Letrozole

目录号:S1235 别名: CGS 20267

Letrozole Chemical Structure

Molecular Weight(MW): 285.3

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。

规格 价格 库存 购买数量  
In DMSO RMB 3930.28 现货
RMB 814.34 现货
RMB 1383.01 现货
RMB 3866.75 现货
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客户使用Selleck该产品发表文献14篇:

客户使用该产品的5个实验数据:

  • 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.

    PLoS One 2014 9(1), e85581. Letrozole purchased from Selleck.

  • Effect of aromatase inhibitor letrozole on cellular proliferation marker Ki-67 expression in LNCaP tumor xenografts. A, Ki-67 immunostaining in transverse sections of xenograft tumors from C, C+T, C+T+D, C+T+L, and C+T+D+L mice 2 days after testosterone replacement. Panel B, Quantification of Ki-67–positive cells in LNCaP tumors at day 2 post testosterone replacement. Error bars represent SEM. Number of animals in each group is shown in parentheses. ***, P <.0001.

    Endocrinology 2013 154, 2296-307. Letrozole purchased from Selleck.

  • Clin Sci (Lond), 2018, 132(7):759-776. Letrozole purchased from Selleck.

  • Letrozole impairs object recognition and object placement memory consolidation. (A) Mice receiving bilateral dorsal hippocampal infusion of vehicle (n = 13), but not 0.005 μg (n = 9), 0.025 μg (n = 10), or 0.05 μg (n = 12) letrozole, immediately after training spent significantly more time with the novel object 24 h after training relative to chance (dashed line at 15 s). Vehicle-infused mice also spent significantly more time with the novel object than mice infused with 0.025 or 0.05 μg letrozole. These data suggest that the 0.025 and 0.05 μg doses of letrozole blocked object recognition memory consolidation. (B) Mice receiving bilateral dorsal hippocampal infusions of vehicle (n = 12) or 0.005 μg (n = 9) letrozole, but not 0.025 μg (n = 9) or 0.05 μg (n = 9) letrozole, immediately after training spent significantly more time than chance (*p < 0.05) with the moved object 4 h after training. Vehicle-infused mice also spent significantly more time with the moved object than mice infused with 0.025 or 0.05 μg letrozole, suggesting that the 0.025 and 0.05 μg doses of letrozole also blocked spatial memory consolidation. This effect was limited to within the first 2–3 h after training, as mice receiving a bilateral infusion of vehicle (n = 11) or 0.025 μg letrozole (n = 10) 3 h after OR training (C), or 2 h after OP training (vehicle: n = 13; letrozole: n = 9) (D), spent significantly more time than chance with the novel object (*p < 0.05), suggesting that the memory-impairing effects of letrozole are specific to the consolidation period immediately after training. *p < 0.05, **p < 0.01, ***p < 0.001 relative to chance; #p < 0.05 for between-group differences measured by Tukey's post hoc tests.

    Horm Behav, 2016, 83:60-7. Letrozole purchased from Selleck.

  • Functional comparison of mono-cultured MCF7 cells and MCF7 cells co-cultured with CAFs before and after letrozole treatment. Cell invasion (a), migration (b), adhesion (c) and proliferation assays (d) revealed that MCF7 cells co-cultured with CAFs displayed increasing adhesion, invasion, migration and proliferation abilities compared with mono-cultured cells either with or without letrozole treatment. The invasion, migration and adhesion of co-cultured MCF7 cells were decreased after letrozole treatment (a–c). Letrozole had no effect on mono-cultured MCF7 cell migration, invasion, adhesion or proliferation (a–d). e–g Representative images of invasion, migration and adhesion assays (magnification: ×100). LET represents letrozole. MO and CO represents mono-cultured and co-cultured, respectively. Data are presented as the mean ± SD. *P < 0.05 and ***P < 0.001, as determined using the independent sample T test

    Med Oncol, 2016, 33(7):64. Letrozole purchased from Selleck.

产品安全说明书

Aromatase抑制剂选择性比较

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。
靶点
Aromatase [1]
(Cell-free assay)
0.07 nM-20 nM
体外研究

