Letrozole (Synonyms: 来曲唑; CGS 20267)

目录号: HY-14248 纯度: 99.95%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Letrozole (CGS 20267) 是一种有效的，选择性的，可逆的和具有口服活性的非甾体类芳香化酶 (aromatase) 抑制剂，IC₅₀ 值为 11.5 nM。Letrozole 选择性抑制雌激素的生物合成，可用于乳腺癌的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Letrozole Chemical Structure

CAS No. : 112809-51-5

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥715	In-stock
25 mg	￥650	In-stock
50 mg	￥900	In-stock
100 mg	￥1600	In-stock
200 mg	￥2800	In-stock
500 mg	￥4100	In-stock
1 g		询价
5 g		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Letrozole:

Letrozole-d₄ In-stock
Letrozole (Standard) 询价

MCE 顾客使用本产品发表的 16 篇科研文献

: Letrozole purchased from MCE. Usage Cited in: Exp Ther Med. 2018 Jun;15(6):5269-5274. [Abstract]; Letrozole significantly increases the protein levels of Ras/ERK1/c-Myc in the classical MAPK pathway.

: Letrozole purchased from MCE. Usage Cited in: Exp Ther Med. 2018 Jun;15(6):5269-5274. [Abstract]; Detection of the effects of Letrozole and the MAPK pathway on the proliferation of GC-1 spg cells by BrdU. MAPK, mitogen-activated protein kinase; spg, spermatogonia; BrdU, bromodeoxyuridine.

Letrozole 相关产品

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查看 Cytochrome P450 亚型特异性产品:

查看所有亚型

CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

生物活性
纯度 & 产品资料
参考文献

生物活性

Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC₅₀ of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer^[1]^[2]^[3].

