product name Exemestane
Description: Exemestane (also known as FCE24304, PNU155971) is a synthetic aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively. Exemestane binds irreversibly to and inhibits the enzyme aromatase, thereby blocking the conversion of cholesterol to pregnenolone and the peripheral aromatization of androgenic precursors into estrogens. Structurally similar to androstenedione, exemestane might have a big impact on androgenic effect.
References: J Steroid Biochem Mol Biol. 1994 Jun;49(4-6):289-94; Clin Cancer Res. 2004 Sep 1;10(17):5717-23.
296.4
Formula
C20H24O2
CAS No.
107868-30-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 54 mg/mL (182.2 mM)
Water: <1 mg/mL
Ethanol: 15 mg/mL (50.6 mM)
Solubility (In vivo)
Synonyms
FCE24304, PNU155971
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19393292/
| In Vitro |
In vitro activity: 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. 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. Exemestane causes aromatase degradation in a dose-responsive manner in MCF-7aro cells. Kinase Assay: 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. Cell Assay: 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. |
|---|---|
| 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. 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. |
| Animal model | Estrogen-deficient ovariectomized (OVX) rats |
| Formulation & Dosage | Dissolved in saline; 100 mg/kg; Intramuscular injection |
| References | J Steroid Biochem Mol Biol. 1994 Jun;49(4-6):289-94; Clin Cancer Res. 2004 Sep 1;10(17):5717-23. |
Related Posts
product name Exemestane
Description: Exemestane (also known as FCE24304, PNU155971) is a synthetic aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively. Exemestane binds irreversibly to and inhibits the enzyme aromatase, thereby blocking the conversion of cholesterol to pregnenolone and the peripheral aromatization of androgenic precursors into estrogens. Structurally similar to androstenedione, exemestane might have a big impact on androgenic effect.
References: J Steroid Biochem Mol Biol. 1994 Jun;49(4-6):289-94; Clin Cancer Res. 2004 Sep 1;10(17):5717-23.
296.4
Formula
C20H24O2
CAS No.
107868-30-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 54 mg/mL (182.2 mM)
Water: <1 mg/mL
Ethanol: 15 mg/mL (50.6 mM)
Solubility (In vivo)
Synonyms
FCE24304, PNU155971
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19393292/
| In Vitro |
In vitro activity: 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. 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. Exemestane causes aromatase degradation in a dose-responsive manner in MCF-7aro cells. Kinase Assay: 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. Cell Assay: 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. |
|---|---|
| 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. 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. |
| Animal model | Estrogen-deficient ovariectomized (OVX) rats |
| Formulation & Dosage | Dissolved in saline; 100 mg/kg; Intramuscular injection |
| References | J Steroid Biochem Mol Biol. 1994 Jun;49(4-6):289-94; Clin Cancer Res. 2004 Sep 1;10(17):5717-23. |