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MCF7a cells NEHMU5dEgXSxdH;4bYNqfHliYYPzZZk> MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4[SClZXzsd{BmgHC{ZYPzbY5oKFSndD3v[oYuO2KndHHIV2QyNUG{b32gZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDUV3Que3SrbYXsZZRm\CClZXzsJJBzd2yrZnXyZZRqd25ibXXhd5Vz\WRiYX\0[ZIhOTBiZHH5d{whTUN3ME20[U0xPiEQvF2= M2TnNFIzQTVzMEe0
human JEG3 cells MYTGeY5kfGmxbjDhd5NigQ>? MX\Jcohq[mm2aX;uJI9nKGG{b33heIF{\SCjY4Tpeol1gSCrbjDoeY1idiCMRVezJINmdGy|LDDJR|UxRTBwMECwPFkh|ryP NH\HNVAyQDV7MEK3Ni=>
human MCF7 cells MonFR5l1d3SxeHnjbZR6KGG|c3H5 MUi3NkBp MWHDfZRwfG:6aXPpeJkh[WejaX7zeEBme3S{b3flck1l\XCnbnTlcpQhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFA4KM7:TR?= NVPQSXFROjR|NEW0PFE>
human MDA-MB-435 cells M1zncWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2HoWlQ5KGh? NXfTNYhLT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVQ{PSClZXzsd{Bi\nSncjC0PEBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiR1m1NF0xNjB4NzFOwG0> NIjxelQzODl3MEi5PC=>
human IGROV1 cells NIjUcW1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M13OZ|Q5KGh? MmnGS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTWdTV1ZzIHPlcIx{KGGodHXyJFQ5KGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDHTVUxRTBwMEm1JO69VQ>? M2XLbFIxQTVyOEm4
human MDA-MB-231 cells MkfKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHi5PIs1QCCq M{XUd2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEeLNUC9NE4yPSEQvF2= M4XWSFIxQTVyOEm4
human T47D cells MleyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{nDclQ5KGh? MYXHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDUOFdFKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCJSUWwQVAvPDRizszN M2j1WFIxQTVyOEm4
human MCF7 cells NVvhRmI6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3zZcVQ5KGh? M3vyU2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgOFghcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFfJOVA:OC55IN88US=> MlXLNlA6PTB6OUi=
human OVCAR4 cells MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUm0PEBp MX3Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDPWmNCWjRiY3XscJMh[W[2ZYKgOFghcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFfJOVA:OC56ODFOwG0> M1vKT|IxQTVyOEm4
human BT549 cells NF73NWZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn\3OFghcA>? M2LzRmdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGJVPTR7IHPlcIx{KGGodHXyJFQ5KGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDHTVUxRTBwOEmg{txO NYG2cIVYOjB7NUC4PVg>
human SKOV3 cells M2nWTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUHiNYxWPDhiaB?= NWfwelJ3T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hW0uRVkOgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGdKPTB;MT6wPUDPxE1? NVT0VlJFOjB7NUC4PVg>
human NCI/ADR-RES cells MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXy3RpFSPDhiaB?= MY\Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDOR2kwSUSULWLFV{Bk\WyuczDh[pRmeiB2ODDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhT0l3ME2xMlE3KM7:TR?= MljmNlA6PTB6OUi=
human MDA-N cells NWrWboxVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVfmfGdSPDhiaB?= NULJbXVmT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV6gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGdKPTB;MT62NUDPxE1? MV6yNFk2ODh7OB?=
human OVCAR5 cells NEfyfnRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NILuWFk1QCCq MVTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDPWmNCWjViY3XscJMh[W[2ZYKgOFghcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFfJOVA:OS54MjFOwG0> MYCyNFk2ODh7OB?=
human OVCAR8 cells NHHFVVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3Xoc|Q5KGh? NEPydHFIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBQXkODUkigZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGdKPTB;ND61JO69VQ>? MXqyNFk2ODh7OB?=

... Click to View More Cell Line Experimental Data

体内研究 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 (DMBA)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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[6]

- 合并

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:

[3]

- 合并
  • Cell lines: 人类乳腺癌细胞 MCF-7
  • Concentrations: ~100 nM
  • Incubation Time: 1天
  • Method:

    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。


    (Only for Reference)
动物实验:

[5]

- 合并
  • 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
  • Formulation: 0.5% (w/v)羧甲基纤维素溶液
  • Dosages: 20毫克/千克/天
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 57 mg/mL (199.78 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
0.5% CMC Na
10mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 285.3
化学式

C17H11N5

CAS号 112809-51-5
储存条件 粉状
溶于溶剂
别名 CGS 20267

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03870919 Not yet recruiting Drug: Palbociclib|Other: locoregional treatment Breast Cancer Stage IV|Radiotherapy|Surgery UNICANCER|Pfizer October 15 2019 Not Applicable
NCT03900884 Not yet recruiting Drug: Venetoclax|Drug: Palbociclib|Drug: Letrozole Breast Neoplasm Female Peter MacCallum Cancer Centre Australia September 2019 Phase 1
NCT04095364 Recruiting Drug: Carboplatin|Drug: Letrozole|Drug: Paclitaxel Low Grade Ovarian Serous Adenocarcinoma|Primary Peritoneal Low Grade Serous Adenocarcinoma|Stage II Ovarian Cancer AJCC v8|Stage IIA Ovarian Cancer AJCC v8|Stage IIB Ovarian Cancer AJCC v8|Stage III Ovarian Cancer AJCC v8|Stage IIIA Ovarian Cancer AJCC v8|Stage IIIA1 Ovarian Cancer AJCC v8|Stage IIIA2 Ovarian Cancer AJCC v8|Stage IIIB Ovarian Cancer AJCC v8|Stage IIIC Ovarian Cancer AJCC v8|Stage IV Ovarian Cancer AJCC v8|Stage IVA Ovarian Cancer AJCC v8|Stage IVB Ovarian Cancer AJCC v8|TP53 Negative NRG Oncology|National Cancer Institute (NCI) August 26 2019 Phase 3
NCT04002141 Not yet recruiting Drug: Placebo oral tablet|Drug: Letrozole Endometriosis|Ovarian Hyperstimulation University of California San Francisco June 28 2019 Phase 2

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Aromatase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID