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Fulvestrant (ICI-182780) antagonista del recettore degli estrogeni

Name: Fulvestrant (ICI-182780)
Brand: Selleck Chemicals
SKU: S1191
Rating: 5 (180 reviews)

N. Cat.S1191

Il Fulvestrant è un antagonista del recettore degli estrogeni (ER) con IC50 di 0,94 nM in un saggio senza cellule. Il Fulvestrant induce anche l'autophagy e l'apoptosis e ha attività antitumorale.

Fulvestrant (ICI-182780) Estrogen/progestogen Receptor antagonista Chemical Structure

Struttura chimica

Peso molecolare: 606.77

Vai a

Controllo Qualità

Lotto: Purezza: 99.97%

99.97

Target correlati	Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR
Altro Estrogen/progestogen Receptor Inibitori	Elacestrant (RAD1901) Dihydrochloride Vepdegestrant (ARV-471) MPP dihydrochloride Kaempferol Cholesterol G15 Endoxifen HCl Licochalcone A Chrysin Pregnenolone

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Formulazione	Descrizione dellattività	PMID
MCF-7	Growth Inhibition Assay	1.3-1000 nM	48 h		inhibits cell growth in a dose-dependent manner	24979294
MCF-7/LTED	Growth Inhibition Assay	1.3-1000 nM	48 h		inhibits cell growth in a dose-dependent manner	24979294
HCC1428	Growth Inhibition Assay	1.3-1000 nM	48 h		inhibits cell growth in a dose-dependent manner	24979294
HCC1428/LTED	Growth Inhibition Assay	1.3-1000 nM	48 h		inhibits cell growth in a dose-dependent manner	24979294
LCC1	Function Assay	100 nM	48-144 h		activates UPR signaling	24858277
LCC9	Function Assay	100 nM	48-144 h		activates UPR signaling	24858277
MCF-7	Growth Inhibition Assay	100 nM	5 d		inhibits cell growth to 10％	24819550
mesangial	Function Assay	0.1-100 nM	48 h		suppresses TGF-β1-induced type IV collagen	24793639
Mesangial	Function Assay	0.1-100 nM	0.5 h		inhibits TGF-β1-induced Smad2 phosphorylation via GPER	24793639
ER+ MCF-7/2a	Growth Inhibition Assay				IC50=0.004 μM	15324884
ER+ MCF-7	Growth Inhibition Assay		200 h		IC50=0.21 nM	15324884
MCF-7	Function Assay	10 nM	72 h		reverses the estrogen effect(IC50 1.9 × 10−9 M)	24908652
MCF-7	Growth Inhibition Assay				IC50 of approximately 2 nM	23448346
H1975	Growth Inhibition Assay	3 μM	1 m		increases the gefitinib sensitivity of H1975 cells	24268810
H1975	Function Assay	3 μM	1 m		upregulates the level of Let-7c	24268810
MCF-7	Function Assay	100 nM	72 h		reverses the protective effect of E2 in cell invasion	23936773
MCF-7	Function Assay	100 nM	24/48 h		facilitates invasion through MMPs' modulation	23936773
BT474-tet-shMED1	Growth Inhibition Assay	0.1-5 μM	7 d		increases +Dox induced cell death in a dose-dependent manner	23936234
ZR75-1-tet-shMED1	Growth Inhibition Assay	0.1-5 μM	7 d		increases +Dox induced cell death in a dose-dependent manner	23936234
MCF-7-tet-shMED1	Growth Inhibition Assay	0.1-5 μM	7 d		increases +Dox induced cell death in a dose-dependent manner	23936234
HepG2	Function Assay	0.01-10 μM	18 h		activates the ERE-mediated transcription of AF2ER	23733188
MCF-7L	Function Assay	100 nM	10 min/24 h/48 h		results in EGFR, HER2 and HER3 phosphorylation at prolonged exposure	23686416
MCF-7L	Function Assay	100 nM	48 h		induces upregulation of mRNA of EGFR ligand HB-EGF	23686416
MCF-7L	Function Assay	100 nM	48 h		induces EGFR family member activation required ER	23686416
C4-12	Function Assay	100 nM	48 h		induces EGFR family member activation required ER	23686416
MCF-7L	Function Assay	100 nM	24 h		induces EGFR phosphorylation required HB-EGF function	23686416
