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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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10g |
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Other Sizes |
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Purity: ≥98%
Exemestane (formerly also known as FCE24304, PNU155971; FCE 24304; EXE), a drug used in ER-positive breast cancer, is a synthetic and potent aromatase inhibitor, which 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.
ln Vitro |
Exemestane dramatically boosts the number of cells in hFOB, Saos-2 cells (1-1000 nM; 72 h) [2]. Exemestane (72 h) stimulates the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and glypican 2 in hFOB cells and boosts alkaline phosphatase activity in Saos-2 and hFOB cells [2]. With a Ki of 4.3 nM, exemestane competitively inhibits and inactivates human placental aromatase in a time-dependent manner. With an IC50 of 0.9 μM, exemestane substitutes [3H]5α-dihydrotestosterone in the rat prostate androgen receptor [1].
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ln Vivo |
Treatment with exemestane (20–100 mg/kg; intramuscular injection; once weekly; for 16 weeks) resulted in significant increases in trabecular bone volume, fifth lumbar vertebra compressive strength, femoral flexural strength, and lumbar and femoral BMD. Exemestane considerably lowers the elevations in serum osteocalcin and pyridinoline that are brought on by ovariectomy. Serum cholesterol and LDL cholesterol are markedly lowered with exemestane [3]. Rats with mammary tumors produced by 7,12-dimethylbenzanthracene (DMBA) show 26% complete (CR) and 18% partial (PR) tumor regression when exposed to exemestane (20 mg/kg/day) subcutaneously [4].
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Cell Assay |
Cell Viability Assay[2]
Cell Types: hFOB, Saos-2 cells Tested Concentrations: 1 nM, 10 nM, 100 nM, 1000 nM Incubation Duration: 72 hrs (hours) Experimental Results: Induced cell proliferation. |
Animal Protocol |
Animal/Disease Models: Female Sprague Dawley rats (10-month-old) bearing ovariectomy [3]
Doses: 20 mg/kg, 50 mg/kg, or 100 mg/kg Route of Administration: intramuscular (im) injection; once weekly; for 16 weeks Experimental Results: Dramatically increased the lumbar vertebral and femoral BMD, bending strength of the femur, compressive strength of the fifth lumbar vertebra, and trabecular bone volume. |
References |
[1]. Di Salle, E., et al., Novel aromatase and 5 alpha-reductase inhibitors. J Steroid Biochem Mol Biol, 1994. 49(4-6): p. 289-94.
[2]. Miki, Y, et al. Effects of aromatase inhibitors on human osteoblast and osteoblast-like cells: a possible androgenic bone protective effects induced by exemestane. Bone. 2004 Sep 1;10(17):5717-23. [3]. Goss, P.E., et al., Effects of the steroidal aromatase inhibitor exemestane and the nonsteroidal aromatase inhibitor letrozole on bone and lipid metabolism in ovariectomized rats. Clin Cancer Res, 2004. 10(17): p. 5717-23. [4]. Zaccheo, T., D. Giudici, and E. Di Salle, Inhibitory effect of combined treatment with the aromatase inhibitor exemestane and tamoxifen on DMBA-induced mammary tumors in rats. J Steroid Biochem Mol Biol, 1993. 44(4-6): p. 677-80. |
Molecular Formula |
C20H24O2
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Molecular Weight |
296.4
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CAS # |
107868-30-4
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SMILES |
O=C(C=C1C(C[C@@]2([H])[C@]3([H])CC4)=C)C=C[C@]1(C)[C@@]2([H])CC[C@]3(C)C4=O
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InChi Key |
BFYIZQONLCFLEV-DAELLWKTSA-N
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InChi Code |
InChI=1S/C20H24O2/c1-12-10-14-15-4-5-18(22)20(15,3)9-7-16(14)19(2)8-6-13(21)11-17(12)19/h6,8,11,14-16H,1,4-5,7,9-10H2,2-3H3/t14-,15-,16-,19+,20-/m0/s1
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Chemical Name |
(8R,9S,10R,13S,14S)-10,13-dimethyl-6-methylene-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione.
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Synonyms |
FCE24304, PNU155971; PNU155971; PNU-155971; PNU 155971; FCE24304; FCE-24304; FCE 24304; Exemestane; US trade name: Aromasin.
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3738 mL | 16.8691 mL | 33.7382 mL | |
5 mM | 0.6748 mL | 3.3738 mL | 6.7476 mL | |
10 mM | 0.3374 mL | 1.6869 mL | 3.3738 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.