Aromatase
信号通路图
研究领域
抑制剂选择性比较
Aromatase产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1235 |
Letrozole (CGS 20267)Letrozole (CGS 20267) 是第三代aromatase抑制剂，无细胞试验中IC50为0.07-20 nM。在临床研究中，对17α-OH progesterone、TSH、促黄体激素、促卵泡激素或雄烯二酮的血浆浓度没有作用，不影响正常的尿电解质排泄或甲状腺功能。Letrozole 可诱导自噬。 |
Uterus from mice treated with Letrozole. (A) 13 weeks old aP2-Cre/ERαflox/flox mice treated with vehicle have swollen abdomen while littermates treated with Letrozole for 17 days looks normal (B). (C) Uterus from vehicle treated aP2-/ERαflox/flox mice with severe hydrometra. (D) Uterus from Letrozole treated aP2-Cre/ERαflox/flox mice looks normal.
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| S1188 |
Anastrozole (ZD-1033)Anastrozole (ZD-1033) 是第三代非甾体类选择性的aromatase抑制剂。相较于其他aromatase抑制剂，它具有更高的选择性，对内源性内分泌没有影响、对肾上腺类固醇也没有明显作用。 |
Cell viability analysis of BCSCs transduced as in A and treated with Anastrozole or Docetaxel, alone or in combination with BKM120 up to 72 hours. Data are mean ± SD of 3 independent experiments.
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| S1196 |
Exemestane (FCE 24304)Exemestane (FCE24304, PNU155971) 是一种Aromatase抑制剂，抑制人胎盘和大鼠卵巢芳香化酶，IC50分别为30 nM和40 nM。 |
Expression of ER, PR, Bcl-2, HER receptors and CYP19A1 mRNA in MCF-7 and AI-resistant cell lines. (A) Western blot analysis of lysates from MCF-7 cells grown with 10% NCS+10-7 M testosterone (MCF-7) and LetR-1, LetR-3, ExeR-1 and ExeR-3 grown in their standard growth medium with 10-6 M letrozole and 10-7 M exemestane, respectively. β-actin and Hsp70 were used as loading controls. (B) Western blot analysis of lysates from MCF-7, LetR-1 and ExeR-1 cells grown for five days in 10% NCS (C) or 10% NCS + 10-12 M estradiol (E2), 10% NCS + 10-7 M testosterone (T), 10% NCS + 10-7 M testosterone + 10-6 M letrozole (T + L), 10% NCS + 10-7 M testosterone + 10-7 M exemestane (T+E). LetR-1 and ExeR-1 cells were withdrawn from testosterone and their respective AI one week before onset of experiment. β-actin was used as loading control. (C) CYP19A1 mRNA level in MCF-7 cells grown with 10% NCS + 10-7 M testosterone for five days and AI-resistant cell lines grown in their standard medium determined by quantitative RT-PCR |
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| S2208 |
FormestaneFormestane (CGP-32349, NSC 282175)是第二代选择性芳香酶抑制剂，IC50为80 nM。 |
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| S1672 |
AminoglutethimideAminoglutethimide (BA-16038, NSC-330915) 是一种芳香化酶抑制剂，IC50为10 μM。 |
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| S9519 |
Fadrozole (CGS16949A)Fadrozole (CGS16949A)是一种有效的、选择性aromatase抑制剂，IC50为4.5 nM, 对aromatase比对其他细胞色素P450酶更有选择性。 |
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| S5158 |
alpha-NaphthoflavoneAlpha-Naphthoflavone (7,8-benzoflavone), a synthetic flavonoid, is a potent inhibitor of aromatase with an I50 value of 0.5 μM. |
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| S3784 |
Obacunone (AI3-37934)Obacunone (AI3-37934, CCRIS 8657), a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. It significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; also a novel activator of Nrf2. |
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| S7867 |
OleuropeinOleuropein 是一种从橄榄叶中分离出的抗氧化多酚。Oleuropein 具有抗氧化、抗炎和抗动脉粥样硬化的作用，并在体外抑制脂肪细胞的分化。Oleuropein 抑制 PPARγ 活性。Oleuropein 通过直接抑制PPARγ转录活性发挥抗脂肪形成作用。Oleuropein 还可抑制aromatase。Oleuropein 可诱导凋亡。Phase 2。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1235 |
Letrozole (CGS 20267)Letrozole (CGS 20267) 是第三代aromatase抑制剂，无细胞试验中IC50为0.07-20 nM。在临床研究中，对17α-OH progesterone、TSH、促黄体激素、促卵泡激素或雄烯二酮的血浆浓度没有作用，不影响正常的尿电解质排泄或甲状腺功能。Letrozole 可诱导自噬。 |
Uterus from mice treated with Letrozole. (A) 13 weeks old aP2-Cre/ERαflox/flox mice treated with vehicle have swollen abdomen while littermates treated with Letrozole for 17 days looks normal (B). (C) Uterus from vehicle treated aP2-/ERαflox/flox mice with severe hydrometra. (D) Uterus from Letrozole treated aP2-Cre/ERαflox/flox mice looks normal.