MMQ	Function Assay	0-625 nM	72 h		down-regulates the expression of estrogen receptor-α (ERα)	23523357
H1975	Growth Inhibition Assay	0.3125-10 μM	6 d		inhibits cell growth in a dose-dependent manner	23399957
H1975	Apoptosis Assay	200 nM	72 h		enhances erlotinib induced apoptosis	23399957
MCF-7	Growth Inhibition Assay	10/100/1000 nM	2/4/6 d	DMSO	inhibits cell growth in both dose- and time- dependent manner	23313506
MCF-7	Growth Inhibition Assay	100 nM	4 d	DMSO	induces a higher proportion of cells in the G1 phase	23313506
MLO-Y4	Function Assay	1 μM	1 h		inhibits E2-induced Cx43 expression	23247057
MCF-7	Growth Inhibition Assay	100 nM	48 h		abrogates the proliferative effect of moderate nitrosative stress	23216744
TG1-1	Function Assay	1 μM	24 h		abrogates E2 induced accumulation of HIF-1α	23088607
TG1-1	Function Assay	1 μM	24 h		abrogates E2 induced accumulation of PI3K	23088607
MCF7	Growth Inhibition Assay	100 nM	48 h		leads to a similar loss in survival as with doxorubicin alone	23077249
MCF7	Growth Inhibition Assay	100 nM	48 h		enhances nutlin-mediated cell death	23077249
MCF-7	Function Assay		6 h	DMSO	attenuates the fludioxonil- or fenhexamid-induced increase in miR-21 expression	23052036
MCF-7	Growth Inhibition Assay	100 nM/1 μM	5 d		inhibits the stimulation of 17β-estradiol	22982765
MCF-7	Growth Inhibition Assay	100 nM	5 d		inhibits the stimulation of fusarielin H	22982765
1471.1	Function Assay	100 nM	1 h	EtOH	takes on a punctate staining pattern	22869106
MCF-7	Function Assay	100 nM	1 h	EtOH	takes on a punctate staining pattern	22869106
HeLa	Function Assay	100 nM	1 h	EtOH	takes on a punctate staining pattern	22869106
COS-7	Function Assay	100 nM	1 h	EtOH	takes on a punctate staining pattern	22869106
BG1L-OHTLT	Function Assay	10 nM	24 h		inhibits ERα expression	22652558
BG1L-ICILT	Function Assay	10 nM	24 h		inhibits ERα expression	22652558
PC-9	Growth Inhibition Assay	0.003-30 μM	48 h		inhibits cell growth in a dose-dependent manner	22560634
H1650	Growth Inhibition Assay	0.003-30 μM	48 h		inhibits cell growth in a dose-dependent manner	22560634
H1975	Growth Inhibition Assay	0.003-30 μM	48 h		inhibits cell growth in a dose-dependent manner	22560634
H1975	Function Assay	3 μM	3 h		abrogates the phospho-EGFR induction by estrogen	22560634
H1975	Function Assay	3 μM	7 d		induces EGFR expression	22560634
HTR-8	Function Assay	1 μM	1-48 h		down-regulates the expression of IGFBP7 mRNA	22383111
JEG-3	Function Assay	1 μM	1-48 h		down-regulates the expression of IGFBP7 mRNA	22383111
Huh7	Function Assay	50 μM	48 h		inhibits genistein-mediated PON1 transactivation	22304296
201T	Growth Inhibition Assay	5 μM	72 h		inhibits cell growth significantly combined with vandetanib	22258476
A549	Growth Inhibition Assay	5 μM	72 h		inhibits cell growth significantly combined with vandetanib	22258476
MCF-7	Function Assay	1 μM	24 h		downregulates ER expression induced by 4-OH-T	22049316
HCC-1428	Function Assay	1 μM	24 h		downregulates ER expression induced by 4-OH-T	22049316
MDA-361	Function Assay	1 μM	24 h		downregulates ER expression induced by 4-OH-T	22049316
ZR75-1	Function Assay	1 μM	24 h		downregulates ER expression induced by 4-OH-T	22049316
MCF-7	Growth Inhibition Assay	1 μM	5-10 d		suppresses E2-induced growth inhibition	22049316
HCC-1428	Growth Inhibition Assay	1 μM	5-10 d		suppresses E2-induced growth inhibition	22049316
MDA-361	Growth Inhibition Assay	1 μM	5-10 d		suppresses E2-induced growth inhibition	22049316
ZR75-1	Growth Inhibition Assay	1 μM	5-10 d		suppresses E2-induced growth inhibition	22049316
