Letrozole
别名: CGS 20267 中文名称：来曲唑
Letrozole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。
Letrozole Chemical Structure
CAS: 112809-51-5
产品质控
批次：
纯度：
99.99%
99.99
Letrozole相关产品
| 相关产品 | Fadrozole (CGS16949A) Obacunone (AI3-37934) | 点击展开 |
|---|---|---|
| 相关化合物库 | FDA药物库 天然产物库 已知活性药物库-I 外泌体分泌相关化合物库 人类激素相关化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| H295R | Function assay | 5 uM | 24 hrs | Inhibition of CYP19 in human H295R cells using [1beta-3H(N)]-androst-4-ene-3,17-dione at 5 uM after 24 hrs by tritiated water release assay | 24025069 |
| MDA-MB-231 | Growth inhibition assay | 72 hrs | Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by cell counting based method, GI50=10μM | 30822713 | |
| MCF7 | Growth inhibition assay | 72 hrs | Growth inhibition of human MCF7 cells incubated for 72 hrs by cell counting based method, GI50=4.1μM | 30822713 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=4.73μM | 29202405 | |
| T47D | Function assay | 24 hrs | Inhibition of aromatase activity in human T47D cells after 24 hrs, IC50=29.5μM | 27770735 | |
| T47D | Function assay | 24 hrs | Inhibition of aromatase activity in human T47D cells after 24 hrs, IC50=29.5μM | 28427017 | |
| insect cells | Function assay | 30 mins | Inhibition of recombinant human CYP19 expressed in baculovirus infected insect cells using MFC as substrate measured after 30 mins by fluorometric analysis, IC50=0.0053μM | 27647367 | |
| MCF7 | Cytotoxicity assay | 24 to 96 hrs | Cytotoxicity against human MCF7 cells after 24 to 96 hrs, IC50=0.02μM | 24345481 | |
| MCF-7aro | Function assay | 1 hr | Inhibition of aromatase in human MCF-7aro cells using [1beta-3H] androstenedione as substrate incubated for 1 hr by liquid scintillation counting method, IC50=0.0019μM | 31732252 | |
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against estrogen-dependent human MCF7 cells after 72 hrs by MTT assay, IC50=0.007μM | 24345481 | |
| MCF7a | Cytotoxicity assay | 10 days | Cytotoxicity against human MCF7a cells expressing Tet-off-3betaHSD1-Arom assessed as inhibition of TST-stimulated cell proliferation measured after 10 days, EC50=0.000004μM | 22951074 | |
| OVCAR3 | Growth inhibition assay | 48 hrs | Growth inhibition of human OVCAR3 cells after 48 hrs by sulforhodamine B assay, GI50=5.87μM | 20950898 | |
| OVCAR8 | Growth inhibition assay | 48 hrs | Growth inhibition of human OVCAR8 cells after 48 hrs by sulforhodamine B assay, GI50=4.5μM | 20950898 | |
| Hs 578T | Growth inhibition assay | 48 hrs | Growth inhibition of human Hs 578T cells after 48 hrs by sulforhodamine B assay, GI50=2.17μM | 20950898 | |
| OVCAR5 | Growth inhibition assay | 48 hrs | Growth inhibition of human OVCAR5 cells after 48 hrs by sulforhodamine B assay, GI50=1.62μM | 20950898 | |
| MDA-N | Growth inhibition assay | 48 hrs | Growth inhibition of human MDA-N cells after 48 hrs by sulforhodamine B assay, GI50=1.61μM | 20950898 | |
| NCI/ADR-RES | Growth inhibition assay | 48 hrs | Growth inhibition of human NCI/ADR-RES cells after 48 hrs by sulforhodamine B assay, GI50=1.16μM | 20950898 | |
| SKOV3 | Growth inhibition assay | 48 hrs | Growth inhibition of human SKOV3 cells after 48 hrs by sulforhodamine B assay, GI50=1.09μM | 20950898 | |
| BT549 | Growth inhibition assay | 48 hrs | Growth inhibition of human BT549 cells after 48 hrs by sulforhodamine B assay, GI50=0.89μM | 20950898 | |
| OVCAR4 | Growth inhibition assay | 48 hrs | Growth inhibition of human OVCAR4 cells after 48 hrs by sulforhodamine B assay, GI50=0.88μM | 20950898 | |
| MCF7 | Growth inhibition assay | 48 hrs | Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B assay, GI50=0.7μM | 20950898 | |
| T47D | Growth inhibition assay | 48 hrs | Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay, GI50=0.44μM | 20950898 | |
| MDA-MB-231 | Growth inhibition assay | 48 hrs | Growth inhibition of human MDA-MB-231cells after 48 hrs by sulforhodamine B assay, GI50=0.15μM | 20950898 | |
| IGROV1 | Growth inhibition assay | 48 hrs | Growth inhibition of human IGROV1 cells after 48 hrs by sulforhodamine B assay, GI50=0.095μM | 20950898 | |
