Exemestane (FCE 24304) 是一种选择性，不可逆和具有口服活性的甾体芳香酶 (aromatase) 抑制剂，对人胎盘和大鼠卵巢芳香酶的IC50分别为 30 nM 和 40 nM。Exemestane 可用于激素依赖性乳腺癌研究。
| 生物活性 | Exemestane (FCE 24304) is a selective, irreversible and orally active steroidalaromataseinhibitor withIC50s of 30 nM and 40 nM forhuman placental andrat ovarianaromatase, respectively. Exemestane can be used for hormone-dependent breastcancerresearch[1][2]. |
| IC50& Target | IC50: 30 nM (Human placenta aromatase) and 40 nM (Rat ovarian aromatase)[1] |
体外研究
(In Vitro) | Exemestane (EXE; 1-1000 nM; 72 hours; hFOB, Saos-2 cells<) treatment significantly increases the number of the cells[2].
Exemestane (0.1- μM; 72 hours) 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 competitively inhibits and time-dependently inactivates of human placental aromatase with Kiof 4.3 nM. Exemestane displaces [3H]5α-dihydrotestosterone from rat prostate androgen receptor with IC50of 0.9 μM[1].
Cell Viability Assay[2] | Cell Line: | hFOB, Saos-2 cells | | Concentration: | 1 nM, 10 nM, 100 nM, 1000 nM | | Incubation Time: | 72 hours | | Result: | Induced cell proliferation. |
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体内研究
(In Vivo) | Exemestane (EXE; 20-100 mg/kg; intramuscular injection; once weekly; for 16 weeks) treatment significantly increases the lumbar vertebral and femoral BMD, bending strength of the femur, compressive strength of the fifth lumbar vertebra, and trabecular bone volume. Exemestane significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin. Exemestane causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol[3].
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[4].
| Animal Model: | Female Sprague Dawley rats (10-month-old) bearing ovariectomy[3] | | Dosage: | 20 mg/kg, 50 mg/kg, or 100 mg/kg | | Administration: | Intramuscular injection; once weekly; for 16 weeks | | Result: | Significantly increased the lumbar vertebral and femoral BMD, bending strength of the femur, compressive strength of the fifth lumbar vertebra, and trabecular bone volume. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 54 mg/mL(182.19 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (8.43 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.43 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (8.43 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.43 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.43 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.43 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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