MCF-7/AC-1	Growth Inhibition Assay	0-0.2 μM	6 d		inhibits cell growth modestly	22042792
MCF7	Growth Inhibition Assay	10 µM	48 h		induces cell inhibition which can be enhanced by fibroblasts	22041887
MMQ	Growth Inhibition Assay	0-625 nM	72 h		produces statistically significant inhibition of cell proliferation	22015101
MMQ	Function Assay	0-625 nM	72 h		produces a statistically significant, dose-dependent reduction in PRL secretion	22015101
MCF7	Growth Inhibition Assay	0-1 μM	24-120 h		inhibits the growth of MCF7-YB-1	21863258
HepG2	Apoptosis Assay	0.1 μM	24 h		abolishes the estrogen-induced up-regulation of apoAI and apoM	21816233
MCF7–iFR3	Growth Inhibition Assay	20-100 nM	96 h		enhances AP-induced cell growth inhibition	21792889
MCF7S	Function Assay	1 μM	48 h		downregulates overall ERα protein levels	21533195
MCF7	Function Assay	1 μM	48 h		downregulates overall ERα protein levels	21533195
MCF7S	Function Assay	1 μM	7 d		attenuates tumorsphere formation and proliferation	21533195
MCF7S	Growth Inhibition Assay	0.5/1 μM	7 d	DMSO	decreases cell expansion	21533195
T47D	Growth Inhibition Assay	4 nM	40 h		suppresses cell growth moderately	21480391
BT474	Growth Inhibition Assay	4 nM	40 h		suppresses cell growth moderately	21480391
T47D	Function Assay	10 nM	40 h		downregulates ERα protein	21480391
BT474	Function Assay	10 nM	40 h		downregulates ERα protein	21480391
MCF7	Function Assay	100 nM	7 d		reduces ERα expression significantly	21396094
T47D	Function Assay	100 nM	7 d		reduces ERα expression significantly	21396094
BT474	Function Assay	100 nM	7 d		reduces ERα expression significantly	21396094
MDAMB361	Function Assay	100 nM	7 d		reduces ERα expression significantly	21396094
MCF7	Growth Inhibition Assay	0.01-1 μM	7 d		reduces cell growth significantly	21396094
T47D	Growth Inhibition Assay	0.01-1 μM	7 d		reduces cell growth significantly	21396094
BT474	Growth Inhibition Assay	0.01-1 μM	7 d		reduces cell growth significantly	21396094
MDAMB361	Growth Inhibition Assay	0.01-1 μM	7 d		reduces cell growth significantly	21396094
MCF7	Function Assay	100 nM	7 d		induces of ErbB3 and ErbB4 receptor expression and signalling	21396094
T47D	Function Assay	100 nM	7 d		induces of ErbB3 and ErbB4 receptor expression and signalling	21396094
BT474	Function Assay	100 nM	7 d		induces of ErbB3 and ErbB4 receptor expression and signalling	21396094
MDAMB361	Function Assay	100 nM	7 d		induces of ErbB3 and ErbB4 receptor expression and signalling	21396094
MCF7	Function Assay	10 nM	96 h		downregulates ER expression	21378333
MDA-MB-231	Function Assay	10 nM	96 h		downregulates ER expression	21378333
SK-BR-3	Function Assay	10 nM	96 h		downregulates ER expression	21378333
MCF-7	Growth Inhibition Assay	100 nM	72/96 h		causes cell cycle arrest	21299862
MMQ	Growth Inhibition Assay	0.008-625 nM	72 h		inhibits cell growth in both time- and dose-dependent manner	20700755
MMQ	Function Assay	0.008-625 nM	72 h		inhibits PRL secretion in a dose-dependent manner	20700755
MMQ	Function Assay	0.04-625 nM	72 h		inhibits ERα expression	20700755
MMQ	Function Assay	0.04-625 nM	72 h		upregulates TGFβ3 and TGFβRII expression	20700755
MCF7	Function assay		6 days		Induction of ERalpha degradation in human MCF7 cells assessed as inhibition of insulin-mediated cell proliferation after 6 days by Hoechst 33258 dye-based assay, IC50 = 0.00006 μM.	28296398
MCF7	Function assay				Antagonist activity at ERalpha receptor in human MCF7 cells, IC50 = 0.0000631 μM.	26407012
