Letrozole (Synonyms: CGS 20267)

Name: Letrozole
Brand: MedChemExpress
SKU: HY-14248
Rating: 5.0 (20 reviews)

Art. -Nr.: HY-14248 Reinheit: 99.95%: Data Sheet
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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.

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CAS. Nr. : 112809-51-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
25 mg	Auf Lager	Estimated Time of Arrival: December 31
50 mg	Auf Lager	Estimated Time of Arrival: December 31
100 mg	Auf Lager	Estimated Time of Arrival: December 31
200 mg	Auf Lager	Estimated Time of Arrival: December 31
500 mg	Auf Lager	Estimated Time of Arrival: December 31
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Based on 20 publication(s) in Google Scholar

Other Forms of Letrozole:

Letrozole-d₄ In-stock
Letrozole (Standard) In-stock

20 Publications Citing Use of MCE Letrozole

Cell Proliferation/Viability Assay

Cell Imaging/Staining

RT-PCR

In Vivo Imaging

IHC

: Letrozole purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2023 May;30(5):1260-1278. [Abstract]; Letrozole (10^-9-10^-1 M; 4 weeks). The IC50 experiment revealed that BAP18 deletion dramatically lowered the half-death concentration of Letrozole in MCF7 cells. Cells were treated with different concentrations of Letrozole for four weeks before counting the number of cells in each concentration group using cell counts.

: Letrozole purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2021 Jul 1:217:112255. [Abstract]; PC3 cells were treated with 50 nM Letrozole for 0 h, 24 h, 48 h and 72 h, and the mRNA expression level of MMP12 was assayed by RT-PCR.

: Letrozole purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2021 Jul 1:217:112255. [Abstract]; Letrozole (LE; 10 μg/day for 30 days; ip). Representative images of in vivo bioluminescent imaging for mice in the 5 groups using the IVIS imaging system.

: Letrozole purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2021 Jul 1:217:112255. [Abstract]; Letrozole (LE; 10 μg/day for 30 days; ip). Representative images of the tumours immunostained with antibodies against aromatase, CD44 and MMP12.

: Letrozole purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2020 Nov 4;48(19):10768-10784. [Abstract]; Letrozole (10-50 nM; 14 days). The influence of BAP18 on endocrine drug sensitivity in T47D cells. T47D cells were pre-transfected with FLAG-tagged PcDNA3 plasmids (Parental) and BAP18 expression plasmids (oeBAP18). Cultured in different concentrations of three kinds of endocrine drugs for 14 days, cells in wells were stained by R250 and photographs represented one of three independent experiments.

: Letrozole purchased from MedChemExpress. Usage Cited in: Exp Ther Med. 2018 Jun;15(6):5269-5274. [Abstract]; Letrozole (100 nM; 72 h). 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 purchased from MedChemExpress. Usage Cited in: Exp Ther Med. 2018 Jun;15(6):5269-5274. [Abstract]; Letrozole (100 nM; 72 h). Detection of the effect of Letrozole on the MAPK pathway by western blotting.

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

Biologische Aktivität
Reinheit & Dokumentation
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Beschreibung

