来曲唑|T1590|TargetMol

Letrozole
112809-51-5

询价 1下架起订

上海更新日期：2024-09-23

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

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邮箱：marketing@targetmol.com

产品详情:

中文名称：: 来曲唑

英文名称：: Letrozole

CAS号：: 112809-51-5

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

纯度规格：: 99.84%

产品类别：: 抑制剂

货号：: T1590

Product Introduction

Bioactivity

名称	Letrozole
描述	Letrozole (CGS 20267) 是一种可口服的，选择性可逆的非甾体类芳香化酶抑制剂，IC50值为 11.5 nM。它选择性抑制雌激素的生物合成，可研究乳腺癌。
细胞实验	Cells are seeded in duplicate at 5,000 to 10,000 cells per well in 24-well plates. The day after plating, different concentrations of Letrozole are added. At the end of incubation, cells are trypsinizated and placed in Isotone solution and counted immediately using a Coulter particle-counter. (Only for Reference)
激酶实验	Human placental aromatase activity: The assay is performed in a total volume of 1 mL at 37 ℃. Unless otherwise noted, the incubation mixture contains 11 nM [4- 14C] androstene-3, 17-dione ([4- 14C]A), 24 mM NADPH (tetrasodium salt Type III), the appropriate concentrations of the desired inhibitor, and 120 μg of microsomal protein. The (4- 14C)A is added as a solution in 1.7% ethanol in 0.05 M potassium phosphate buffer (pH 7.4), so that the final concentration of ethanol does not exceed 0.02% (v/v). The reaction is started by the addition of enzyme and stopped after 20 min by the addition of 7 vol of ethyl acetate. The mixture is agitated on a vortex mixer and centrifuged at 600 g for 5 min. The aqueous phase is re-extracted with 7 vol of ethyl acetate, and the combined extracts are evaporated to dryness using an Evapo-Mix. Over 99% of the radio- active of [4- 14C] added is recovered using this extraction system. The residue obtained is dissolved in 150 μL acetone, and 100 μL aliquots are chromatographed for 65 min on thin-layer plates precoated with silica gel 60 using ethyl: acetate: isooctane (140:60, v/v; system A) or toluene: chloroform: methanol (70:140:20; system B). The radioactive zones of the plate are located with a Berthold LB 2760 thin-layer scanner. The radioactive estradiol (E2) and estrone (E1) neaks are identified by comparison with authentic standards. The corresponding bonding band of silica gel is transferred to vials containing 10 mL of scintillation fluid, and counted with a 6880 Liquid Scintillation system.
体外活性	Letrozole对植入无胸腺裸鼠的人芳香化酶基因（MCF-7Ca）转染的MCF-7细胞的肿瘤生长产生剂量依赖性抑制,在20 mg/kg/天时完全抑制.Letrozole在体内实验中,能抑制芳香酶活性,口服ED50 是1-3 μg/mg.
体内活性	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,不明显影响孕酮的产生。Letrozole在LH在促肾上腺皮质激素诱导的大鼠肾组织中,抑制醛甾酮的产生,IC50 是210 μM. Letrozole在非细胞系统中,IC50是1-13 nM。Letrozole能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、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。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year
溶解度	DMSO : 50 mg/mL (175.25 mM)
关键字	CGS-20267 \| CGS20267 \| Aromatase \| Letrozole \| cancer \| inhibit \| breast \| Inhibitor \| estrogen \| Autophagy
相关产品	Org30958 \| Endoxifen \| (-)-Vorozole \| Anastrozole \| alpha-Naphthoflavone \| Minamestane \| Fadrozole \| Obacunone \| Calceolarioside B \| Finrozole
相关库	Approved Drug Library \| Anti-Breast Cancer Compound Library \| Anti-Cancer Drug Library \| Anti-Ovarian Cancer Compound Library \| Anti-Cancer Clinical Compound Library \| Inhibitor Library \| Pediatric Drug Library \| Anti-Cancer Active Compound Library \| Anti-Cancer Approved Drug Library \| Target-Focused Phenotypic Screening Library

CGS 20267|||来曲唑|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子