Name: Letrozole
Brand: Selleck Chemicals
SKU: S1235
Rating: 5 (39 reviews)

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Controllo Qualità (Quality Control)

Lotto: Purezza: 99.99%

99.99

Target correlati	Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR
Altro Aromatase Inibitori	Obacunone (AI3-37934) Fadrozole (CGS16949A) alpha-Naphthoflavone

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dell'attività	PMID
JEG3	Function assay			Inhibition of aromatase activity in human JEG3 cells, IC50=0.00089μM	18590272
JEG3	Function assay			Inhibition of aromatase in human JEG3 cells by scintillation spectrometry, IC50=0.00089μM	20148564
MDA-MB-435	Growth inhibition assay		48 hrs	Growth inhibition of human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay, GI50=0.067μM	20950898
IGROV1	Growth inhibition assay		48 hrs	Growth inhibition of human IGROV1 cells after 48 hrs by sulforhodamine B assay, GI50=0.095μM	20950898
MDA-MB-231	Growth inhibition assay		48 hrs	Growth inhibition of human MDA-MB-231cells after 48 hrs by sulforhodamine B assay, GI50=0.15μM	20950898
T47D	Growth inhibition assay		48 hrs	Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay, GI50=0.44μM	20950898
MCF7	Growth inhibition assay		48 hrs	Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B assay, GI50=0.7μM	20950898
OVCAR4	Growth inhibition assay		48 hrs	Growth inhibition of human OVCAR4 cells after 48 hrs by sulforhodamine B assay, GI50=0.88μM	20950898
BT549	Growth inhibition assay		48 hrs	Growth inhibition of human BT549 cells after 48 hrs by sulforhodamine B assay, GI50=0.89μM	20950898
SKOV3	Growth inhibition assay		48 hrs	Growth inhibition of human SKOV3 cells after 48 hrs by sulforhodamine B assay, GI50=1.09μM	20950898
NCI/ADR-RES	Growth inhibition assay		48 hrs	Growth inhibition of human NCI/ADR-RES cells after 48 hrs by sulforhodamine B assay, GI50=1.16μM	20950898
MDA-N	Growth inhibition assay		48 hrs	Growth inhibition of human MDA-N cells after 48 hrs by sulforhodamine B assay, GI50=1.61μM	20950898
OVCAR5	Growth inhibition assay		48 hrs	Growth inhibition of human OVCAR5 cells after 48 hrs by sulforhodamine B assay, GI50=1.62μM	20950898
Hs 578T	Growth inhibition assay		48 hrs	Growth inhibition of human Hs 578T cells after 48 hrs by sulforhodamine B assay, GI50=2.17μM	20950898
OVCAR8	Growth inhibition assay		48 hrs	Growth inhibition of human OVCAR8 cells after 48 hrs by sulforhodamine B assay, GI50=4.5μM	20950898
OVCAR3	Growth inhibition assay		48 hrs	Growth inhibition of human OVCAR3 cells after 48 hrs by sulforhodamine B assay, GI50=5.87μM	20950898
MCF7a	Cytotoxicity assay		10 days	Cytotoxicity against human MCF7a cells expressing Tet-off-3betaHSD1-Arom assessed as inhibition of TST-stimulated cell proliferation measured after 10 days, EC50=0.000004μM	22951074
V79MZh	Function assay			Inhibition of human CYP11B2 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxy-corticosterone as substrate, IC50=1.42μM	23281812
V79MZh	Function assay			Inhibition of human CYP11B1 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxy-corticosterone as substrate, IC50=2.62μM	23281812
H295R	Function assay	5 uM	24 hrs	Inhibition of CYP19 in human H295R cells using [1beta-3H(N)]-androst-4-ene-3,17-dione at 5 uM after 24 hrs by tritiated water release assay	24025069
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against estrogen-dependent human MCF7 cells after 72 hrs by MTT assay, IC50=0.007μM	24345481
MCF7	Cytotoxicity assay		24 to 96 hrs	Cytotoxicity against human MCF7 cells after 24 to 96 hrs, IC50=0.02μM	24345481
JEG-3	Function assay			Inhibition of aromatase (unknown origin) expressed in JEG-3 cells, IC50=0.00089μM	25992880
insect cells	Function assay		30 mins	Inhibition of recombinant human CYP19 expressed in baculovirus infected insect cells using MFC as substrate measured after 30 mins by fluorometric analysis, IC50=0.0053μM	27647367
T47D	Function assay		24 hrs	Inhibition of aromatase activity in human T47D cells after 24 hrs, IC50=29.5μM	27770735
T47D	Function assay		24 hrs	Inhibition of aromatase activity in human T47D cells after 24 hrs, IC50=29.5μM	28427017
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=4.73μM	29202405
MCF7	Growth inhibition assay		72 hrs	Growth inhibition of human MCF7 cells incubated for 72 hrs by cell counting based method, GI50=4.1μM	30822713
MDA-MB-231	Growth inhibition assay		72 hrs	Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by cell counting based method, GI50=10μM	30822713
insect cells	Function assay			Inhibition of recombinant human aromatase expressed in baculovirus infected insect cells using O-benzyl fluorescein benzyl ester as substrate in presence of NADPH generating system by fluorescence based analysis, IC50=0.0019μM	31416738
MCF-7aro	Function assay		1 hr	Inhibition of aromatase in human MCF-7aro cells using [1beta-3H] androstenedione as substrate incubated for 1 hr by liquid scintillation counting method, IC50=0.0019μM	31732252
insect cells	Function assay		30 mins	Inhibition of human recombinant aromatase expressed in baculovirus infected insect cells using O-benzylfluorescein benzyl ester as substrate after 30 mins, IC50=0.0011μM	ChEMBL
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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	285.3	Formula	C₁₇H₁₁N₅	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	112809-51-5	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	CGS 20267			Smiles	C1=CC(=CC=C1C#N)C(C2=CC=C(C=C2)C#N)N3C=NC=N3