IC₅₀ & Target

Aromatase

Cellular Effect

Cell Line	Type	Value	Description	References
BT-549	GI₅₀	0.89 3 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]
BT-549	GI₅₀	0.89 3 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]
ARO	IC₅₀	1.8 1 Compound: 1; LTZ	Inhibition of human recombinant aromatase using ARO as substrate Inhibition of human recombinant aromatase using ARO as substrate	[PMID: 37037140]
HeLa	GI₅₀	> 100 3 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]
JEG-3	IC₅₀	0.89 1 Compound: 111	Inhibition of aromatase (unknown origin) expressed in JEG-3 cells Inhibition of aromatase (unknown origin) expressed in JEG-3 cells	[PMID: 25992880]
BT-549	GI₅₀	0.89 3 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]
Hs-578T	GI₅₀	2.17 3 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]
JEG-3	IC₅₀	0.89 1 Compound: letrozole	Inhibition of aromatase activity in human JEG3 cells Inhibition of aromatase activity in human JEG3 cells	[PMID: 18590272]
HT-29	GI₅₀	> 100 3 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]
JEG-3	IC₅₀	0.89 1 Compound: letrozole	Inhibition of aromatase in human JEG3 cells by scintillation spectrometry Inhibition of aromatase in human JEG3 cells by scintillation spectrometry	[PMID: 20148564]
IGROV-1	GI₅₀	> 100 3 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]
ARO	IC₅₀	1.8 1 Compound: 1; LTZ	Inhibition of human recombinant aromatase using ARO as substrate Inhibition of human recombinant aromatase using ARO as substrate	[PMID: 37037140]
MCF7	IC₅₀	7 1 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]
IGROV-1	GI₅₀	0.095 3 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 1 Compound: letrozole	Inhibition of aromatase in human JEG3 cells by scintillation spectrometry Inhibition of aromatase in human JEG3 cells by scintillation spectrometry	[PMID: 20148564]
HeLa	GI₅₀	>100 3 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]
MCF7	IC₅₀	20 1 Compound: Letrozole	Cytotoxicity against human MCF7 cells after 24 to 96 hrs Cytotoxicity against human MCF7 cells after 24 to 96 hrs	[PMID: 24345481]
Jurkat	GI₅₀	> 100 3 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]
Hs-578T	GI₅₀	2.17 3 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]
MCF-10A	IC₅₀	> 10 3 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]
HT-29	GI₅₀	> 100 3 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]
MCF7	GI₅₀	> 100 3 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]
HT-29	GI₅₀	>100 3 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]
HeLa	GI₅₀	> 100 3 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]
MCF7	GI₅₀	0.7 3 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]
IGROV-1	GI₅₀	>100 3 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]
Hs-578T	GI₅₀	2.17 3 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]
IGROV-1	GI₅₀	0.095 3 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]
MCF7	IC₅₀	20 1 Compound: Letrozole	Cytotoxicity against human MCF7 cells after 24 to 96 hrs Cytotoxicity against human MCF7 cells after 24 to 96 hrs	[PMID: 24345481]
IGROV-1	GI₅₀	0.095 3 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]
MCF7	IC₅₀	4.1 3 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]
Jurkat	GI₅₀	>100 3 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]
IGROV-1	GI₅₀	> 100 3 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]
MCF7	GI₅₀	4.1 3 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]
MCF-10A	IC₅₀	>10 3 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]
JEG-3	IC₅₀	0.89 1 Compound: 111	Inhibition of aromatase (unknown origin) expressed in JEG-3 cells Inhibition of aromatase (unknown origin) expressed in JEG-3 cells	[PMID: 25992880]
MCF-10A	IC₅₀	>100 3 Compound: 1; LTZ	Cytotoxicity against human MCF-10A cells incubated for 72 hrs by CCK8 assay Cytotoxicity against human MCF-10A cells incubated for 72 hrs by CCK8 assay	[PMID: 37037140]
MCF7	IC₅₀	4.73 3 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]
JEG-3	IC₅₀	0.89 1 Compound: letrozole	Inhibition of aromatase activity in human JEG3 cells Inhibition of aromatase activity in human JEG3 cells	[PMID: 18590272]
MCF7	GI₅₀	>100 3 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	IC₅₀	7 1 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]
JEG-3	IC₅₀	0.89 1 Compound: letrozole	Inhibition of aromatase in human JEG3 cells by scintillation spectrometry Inhibition of aromatase in human JEG3 cells by scintillation spectrometry	[PMID: 20148564]
MDA-MB-231	GI₅₀	0.15 3 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]
MCF7	GI₅₀	0.7 3 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]
Jurkat	GI₅₀	> 100 3 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 3 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]
MDA-MB-231	GI₅₀	10 3 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]
MCF7	GI₅₀	4.1 3 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]
MDA-MB-231	GI₅₀	34 3 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]
MCF7	IC₅₀	4.1 3 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]
MCF-10A	IC₅₀	> 100 3 Compound: 1; LTZ	Cytotoxicity against human MCF-10A cells incubated for 72 hrs by CCK8 assay Cytotoxicity against human MCF-10A cells incubated for 72 hrs by CCK8 assay	[PMID: 37037140]
MDA-MB-435	GI₅₀	0.067 3 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]
MCF7	IC₅₀	>100 3 Compound: 1; LTZ	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay	[PMID: 37037140]
MCF-10A	IC₅₀	> 100 3 Compound: LTZ	Anti-proliferative activity against human MCF-10A cells incubated for 96 hrs by CCK8 assay Anti-proliferative activity against human MCF-10A cells incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
MDA-N	GI₅₀	1.61 3 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]
MCF7	IC₅₀	4.73 3 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	GI₅₀	0.7 3 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]
NCI/ADR-RES	GI₅₀	1.16 3 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]
MDA-MB-231	GI₅₀	34 3 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]
MCF7	GI₅₀	4.1 3 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]
NCI-H295R	GI₅₀	> 100 3 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]
MDA-MB-231	GI₅₀	10 3 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]
MCF7	GI₅₀	> 100 3 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	IC₅₀	20 1 Compound: Letrozole	Cytotoxicity against human MCF7 cells after 24 to 96 hrs Cytotoxicity against human MCF7 cells after 24 to 96 hrs	[PMID: 24345481]
OVCAR-3	GI₅₀	> 100 3 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]
MDA-MB-231	GI₅₀	0.15 3 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]
OVCAR-3	GI₅₀	5.87 3 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]
MDA-MB-435	GI₅₀	0.067 3 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]
MCF7	IC₅₀	4.1 3 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]
OVCAR-4	GI₅₀	0.88 3 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]
MDA-N	GI₅₀	1.61 3 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]
MCF7	IC₅₀	4.73 3 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 1 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]
OVCAR-5	GI₅₀	1.62 3 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]
NCI/ADR-RES	GI₅₀	1.16 3 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]
MCF7	IC₅₀	8.8 3 Compound: LTZ	Anti-proliferative activity against ERalpha positive human MCF7 cells incubated for 96 hrs by CCK8 assay Anti-proliferative activity against ERalpha positive human MCF7 cells incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
OVCAR-8	GI₅₀	4.5 3 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]
NCI-H295R	GI₅₀	>100 3 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]
MCF7	IC₅₀	> 100 3 Compound: 1; LTZ	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay	[PMID: 37037140]
RS4-11	GI₅₀	> 100 3 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]
OVCAR-3	GI₅₀	>100 3 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]
SEM	GI₅₀	> 100 3 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]
OVCAR-3	GI₅₀	5.87 3 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]
MCF7	IC₅₀	> 100 3 Compound: LTZ	Antiproliferative activity against human resistant MCF7 cells harboring EGFR assessed as cell viability incubated for 96 hrs by CCK8 assay Antiproliferative activity against human resistant MCF7 cells harboring EGFR assessed as cell viability incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
SK-OV-3	GI₅₀	1.09 3 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]
OVCAR-4	GI₅₀	0.88 3 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]
MCF7	IC₅₀	> 100 3 Compound: LTZ	Antiproliferative activity against human resistant MCF7 cells harboring ERalpha D538G mutant at LBD assessed as cell viability incubated for 96 hrs by CCK8 assay Antiproliferative activity against human resistant MCF7 cells harboring ERalpha D538G mutant at LBD assessed as cell viability incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
T47D	GI₅₀	0.44 3 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]
OVCAR-5	GI₅₀	1.62 3 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]
MCF7	IC₅₀	> 100 3 Compound: LTZ	Antiproliferative activity against human resistant MCF7 cells harboring ERalpha Y537S mutant at LBD assessed as cell viability incubated for 96 hrs by CCK8 assay Antiproliferative activity against human resistant MCF7 cells harboring ERalpha Y537S mutant at LBD assessed as cell viability incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
T47D	IC₅₀	29.5 3 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]
OVCAR-8	GI₅₀	4.5 3 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]
MDA-MB-231	GI₅₀	0.15 3 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]
RS4-11	GI₅₀	>100 3 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]
MDA-MB-231	GI₅₀	10 3 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]
SEM	GI₅₀	>100 3 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]
MDA-MB-231	GI₅₀	34 3 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]
SK-OV-3	GI₅₀	1.09 3 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]
MDA-MB-435	GI₅₀	0.067 3 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]
T47D	GI₅₀	0.44 3 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]
MDA-N	GI₅₀	1.61 3 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]
T47D	IC₅₀	29.5 3 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]
NCI-H295R	GI₅₀	> 100 3 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]
NCI/ADR-RES	GI₅₀	1.16 3 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]
OVCAR-3	GI₅₀	5.87 3 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-3	GI₅₀	> 100 3 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-4	GI₅₀	0.88 3 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 3 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 3 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 3 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 3 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 3 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 3 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 3 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]

