the following equation: (cell OD value after test materials treated /vehicle control cell OD value)× 10
動物実験 動物モデル estrogen-deficient ovariectomized (OVX) rats
投薬量 100 mg/kg
投与方法 Intramuscular injection

カスタマーフィードバック

, , Int J Oncol, 2015, 46(4):1481-90.

Data from [Data independently produced by , , Cell Physiol Biochem, 2017, 42(1):1-12]

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：

SERPINA3-ANKRD11-HDAC3 pathway induced aromatase inhibitor resistance in breast cancer can be reversed by HDAC3 inhibition [ Commun Biol, 2023, 6(1):695] PubMed: 37414914
Predicting clinical response to everolimus in ER+ breast cancers using machine-learning [ Front Mol Biosci, 2022, 9:981962] PubMed: 36304922
Predicting clinical response to everolimus in ER+ breast cancers using machine-learning [ Front Mol Biosci, 2022, 9:981962] PubMed: 36304922
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] PubMed: 35207746
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] PubMed: 35118583
Characterization of the Major Single Nucleotide Polymorphic Variants of Aldo-Keto Reductase 1C3 (Type 5 17β-Hydroxysteroid Dehydrogenase) [ J Steroid Biochem Mol Biol, 2022, S0960-0760(22)00072-3] PubMed: 35489629
Systems Pharmacology-Based Precision Therapy and Drug Combination Discovery for Breast Cancer [ Cancers (Basel), 2021, 13(14)3586] PubMed: 34298802
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4] PubMed: 34731453
Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z] PubMed: 34304386
Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918] PubMed: 34383271

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