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 57 mg/mL (199.78 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	2.850mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 57 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	0.450mg/ml (1.58mM)	Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Targets/IC₅₀/Ki	Aromatase (Cell-free assay) 0.07 nM-20 nM
In vitro	Letrozole potently inhibits aromatase derived from a variety of different sources including human placental microsomes, particulate fractions of human breast cancer, rat ovarian microsomes, MCF-7 cells transfected with aromatase (MCF-7Ca), JEG-3 human choriocarcinoma cells , CHO cells, hamster ovarian tissue, and particulate fractions of human breast cancer with IC50 of 11, 2, 7, 0.07, 0.07, 1.4, 20 and 0.8 nM. In the non-cellular systems, the IC50 of this compound is calculated to be 1-13 nM. It maximally inhibits estradiol production in vitro in LH-stimulated hamster ovarian tissue at 0.1 μM with an IC50 of 0.02 μM and does not significantly affect progesterone production up to 350 μM. In ACTH-stimulated rat adrenal tissue in vitro, aldosterone production is inhibited by with an IC50 of 210 μM. This chemical inhibits growth of the MCF-7 epithelial breast cancer cells in a dose-dependent way with IC50 of 1 nM. Inhibition can be observesed even at the very low concentrations tested (0.1 nM). Treatment of normal MCF-12A epithelial cells with this compound did not affect their growth even when high letrozole concentrations (100 nM) or prolonged culture times. Concurrent administration of 17-β-estradiol with it (10 nM) decreased the stimulatory effect of the enzymatic activity of MMP-2 and - 9 released by estradiol.
Saggio chinasico	Attività dell'aromatasi placentare umana
Saggio chinasico	Il saggio viene eseguito in un volume totale di 1 mL a 37 ℃. Se non diversamente specificato, la miscela di incubazione contiene 11 nM di [4- ¹⁴C] androstene-3, 17-dione ([4- ¹⁴C]A), 24 mM di NADPH (sale tetrasodico Tipo III), le concentrazioni appropriate dell'inibitore desiderato e 120 μg di proteina microsomiale. Il (4- ¹⁴C)A viene aggiunto come soluzione in 1,7% di etanolo in tampone fosfato di potassio 0,05 M (pH 7,4), in modo che la concentrazione finale di etanolo non superi lo 0,02% (v/v). La reazione viene avviata con l'aggiunta dell'enzima e interrotta dopo 20 min con l'aggiunta di 7 volumi di acetato di etile. La miscela viene agitata su un vortex e centrifugata a 600 g per 5 min. La fase acquosa viene ri-estratta con 7 volumi di acetato di etile, e gli estratti combinati vengono evaporati a secco utilizzando un Evapo-Mix. Oltre il 99% della radioattività del [4- ¹⁴C] aggiunto viene recuperato utilizzando questo sistema di estrazione. Il residuo ottenuto viene disciolto in 150 μL di acetone, e aliquote da 100 μL vengono cromatografate per 65 min su piastre a strato sottile pre-rivestite con gel di silice 60 utilizzando etil acetato: isooctano (140:60, v/v; sistema A) o toluene: cloroformio: metanolo (70:140:20; sistema B). Le zone radioattive della piastra vengono localizzate con uno scanner a strato sottile Berthold LB 2760. I picchi radioattivi di estradiolo (E2) ed estrone (E1) vengono identificati per confronto con standard autentici. La corrispondente banda di legame del gel di silice viene trasferita in fiale contenenti 10 mL di liquido di scintillazione e contata con un sistema di scintillazione liquida 6880.
In vivo	Letrozole inhibits aromatase in vivo with ED50 of 1-3 μg/kg p.o.. This compound displays anti-endocrine effects. It inhibits androstenedione-induced uterine hypertrophy in immature rats with ED50 of 1-3 μg/kg. In the adult female rat, this compound (0.3-1 mg/kg daily p.o., 14 days) completely interrupts ovarian cyclicity and reduces uterine weight and serum estradiol (E2) concentrations to a similar extent to that seen after ovariectomy. This chemical induces dose-dependent regression of estrogen-dependent, 9,10-dimethylbenz-a-anthracene-induced mammary tumors in adult female rats. The ED50 for it is determined to be 10 - 30 µg/kg/day, with complete inhibition at a daily dose of 10 µg/day. It produces dose-dependent inhibition of tumor growth of MCF-7 cells transfected with human aromatase gene (MCF-7Ca) implanted athymic nude mice, with complete inhibition at 20 mg/kg per day p.o..
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/14630089/ [2] https://pubmed.ncbi.nlm.nih.gov/2149502/ [3] https://pubmed.ncbi.nlm.nih.gov/12569569/ [4] https://pubmed.ncbi.nlm.nih.gov/20095792/ [5] https://pubmed.ncbi.nlm.nih.gov/7628871/ [6] https://pubmed.ncbi.nlm.nih.gov/2973160/