In Vitro

Letrozole (0.1-100 nM; 24-96 h) significantly inhibits growth of the MCF-7 epithelial breast cancer cells in a dose- and time-dependent manner^[2].
Letrozole (10 nM) significantly suppresses the stimulatory effects of testosterone on MCF-7 cell proliferation^[2].
Letrozole (10 nM; 24-48 h) suppresses the levels of secreted metalloproteinases (MMP‐2 and MMP‐9) in MCF-7 cells^[2].

MedChemExpress (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.

In Vivo

Letrozole (3-300 μg/kg; oral gavage once daily for 6 weeks) exhibits anti-tumor effects in rats^[3].

MedChemExpress (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.

Klinische Studie

Molekulargewicht

285.30

Formel

C₁₇H₁₁N₅

CAS. Nr.

112809-51-5

Appearance

Solid

Color

White to off-white

SMILES

N#CC1=CC=C(C(N2C=NC=N2)C3=CC=C(C#N)C=C3)C=C1

Structure Classification

Initial Source

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (175.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner
Verdünnungsrechner

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Reinheit & Dokumentation

Purity: 99.95%

Select Batch:

Data Sheet (276 KB) SDS (418 KB)

COA (249 KB) HNMR (234 KB) RP-HPLC (245 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

Verweise

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

Letrozole Related Classifications

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 20267CGS20267CGS-20267Cytochrome P450AutophagyCYPsaromataseestrogenbreastcancerInhibitorinhibitorinhibit

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Letrozole (Synonyms: CGS 20267)

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Letrozole Related Antibodies

20 Publications Citing Use of MCE Letrozole

Spezialitätsempfehlungen

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Biologische Aktivität

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Verweise

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Letrozole Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

Letrozole Related Classifications

Keywords:

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