MCF7	Function assay		4 hrs		Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal dextran-treated FBS incubated for 4 hrs by SP1 and anti-ER rabbit monocolnal antibody based in-cell Western assay, Activity = 0.0001 μM.	30086626
MCF7	Function assay		24 hrs		Proteolysis targeting chimera activity in human MCF7 cells assessed as induction of E3 ubiquitin ligase-mediated ERalpha degradation by proteasome after 24 hrs by in-cell Western assay, IC50 = 0.0001 μM.	30128071
MCF7	Function assay				Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor response, IC50 = 0.0002089 μM.	26407012
MCF7	Function assay		24 hrs		Downregulation of human ERalpha in human MCF-7 cells after 24 hrs by in-cell Western immunoassay method, IC50 = 0.0003 μM.	28657320
MCF7	Function assay		4 hrs		Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay, EC50 = 0.0004 μM.	25879485
MCF7	Function assay		4 hrs		Decrease in estrogen receptor alpha level in human MCF7 cells after 4 hrs by in-cell western assay, EC50 = 0.0004 μM.	26463130
MCF7	Function assay				Antagonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha, IC50 = 0.00047 μM.	10673099
MCF7	Function assay				Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells, IC50 = 0.00049 μM.	9154963
MCF7	Function assay		24 hrs		Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay, IC50 = 0.0006 μM.	25879485
MCF7	Function assay		18 to 24 hrs		Induction of ERalpha degradation in human MCF7 cells after 18 to 24 hrs by Western blot analysis, IC50 = 0.001 μM.	28296398
MCF7	Function assay		18 hrs		Induction of ERalpha degradation in human MCF7 cells after 18 hrs by Western blot analysis, IC50 = 0.0012 μM.	28296398
MCF7	Function assay		18 to 24 hrs		Induction of selective estrogen receptor alpha degradation in human MCF7 cells after 18 to 24 hrs by in-cell Western analysis, IC50 = 0.0012 μM.	29562737
MCF7	Function assay		24 hrs		Antagonist activity at ERalpha in human MCF7 cells assessed as inhibition of estrogen-induced transcription preincubated overnight followed by estrogen addition measured after 24 hrs by dual luciferase reporter gene assay, IC50 = 0.0034 μM.	28296398
MCF7	Function assay		24 hrs		Induction of selective estrogen receptor alpha degradation in human MCF7 cells harboring TK-ERE-Luc assessed as reduction in estradiol-induced transcriptional activity after 24 hrs by luciferase reporter gene assay, IC50 = 0.0034 μM.	29562737
COS7	Function assay				Antagonist activity at estrogen receptor beta ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay, IC50 = 0.0038 μM.	19863083
MCF7	Function assay		24 hrs		Induction of selective estrogen receptor alpha degradation in human MCF7 cells harboring TK-ERE-Luc assessed as reduction in estradiol-induced GREB1 mRNA expression after 24 hrs by TaqMan assay, IC50 = 0.0038 μM.	29562737
COS7	Function assay				Antagonist activity at estrogen receptor alpha ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay, IC50 = 0.004 μM.	19863083
Rosetta 2 DE3 competent cell	Function assay		1 hr		Displacement of [3H]-estradiol from recombinant human N-terminal His-tagged ERalpha LBD harboring C381S/C417S/C530S mutant expressed in Rosetta 2 DE3 competent cells after 1 hr by SPA binding assay, IC50 = 0.0084 μM.	28296398
HepG2	Function assay		16 hrs		Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay, EC50 = 1.95 μM.	23688559
MCF7	Function assay	10 uM	3 days		Inhibition of increase in proliferation of estrogen receptor expressing MCF7 cells at 10 uM after 3 days	17275315