| MDA-MB-435 | Growth inhibition assay | 48 hrs | Growth inhibition of human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay, GI50=0.067μM | 20950898 | |
| insect cells | Function assay | 30 mins | Inhibition of human recombinant aromatase expressed in baculovirus infected insect cells using O-benzylfluorescein benzyl ester as substrate after 30 mins, IC50=0.0011μM | ChEMBL | |
| insect cells | Function assay | Inhibition of recombinant human aromatase expressed in baculovirus infected insect cells using O-benzyl fluorescein benzyl ester as substrate in presence of NADPH generating system by fluorescence based analysis, IC50=0.0019μM | 31416738 | ||
| JEG-3 | Function assay | Inhibition of aromatase (unknown origin) expressed in JEG-3 cells, IC50=0.00089μM | 25992880 | ||
| V79MZh | Function assay | Inhibition of human CYP11B1 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxy-corticosterone as substrate, IC50=2.62μM | 23281812 | ||
| V79MZh | Function assay | Inhibition of human CYP11B2 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxy-corticosterone as substrate, IC50=1.42μM | 23281812 | ||
| JEG3 | Function assay | Inhibition of aromatase activity in human JEG3 cells, IC50=0.00089μM | 18590272 | ||
| JEG3 | Function assay | Inhibition of aromatase in human JEG3 cells by scintillation spectrometry, IC50=0.00089μM | 20148564 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Letrozole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。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Letrozole有效抑制不同来源的芳香酶，包括人胎盘微粒体，人乳腺癌颗粒部分，大鼠卵巢微粒体，转染芳香酶的MCF-7细胞(MCF-7Ca)，JEG-3绒膜癌细胞，CHO细胞，仓鼠卵巢组织，人乳腺癌颗粒部分，IC50分别是11, 2, 7, 0.07, 0.07, 1.4, 20和 0.8 nM。在非细胞系统中，letrozole 的IC50是1-13 nM。[1]Letrozole在LH诱导的仓鼠卵巢组织中抑制雌二醇产生，IC50 是0.02 μM，达到350 μM浓度时，不显著影响孕酮的产生。在ACTH诱导的大鼠肾组织中，抑制醛甾酮的产生，IC50 是210 μM. [2] Letrozole以剂量依赖的方式抑制MCF-7乳腺癌细胞的生长，IC50是1 nM。在低浓度下(0.1 nM)抑制作用依然可以观测到。letrozole 处理MCF-12A不影响生长，即使letrozole 浓度达到 (100 nM)或者延长培养时间。Letrozole (10 nM) 显著抑制4-雄甾烯-3,17-二酮(100 nM) 或者睾酮 (100 nM) 对MCF-7在细胞增殖方面的激活作用。联合使用17-β-雌二醇和letrozole (10 nM)降低由雌二醇诱导的MMP-2和MMP-9的活化作用。[3] |
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| 激酶实验 | 人类胎盘芳香酶活性 | |||
| 反应在37℃条件下，总体积为1 mL的体系中进行。孵育的混合物包含11 nM [4- 14C] 雄甾烯-3, 17-二酮([4- 14C]A)，24 mM NADPH (焦磷酸钠盐III型)，适当浓度的化合物，120 μg微粒体蛋白。(4- 14C)A用含有1.7% 溶解，溶于的0.05 M 磷酸钾缓冲液 (pH 7.4)溶解，乙醇终浓度不超过0.02%。加入酶触发反应，20分钟后加入7倍体积乙酸乙酯终止反应。混合物震荡，600g离心5分钟。用7倍体积的乙酸乙酯重新提起，混合两次所得样品，Evapo-Mix蒸干。用这种方法，99%的[4- 14C]的放射性能够保留。获得的残渣溶于150ul丙酮，取100ul做65分钟的薄层层析，用体积比为140:60的乙酸乙酯：异辛烷或者体积比为70:140:20（系统B）。用Berthold LB 2760定位放射性区域。放射性标记的雌二醇和孕酮通过与标准品比对来确认。硅胶结合的条带转移到10ml闪烁缓冲液中，用6880液体闪烁法系统计数。 | ||||
| 细胞实验 | 细胞系 | 人类乳腺癌细胞 MCF-7 | ||
| 浓度 | ~100 nM | |||
| 孵育时间 | 1天 | |||
| 方法 | 细胞以5,000 到10,000个每孔的密度接种于24孔板上，第二天，加入不同浓度的Letrozole。孵育末期，细胞用胰酶消化，用Coulter particle计数器计数。 |
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| 体内研究(In Vivo) | ||
| 体内研究活性 | 在体内实验中， Letrozole抑制芳香酶活性，口服ED50 是1-3 微克/毫克。[2] Letrozole具有抗内分泌效果。在未成年大鼠体内，Letrozole抑制雄烯二酮引起的子宫肥大，ED50 为1-3 微克/千克。在成年雌性大鼠体内，Letrozole (0.3-1 毫克/千克 每天 口服，14 天)完全打断卵巢周期，并降低子宫重量和血清雌二醇(E2)浓度，使其与切除卵巢后的水平相同。[1] Letrozole诱导剂量依赖的雌激素依赖的抑制9,10-二甲苯-a-蒽诱导的雌性大鼠的肿瘤。Letrozole 的ED50是10-30 微克/千克/天，完全抑制的剂量是10微克/天。[4] |
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|---|---|---|
| 动物实验 | Animal Models | 含有人类芳香化酶基因(MCF-7Ca)的人类乳腺癌异种移植MCF-7 |
| Dosages | 20毫克/千克/天 | |
| Administration | 口服 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06143631 | Not yet recruiting | Leiomyoma Uterine|Leiomyoma|Fibroid|Fibroid Uterus |
University of California San Francisco|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) |
May 13 2024 | Phase 4 |
| NCT05872204 | Recruiting | Low Grade Serous Ovarian Carcinoma|Adult Type Granulosa Cell Tumor |
Universitaire Ziekenhuizen KU Leuven|Kom Op Tegen Kanker|Eli Lilly and Company|European Network of Gynaecological Oncological Trial Groups (ENGOT) |
November 30 2023 | Phase 2 |
化学信息&溶解度
| 分子量 | 285.3 | 分子式 | C17H11N5 |
| CAS号 | 112809-51-5 | SDF | Download Letrozole SDF |
| Smiles | C1=CC(=CC=C1C#N)C(C2=CC=C(C=C2)C#N)N3C=NC=N3 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 57 mg/mL ( (199.78 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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