IC₅₀ & Target

Aromatase

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BT-549	GI₅₀	0.89 μM Compound: Letrozole	Growth inhibition of human BT549 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human BT549 cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
HeLa	GI₅₀	> 100 μM Compound: Letrozole	Growth inhibition of non-estrogen-sensitive human HeLa cells after 72 hrs by MTT assay Growth inhibition of non-estrogen-sensitive human HeLa cells after 72 hrs by MTT assay	[PMID: 24025069]
Hs-578T	GI₅₀	2.17 μM Compound: Letrozole	Growth inhibition of human Hs 578T cells after 48 hrs by sulforhodamine B assay Growth inhibition of human Hs 578T cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
HT-29	GI₅₀	> 100 μM Compound: Letrozole	Growth inhibition of non-estrogen-sensitive human HT-29 cells after 72 hrs by MTT assay Growth inhibition of non-estrogen-sensitive human HT-29 cells after 72 hrs by MTT assay	[PMID: 24025069]
IGROV-1	GI₅₀	> 100 μM Compound: Letrozole	Growth inhibition of estrogen-sensitive human IGROV1 cells after 72 hrs by MTT assay Growth inhibition of estrogen-sensitive human IGROV1 cells after 72 hrs by MTT assay	[PMID: 24025069]
IGROV-1	GI₅₀	0.095 μM Compound: Letrozole	Growth inhibition of human IGROV1 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human IGROV1 cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
JEG-3	IC₅₀	0.89 nM Compound: letrozole	Inhibition of aromatase in human JEG3 cells by scintillation spectrometry Inhibition of aromatase in human JEG3 cells by scintillation spectrometry	[PMID: 20148564]
Jurkat	GI₅₀	> 100 μM Compound: Letrozole	Growth inhibition of non-estrogen-sensitive human Jurkat cells after 72 hrs by MTT assay Growth inhibition of non-estrogen-sensitive human Jurkat cells after 72 hrs by MTT assay	[PMID: 24025069]
MCF-10A	IC₅₀	> 10 μM Compound: Letrozole	Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability after 72 hrs by cell counter method Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability after 72 hrs by cell counter method	[PMID: 34364162]
MCF7	GI₅₀	> 100 μM Compound: Letrozole	Growth inhibition of estrogen-sensitive human MCF7 cells after 72 hrs by MTT assay Growth inhibition of estrogen-sensitive human MCF7 cells after 72 hrs by MTT assay	[PMID: 24025069]
MCF7	GI₅₀	0.7 μM Compound: Letrozole	Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
MCF7	IC₅₀	20 nM Compound: Letrozole	Cytotoxicity against human MCF7 cells after 24 to 96 hrs Cytotoxicity against human MCF7 cells after 24 to 96 hrs	[PMID: 24345481]
MCF7	IC₅₀	4.1 μM Compound: Letrozole	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by cell counter method Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by cell counter method	[PMID: 34364162]
MCF7	GI₅₀	4.1 μM Compound: LTZ	Growth inhibition of human MCF7 cells incubated for 72 hrs by cell counting based method Growth inhibition of human MCF7 cells incubated for 72 hrs by cell counting based method	[PMID: 30822713]
MCF7	IC₅₀	4.73 μM Compound: Letrozole	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 29202405]
MCF7	IC₅₀	7 nM Compound: Letrozole	Cytotoxicity against estrogen-dependent human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against estrogen-dependent human MCF7 cells after 72 hrs by MTT assay	[PMID: 24345481]
MDA-MB-231	GI₅₀	0.15 μM Compound: Letrozole	Growth inhibition of human MDA-MB-231cells after 48 hrs by sulforhodamine B assay Growth inhibition of human MDA-MB-231cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
MDA-MB-231	GI₅₀	10 μM Compound: LTZ	Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by cell counting based method Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by cell counting based method	[PMID: 30822713]
MDA-MB-231	GI₅₀	34 μM Compound: LTZ	Growth inhibition of human ER-negative MDA-MB-231 cells incubated for 72 hrs by cell counter method Growth inhibition of human ER-negative MDA-MB-231 cells incubated for 72 hrs by cell counter method	[PMID: 32435378]
MDA-MB-435	GI₅₀	0.067 μM Compound: Letrozole	Growth inhibition of human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
MDA-N	GI₅₀	1.61 μM Compound: Letrozole	Growth inhibition of human MDA-N cells after 48 hrs by sulforhodamine B assay Growth inhibition of human MDA-N cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
NCI/ADR-RES	GI₅₀	1.16 μM Compound: Letrozole	Growth inhibition of human NCI/ADR-RES cells after 48 hrs by sulforhodamine B assay Growth inhibition of human NCI/ADR-RES cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
NCI-H295R	GI₅₀	> 100 μM Compound: Letrozole	Growth inhibition of estrogen-sensitive human NCI-H295R cells after 72 hrs by MTT assay Growth inhibition of estrogen-sensitive human NCI-H295R cells after 72 hrs by MTT assay	[PMID: 24025069]
OVCAR-3	GI₅₀	> 100 μM Compound: Letrozole	Growth inhibition of estrogen-sensitive human OVCAR3 cells after 72 hrs by MTT assay Growth inhibition of estrogen-sensitive human OVCAR3 cells after 72 hrs by MTT assay	[PMID: 24025069]
OVCAR-3	GI₅₀	5.87 μM Compound: Letrozole	Growth inhibition of human OVCAR3 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human OVCAR3 cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
OVCAR-4	GI₅₀	0.88 μM Compound: Letrozole	Growth inhibition of human OVCAR4 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human OVCAR4 cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
OVCAR-5	GI₅₀	1.62 μM Compound: Letrozole	Growth inhibition of human OVCAR5 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human OVCAR5 cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
OVCAR-8	GI₅₀	4.5 μM Compound: Letrozole	Growth inhibition of human OVCAR8 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human OVCAR8 cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
RS4-11	GI₅₀	> 100 μM Compound: Letrozole	Growth inhibition of non-estrogen-sensitive human RS4:11 cells after 72 hrs by MTT assay Growth inhibition of non-estrogen-sensitive human RS4:11 cells after 72 hrs by MTT assay	[PMID: 24025069]
SEM	GI₅₀	> 100 μM Compound: Letrozole	Growth inhibition of non-estrogen-sensitive human SEM cells after 72 hrs by MTT assay Growth inhibition of non-estrogen-sensitive human SEM cells after 72 hrs by MTT assay	[PMID: 24025069]
SK-OV-3	GI₅₀	1.09 μM Compound: Letrozole	Growth inhibition of human SKOV3 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human SKOV3 cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
T47D	GI₅₀	0.44 μM Compound: Letrozole	Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay	[PMID: 20950898]
T47D	IC₅₀	29.5 μM Compound: Letrozole	Inhibition of aromatase activity in human T47D cells after 24 hrs Inhibition of aromatase activity in human T47D cells after 24 hrs	[PMID: 27770735]

体外研究
(In Vitro)

Letrozole（0.1-100 nM；24-96 小时）以剂量和时间依赖性方式显著抑制 MCF-7 上皮性乳腺癌细胞的生长^[2]。
Letrozole (10 nM) 显著抑制睾酮对 MCF-7 细胞增殖的刺激作用^[2]。
Letrozole（10 nM；24-48 小时）可抑制 MCF-7 细胞中分泌的金属蛋白酶（MMP-2 和 MMP-9）的水平^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:	MCF-7 cells
Concentration:	0.1, 1, 10, 100 nM
Incubation Time:	24, 48, 96 hours
Result:	Inhibited cells growth in a dose- and time-dependent manner.

