アロマターゼ
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1235 | Letrozole (CGS 20267) | <1 mg/mL | 57 mg/mL | '<1 mg/mL |
| S1188 | Anastrozole (ZD-1033) | <1 mg/mL | 59 mg/mL | '59 mg/mL |
| S1196 | Exemestane (FCE 24304) | <1 mg/mL | 54 mg/mL | '15 mg/mL |
| S2208 | Formestane | <1 mg/mL | 61 mg/mL | <1 mg/mL |
| S1672 | Aminoglutethimide | <1 mg/mL | 20 mg/mL | 7 mg/mL |
| S9519 | Fadrozole (CGS16949A) | <1 mg/mL | 45 mg/mL | ''45 mg/mL |
| S5158 | alpha-Naphthoflavone | -1 mg/mL | 31 mg/mL | -1 mg/mL |
| S3784 | Obacunone (AI3-37934) | -1 mg/mL | 90 mg/mL | -1 mg/mL |
| S7867 | Oleuropein | 100 mg/mL | 100 mg/mL | 100 mg/mL |
Aromatase製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1235 |
Letrozole (CGS 20267)Letrozole (CGS 20267) is a third generation inhibitor of aromatase with IC50 of 0.07-20 nM in cell-free assays.It has no effect on the plasma levels of 17α-OH progesterone, thyroid-stimulating hormone (TSH), luteinizing hormone (LH), follicle-stimulating hormone (FSH), or androstenedione and does not affect normal urine electrolyte excretion or thyroid function in clinical studies. Letrozole induces autophagy. |
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) is a third-generation nonsteroidal selective aromatase inhibitor. It may offer greater selectivity compared with other aromatase inhibitors, being without any intrinsic endocrine effects and with no apparent effect on the synthesis of adrenal steroids. |
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) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively. |
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) is a second generation selective aromatase inhibitor with an IC50 of 80 nM. |
||
| S1672 |
AminoglutethimideAminoglutethimide (BA-16038, NSC-330915) is an aromatase inhibitor with IC50 of 10 μM. |
||
| S9519 |
Fadrozole (CGS16949A)Fadrozole (CGS16949A) is a potent, selective, nonsteroidal inhibitor of aromatase with an IC50 of 4.5 nM and selectivity over other cytochrome P-450 enzymes. |
||
| 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 is an antioxidant polyphenol isolated from olive leaf. Oleuropein exerts antioxidant, anti-inflammatory and anti-atherogenic effects and suppresses the adipocyte differentiation in vitro. Oleuropein inhibits PPARγ activity. Oleuropein exerts anti-adipogenic effect through direct inhibition of PPARγ transcriptional activity. Oleuropein also inhibits aromatase. Oleuropein induces apoptosis. Phase 2. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1235 |
Letrozole (CGS 20267)Letrozole (CGS 20267) is a third generation inhibitor of aromatase with IC50 of 0.07-20 nM in cell-free assays.It has no effect on the plasma levels of 17α-OH progesterone, thyroid-stimulating hormone (TSH), luteinizing hormone (LH), follicle-stimulating hormone (FSH), or androstenedione and does not affect normal urine electrolyte excretion or thyroid function in clinical studies. Letrozole induces autophagy. |
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) is a third-generation nonsteroidal selective aromatase inhibitor. It may offer greater selectivity compared with other aromatase inhibitors, being without any intrinsic endocrine effects and with no apparent effect on the synthesis of adrenal steroids. |
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) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively. |
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) is a second generation selective aromatase inhibitor with an IC50 of 80 nM. |
||
| S1672 |
AminoglutethimideAminoglutethimide (BA-16038, NSC-330915) is an aromatase inhibitor with IC50 of 10 μM. |
||
| S9519 |
Fadrozole (CGS16949A)Fadrozole (CGS16949A) is a potent, selective, nonsteroidal inhibitor of aromatase with an IC50 of 4.5 nM and selectivity over other cytochrome P-450 enzymes. |
||
| 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 is an antioxidant polyphenol isolated from olive leaf. Oleuropein exerts antioxidant, anti-inflammatory and anti-atherogenic effects and suppresses the adipocyte differentiation in vitro. Oleuropein inhibits PPARγ activity. Oleuropein exerts anti-adipogenic effect through direct inhibition of PPARγ transcriptional activity. Oleuropein also inhibits aromatase. Oleuropein induces apoptosis. Phase 2. |