MVLN	Function assay		24 hrs		Activity at ER assessed as suppression of estrogen response element-driven gene transactivation in MVLN cells after 24 hrs by luciferase reporter gene assay	17275315
T47D	Function assay	5 uM			Agonist activity at human ERalpha in T47D cells assessed as enhancement of AP1-driven transactivation at 5 uM by luciferase reporter assay relative to DMSO	17337183
MCF7	Function assay		45 mins		Binding affinity to estrogen receptor alpha in human MCF7 cells assessed as inhibition of [3H]E2 accumulation after 45 mins by whole cell competition binding assay	19133777
MCF7	Function assay		24 hrs		Down regulation of estrogen receptor alpha expression in human MCF7 cells after 24 hrs by Western blot analysis	19133777
MCF7	Function assay	100 nM	24 hrs		Down regulation of estrogen receptor alpha expression in human MCF7 cells at 100 nM after 24 hrs by immunofluorescence staining	19133777
MCF7:D5L	Function assay	1 uM			Antagonist activity at ERalpha in human MCF7:D5L cells assessed as inhibition of ERE-dependent luciferase expression at 1 uM	19845386
HEK293	Function assay	1 uM			Antagonist activity at ERbeta in HEK293 cells assessed as inhibition of ERE-dependent luciferase expression at 1 uM	19845386
Ishikawa	Function assay	1 uM			Antagonist activity at estrogen receptor in human Ishikawa cells assessed as inhibition of ERE-dependent alkaline phosphatase levels at 1 uM	19845386
HeLa	Function assay	1 uM	48 hrs		Antagonist activity at human ERalpha expressed in human HeLa cells coexpressing ERE-E1b-Luc assessed as inhibition of estradiol-induced transcriptional activation at 1 uM after 48 hrs by luciferase reporter gene assay	20621492
HeLa	Function assay	100 nM	20 to 24 hrs		Antagonist activity at LBD of ERalpha receptor in human HeLa cells assessed as blockade of SRC-1 binding to receptor at 100 nM after 20 to 24 hrs by luciferase reporter gene assay	23448346
MCF7	Function assay	10 nM	72 hrs		Inhibition of 17beta-estradiol-induced in ERalpha positive human MCF7 cells proliferation assessed as [3H]-thymidine incorporation at 10 nM after 72 hrs by liquid scintillation counting	24908652
MCF7	Function assay	1 uM	20 hrs		Induction of estrogen receptor-alpha degradation in human MCF7 cells at 1 uM after 20 hrs by Western blot analysis	25879485
MCF7	Function assay	0.01 to 300 nM	48 hrs		Degradation activity of ERalpha receptor in human MCF7 cells at 0.01 to 300 nM after 48 hrs by Western blot analysis	26407012
Neuro2a	Function assay	1 uM			Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis	26789657
MCF-7	Function assay	3 nM, 30 nM, 300 nM, 3 uM	24 hrs		Downregulation of ERalpha in human MCF-7 cells assessed as reduction of estradiol-induced GREB1 mRNA levels at 3 x 10'-9 M, 3 x 10'-8 M, 3 x 10'-7 M, 3 x 10'-6 M after 24 hrs by RT-PCR method	28657320
MCF-7	Function assay	3 nM, 30 nM, 300 nM, 3 uM	24 hrs		Downregulation of ERalpha in human MCF-7 cells assessed as reduction of estradiol-induced PgR mRNA levels at 3 x 10'-9 M, 3 x 10'-8 M, 3 x 10'-7 M, 3 x 10'-6 M after 24 hrs by RT-PCR method	28657320
MCF-7	Function assay	3 nM, 30 nM, 300 nM, 3 uM	24 hrs		Downregulation of ERalpha in human MCF-7 cells assessed as reduction of estradiol-induced pS2 mRNA levels at 3 x 10'-9 M, 3 x 10'-8 M, 3 x 10'-7 M, 3 x 10'-6 M after 24 hrs by RT-PCR method	28657320
MCF7	Function assay	10 uM	24 hrs		Induction of selective estrogen receptor alpha degradation in human MCF7 cells at 10 uM after 24 hrs by Western blot analysis	29562737
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Informazioni chimiche, conservazione e stabilità