|
|
| S1188 |
Anastrozole (ZD-1033)Anastrozole (ZD-1033) 是第三代非甾体类选择性的aromatase抑制剂。相较于其他aromatase抑制剂，它具有更高的选择性，对内源性内分泌没有影响、对肾上腺类固醇也没有明显作用。 |
Cell viability analysis of BCSCs transduced as in A and treated with Anastrozole or Docetaxel, alone or in combination with BKM120 up to 72 hours. Data are mean ± SD of 3 independent experiments.
|
|
| S1196 |
Exemestane (FCE 24304)Exemestane (FCE24304, PNU155971) 是一种Aromatase抑制剂，抑制人胎盘和大鼠卵巢芳香化酶，IC50分别为30 nM和40 nM。 |
Expression of ER, PR, Bcl-2, HER receptors and CYP19A1 mRNA in MCF-7 and AI-resistant cell lines. (A) Western blot analysis of lysates from MCF-7 cells grown with 10% NCS+10-7 M testosterone (MCF-7) and LetR-1, LetR-3, ExeR-1 and ExeR-3 grown in their standard growth medium with 10-6 M letrozole and 10-7 M exemestane, respectively. β-actin and Hsp70 were used as loading controls. (B) Western blot analysis of lysates from MCF-7, LetR-1 and ExeR-1 cells grown for five days in 10% NCS (C) or 10% NCS + 10-12 M estradiol (E2), 10% NCS + 10-7 M testosterone (T), 10% NCS + 10-7 M testosterone + 10-6 M letrozole (T + L), 10% NCS + 10-7 M testosterone + 10-7 M exemestane (T+E). LetR-1 and ExeR-1 cells were withdrawn from testosterone and their respective AI one week before onset of experiment. β-actin was used as loading control. (C) CYP19A1 mRNA level in MCF-7 cells grown with 10% NCS + 10-7 M testosterone for five days and AI-resistant cell lines grown in their standard medium determined by quantitative RT-PCR |
|
| S2208 |
FormestaneFormestane (CGP-32349, NSC 282175)是第二代选择性芳香酶抑制剂，IC50为80 nM。 |
||
| S1672 |
AminoglutethimideAminoglutethimide (BA-16038, NSC-330915) 是一种芳香化酶抑制剂，IC50为10 μM。 |
||
| S9519 |
Fadrozole (CGS16949A)Fadrozole (CGS16949A)是一种有效的、选择性aromatase抑制剂，IC50为4.5 nM, 对aromatase比对其他细胞色素P450酶更有选择性。 |
||
| S5158 |
alpha-NaphthoflavoneAlpha-Naphthoflavone (7,8-benzoflavone), a synthetic flavonoid, is a potent inhibitor of aromatase with an I50 value of 0.5 μM. |
||
| S3784 |
Obacunone (AI3-37934)Obacunone (AI3-37934, CCRIS 8657), a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. It significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; also a novel activator of Nrf2. |
||
| S7867 |
OleuropeinOleuropein 是一种从橄榄叶中分离出的抗氧化多酚。Oleuropein 具有抗氧化、抗炎和抗动脉粥样硬化的作用，并在体外抑制脂肪细胞的分化。Oleuropein 抑制 PPARγ 活性。Oleuropein 通过直接抑制PPARγ转录活性发挥抗脂肪形成作用。Oleuropein 还可抑制aromatase。Oleuropein 可诱导凋亡。Phase 2。 |
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