Letrozole Inhibitor CAS No. 112809-51-5

Cat. No.	Name	Size	Price
KI1204	Letrozole	25 mg	$130
	Letrozole	50 mg	$170
	Letrozole	250 mg	$530

Chemical Characteristic

Product Name	Letrozole
Synonyms	CGS 20267
CAS No.	112809-51-5
Molecular Weight	285.3
Formula	C₁₇H₁₁N₅
Chemical Name	4,4'-(1H-1,2,4-Triazol-1-ylmethylene)bisbenzonitrile
Smiles	C(n1ncnc1)(c1ccc(C#N)cc1)c1ccc(C#N)cc1
Chemical Structure
Documents	HNMR COA HPLC MS

Biological activities

Letrozole is a third generation potent and selective aromatase inhibitor. Letrozole is used for the treatment of breast cancer. Letrozole inhibits CYP2A6 activity in HLMs (HL-SD109) and expresses CYP2A6, with IC50 of 5.90 and 12.5 µM, respectively. Letrozole also shows modest inhibition of CYP2C19 in HLMs and expresses CYP2C19 with IC50 of 24.8 and 62.9 µM, respectively. ^[1] Letrozole potently inhibits estrogen and aldosterone production with IC50 of 0.02 and 210 µM, respectively. Letrozole potently inhibits aromatase derived from a variety of different sources including human placental and rat ovarian microsomes, hamster ovarian cells. ^[2] Letrozole effectively inhibits the proliferation of MCF-7aro monolayer cell with IC50 of 50??00nM. ^[3] Letrozole inhibits steroid-deprived T47D/Aro cell proliferation with an IC50 of 67 nM. ^[4] Letrozole causes almost complete regression of estrogen-dependent DMBA-induced mammary tumors in adult female rats at a dose of 100 µg/kg per day, with an ED50 of 10-30 µg/kg per day. ^[2]

Protocols

Letrozole is dissolved and diluted in methanol to the required concentrations and any methanol is removed by drying in speed vacuum before the addition of the incubation components. ^[1]

References

[1] Jeong S, et al. Inhibition of drug metabolizing cytochrome P450s by the aromatase inhibitor drug letrozole and its major oxidative metabolite 4,4'-methanol- bisbenzonitrile in vitro. Cancer Chemother Pharmacol. 2009, 64(5): 867-875. [2] Haynes BP, et al. The pharmacology of letrozole. J Steroid Biochem Mol Biol. 2003, 87(1): 35-45. [3] Kijima I, et al. Growth inhibition of estrogen receptor-positive and aromatase-positive human breast cancer cells in monolayer and spheroid cultures by letrozole, anastrozole, and tamoxifen. J Steroid Biochem Mol Biol. 2005, 97(4): 360-368. [4] Lisztwan J, et al. The aromatase inhibitor letrozole and inhibitors of insulin-like growth factor I receptor synergistically induce apoptosis in in vitro models of estrogen-dependent breast cancer. Breast Cancer Res. 2008, 10(4): R56.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services