Peso molecolare	606.77	Formula	C₃₂H₄₇F₅O₃S	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	129453-61-8	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	ICI-182780, ZD 9238, ZM 182780			Smiles	CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F

Solubilità

In vitro
Lotto:

DMSO : 100 mg/mL (164.8 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 100 mg/mL

Water : 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.
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.	1.250mg/ml (2.06mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 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.
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	2%DMSO 1 30%PEG300 2 2%Tween80 3 66%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	0.400mg/ml (0.66mM)	Taking the 1 mL working solution as an example, add 20 μL of clarified DMSO stock solution of 20 mg/ml to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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.

Calcolatore di formulazione in vivo (Soluzione chiara)

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

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 cè 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, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Targets/IC₅₀/Ki	ER (Cell-free assay) 0.94 nM
In vitro	Il Fulvestrant è un efficace inibitore della crescita delle cellule MCF-7 ER-positive (con IC50 di 0,29 nM) ma senza effetti sulla crescita delle cellule di cancro al seno umane BT-20 ER-negative. Questo composto provoca l'accumulo di cellule in G0/G1 e riduce anche la proporzione di cellule capaci di sintesi continua del DNA. Inibisce competitivamente il legame dell'estradiolo al recettore degli estrogeni. Questo agente blocca la localizzazione nucleare dell'ER compromettendo la dimerizzazione del recettore e il trasporto nucleo-citoplasmatico energia-dipendente. A causa dell'instabilità del complesso fulvestrant-ER, il legame di questo composto con l'ER porta infine a una degradazione accelerata della proteina ER. Questa sostanza chimica (10 nM) non solo diminuisce i livelli di mRNA di IGF-IR ma diminuisce anche l'emivita. Il trattamento con 100 μM di questo composto porta a un aumento dipendente dal tempo dei livelli di mRNA a stato stazionario di TNFR1 e TRADD nelle cellule MCF-7. È in grado di down-regolare l'espressione del recettore degli androgeni e diminuisce le risposte androgeniche nelle cellule di cancro alla prostata umane LNCaP. Questo agente attenua anche significativamente la crescita stimolata da R1881 del 70%. È in grado di modulare la mitosi e la morte cellulare nei neuroni cerebellari immaturi tramite rapida attivazione di MAPK.
In vivo	Il Fulvestrant è privo di attività uterotrofica e, quando co-somministrato con estradiolo, blocca efficacemente l'azione uterotrofica dell'estradiolo con ED50 di 0,06 mg/kg/giorno s.c. in ratti femmine immature. Una singola iniezione s.c. di 5 mg di questa sospensione del composto blocca completamente la crescita degli xenotrapianti MCF-7. La crescita dei trapianti del tumore mammario umano BrlO è anche efficacemente soppressa da 10 μM di questa sostanza chimica. Questo composto (10 mg/ratto, s.c.) riduce l'espressione del recettore degli androgeni, la fosforilazione di ERK1/2 e la proliferazione cellulare nella prostata ventrale del ratto. Mostra anche attività anti-angiogenesi nella membrana corioallantoidea dell'uovo di pulcino.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/1855205/ [2] https://pubmed.ncbi.nlm.nih.gov/15094757/ [3] https://pubmed.ncbi.nlm.nih.gov/9816164/ [4] https://pubmed.ncbi.nlm.nih.gov/11110059/ [5] https://pubmed.ncbi.nlm.nih.gov/16818513/ [6] https://pubmed.ncbi.nlm.nih.gov/12832521/ [7] https://pubmed.ncbi.nlm.nih.gov/20874728/ [8] https://pubmed.ncbi.nlm.nih.gov/7678775/

Applicazioni

Metodi	Biomarcatori	PMID
Western blot	ERα ErbB3 p-ErbB3 Y1289 / ErbB3 / p-ErbB4 Y1056 / ErbB4 / p-AKT / AKT / p-ERK / ERK MDM2 / ER	19815064
Immunofluorescence	Snail / E-cadherin IGF-1R / Erα	23936773
Growth inhibition assay	Cell viability	29787591

Informazioni sullo studio clinico

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

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT06239467	Recruiting	Advanced Cancer\|Breast Cancer	OnKure Inc.	March 1 2024	Phase 1
NCT06257264	Recruiting	Breast Cancer\|Small Cell Lung Cancer\|Ovarian Cancer\|Gastric Cancer\|Hormone-receptor-positive Breast Cancer\|Hormone Receptor Positive HER-2 Negative Breast Cancer\|Advanced Solid Tumor\|Endometrial Cancer\|Prostate Cancer	BeiGene	February 28 2024	Phase 1
NCT05905341	Withdrawn	Breast Cancer\|Ovarian Cancer\|Liposarcoma\|Non-small Cell Lung Cancer (NSCLC)\|Endometrial\|Solid Tumors	Pfizer	January 15 2024	Phase 1
NCT05963984	Recruiting	Metastatic Breast Cancer\|Locally Advanced Breast Cancer\|Breast Cancer	Carrick Therapeutics Limited\|Pfizer	December 14 2023	Phase 2
NCT06129786	Recruiting	Breast Cancer	Centro di Riferimento Oncologico - Aviano	May 18 2023	--

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Domande Frequenti

Domanda 1:
Is there any information for the half-life of it (Cat No.S1191)?

Risposta:
Its half life, S1191, is about 13.5 to 18.5 hours in vivo: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2750771/. The half life of this compound in cell culture might be different and we generally recommend replenishing with fresh drug every 24-48 hours.

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