体内研究
(In Vivo)

Letrozole（3-300 μg/kg；口服管饲，每天一次，持续 6 周）在大鼠中表现出抗肿瘤作用^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult female rats bearing mammary tumors^[3]
Dosage:	3, 10, 30, 100, 300 μg/kg
Administration:	Oral gavage once daily for 6 weeks
Result:	Induced complete regression of mammary tumors, with an ED₅₀ of 10-30 μg/kg/day.

Clinical Trial

分子量

285.30

Formula

C₁₇H₁₁N₅

CAS 号

112809-51-5

性状

固体

颜色

White to off-white

中文名称

来曲唑

结构分类

初始来源

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (175.25 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.5051 mL	17.5254 mL	35.0508 mL
5 mM	0.7010 mL	3.5051 mL	7.0102 mL
10 mM	0.3505 mL	1.7525 mL	3.5051 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.29 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.29 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (7.29 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.95%

选择批次：

Data Sheet (639 KB) SDS (418 KB)

COA (286 KB) HNMR (234 KB) RP-HPLC (245 KB) LCMS (93 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Bhatnagar AS, et, al. Highly selective inhibition of estrogen biosynthesis by CGS 20267, a new non-steroidal aromatase inhibitor. J Steroid Biochem Mol Biol. 1990 Dec 20;37(6):1021-7. [Content Brief]

[2]. Mitropoulou TN, et, al. Letrozole as a potent inhibitor of cell proliferation and expression of metalloproteinases (MMP-2 and MMP-9) by human epithelial breast cancer cells. Int J Cancer. 2003 Mar 20;104(2):155-60. [Content Brief]

[3]. Schieweck K, et, al. Anti-tumor and endocrine effects of non-steroidal aromatase inhibitors on estrogen-dependent rat mammary tumors. J Steroid Biochem Mol Biol. 1993 Mar;44(4-6):633-6. [Content Brief]

Letrozole 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.5051 mL	17.5254 mL	35.0508 mL	87.6271 mL
	5 mM	0.7010 mL	3.5051 mL	7.0102 mL	17.5254 mL
	10 mM	0.3505 mL	1.7525 mL	3.5051 mL	8.7627 mL
	15 mM	0.2337 mL	1.1684 mL	2.3367 mL	5.8418 mL
	20 mM	0.1753 mL	0.8763 mL	1.7525 mL	4.3814 mL
	25 mM	0.1402 mL	0.7010 mL	1.4020 mL	3.5051 mL
	30 mM	0.1168 mL	0.5842 mL	1.1684 mL	2.9209 mL
	40 mM	0.0876 mL	0.4381 mL	0.8763 mL	2.1907 mL
	50 mM	0.0701 mL	0.3505 mL	0.7010 mL	1.7525 mL
	60 mM	0.0584 mL	0.2921 mL	0.5842 mL	1.4605 mL
	80 mM	0.0438 mL	0.2191 mL	0.4381 mL	1.0953 mL
	100 mM	0.0351 mL	0.1753 mL	0.3505 mL	0.8763 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Letrozole112809-51-5CGS 20267来曲唑CGS20267CGS-20267Cytochrome P450AutophagyCYPsaromataseestrogenbreastcancerInhibitorinhibitorinhibit

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Letrozole (Synonyms: 来曲唑; CGS 20267)

Customer Review

Other Forms of Letrozole:

MCE 顾客使用本产品发表的 16 篇科研文献

Letrozole 相关产品

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参考文献

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完整储备液配制表

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Letrozole (Synonyms: 来曲唑; CGS 20267)

Customer Review

Other Forms of Letrozole:

Letrozole 相关抗体

MCE 顾客使用本产品发表的 16 篇科研文献

Letrozole 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Cytochrome P450 亚型特异性产品:

生物活性

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参考文献

Letrozole 相关抗体:

摩尔计算器

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