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT06143631	Not yet recruiting	Leiomyoma Uterine\|Leiomyoma\|Fibroid\|Fibroid Uterus	University of California San Francisco\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)	May 13 2024	Phase 4
NCT05872204	Recruiting	Low Grade Serous Ovarian Carcinoma\|Adult Type Granulosa Cell Tumor	Universitaire Ziekenhuizen KU Leuven\|Kom Op Tegen Kanker\|Eli Lilly and Company\|European Network of Gynaecological Oncological Trial Groups (ENGOT)	November 30 2023	Phase 2

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):

Letrozole Aromatase Inibitore

Peso molecolare: 285.3

Controllo Qualità (Quality Control)

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Solubilità (Solubility)

Calcolatore di Molarità

Calcolatore di formulazione in vivo (Soluzione chiara)

Meccanismo d'azione (Mechanism of Action)

Informazioni sullo studio clinico (Clinical Trial Information)

Letrozole Aromatase Inibitore

Peso molecolare: 285.3

Controllo Qualità (Quality Control)

Coltura cellulare, trattamento e concentrazione di lavoro (Cell Culture, Treatment & Working Concentration)

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Solubilità (Solubility)

Calcolatore di Molarità

Calcolatore di formulazione in vivo (Soluzione chiara)

Meccanismo d'azione (Mechanism of Action)

Informazioni sullo studio clinico (Clinical Trial Information)

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)