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Fulvestrant

別名：ICI-182780, ZD 9238, ZM 182780

フルベストラント (Fulvestrant (ICI-182780, ZD 9238, ZM 182780)) はエストロゲン受容体 (estrogen receptor, ER) アンタゴニストであり、cell-free assay における IC50 は 0.94 nM です。フルベストラントはまたオートファジー (autophagy) とアポトーシス (apoptosis) を誘導し、抗腫瘍活性を呈します。

Fulvestrant化学構造

CAS No. 129453-61-8

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 56500 国内在庫あり
JPY 131500 国内在庫あり
JPY 205500 国内在庫あり

代表番号: 045-509-1970|電子メール：[email protected]
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製品安全説明書

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Fulvestrant関連製品

シグナル伝達経路

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptorシグナル伝達経路

Estrogen/progestogen Receptor阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
A549  Growth Inhibition Assay 5 μM 72 h inhibits cell growth significantly combined with vandetanib 22258476
201T Growth Inhibition Assay 5 μM 72 h inhibits cell growth significantly combined with vandetanib 22258476
Huh7 Function Assay 50 μM 48 h inhibits genistein-mediated PON1 transactivation 22304296
JEG-3 Function Assay 1 μM 1-48 h down-regulates the expression of IGFBP7 mRNA 22383111
HTR-8 Function Assay 1 μM 1-48 h down-regulates the expression of IGFBP7 mRNA 22383111
H1975 Function Assay 3 μM 7 d induces EGFR expression 22560634
H1975 Function Assay 3 μM 3 h abrogates the phospho-EGFR induction by estrogen 22560634
H1975 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
PC-9 Growth Inhibition Assay 0.003-30 μM 48 h inhibits cell growth in a dose-dependent manner 22560634
BG1L-ICILT Function Assay 10 nM 24 h  inhibits ERα expression 22652558
BG1L-OHTLT  Function Assay 10 nM 24 h  inhibits ERα expression 22652558
COS-7  Function Assay 100 nM 1 h takes on a punctate staining pattern 22869106
HeLa Function Assay 100 nM 1 h takes on a punctate staining pattern 22869106
MCF-7 Function Assay 100 nM 1 h takes on a punctate staining pattern 22869106
1471.1 Function Assay 100 nM 1 h takes on a punctate staining pattern 22869106
MCF-7 Growth Inhibition Assay 100 nM 5 d inhibits the stimulation of fusarielin H 22982765
MCF-7 Growth Inhibition Assay 100 nM/1 μM 5 d inhibits the stimulation of 17β-estradiol 22982765
MCF7 Growth Inhibition Assay 100 nM 48 h enhances nutlin-mediated cell death 23077249
MCF7 Growth Inhibition Assay 100 nM 48 h leads to a similar loss in survival as with doxorubicin alone 23077249
TG1-1  Function Assay 1 μM 24 h abrogates E2 induced accumulation of PI3K 23088607
TG1-1  Function Assay 1 μM 24 h abrogates E2 induced accumulation of HIF-1α 23088607
MCF-7 Growth Inhibition Assay 100 nM 48 h abrogates the proliferative effect of moderate nitrosative stress 23216744
MLO-Y4  Function Assay 1 μM 1 h inhibits E2-induced Cx43 expression 23247057
MCF-7  Growth Inhibition Assay 100 nM 4 d induces a higher proportion of cells in the G1 phase  23313506
MCF-7  Growth Inhibition Assay 10/100/1000 nM 2/4/6 d inhibits cell growth in both dose- and time- dependent manner 23313506
H1975  Apoptosis Assay 200 nM 72 h enhances erlotinib induced apoptosis 23399957
H1975  Growth Inhibition Assay 0.3125-10 μM 6 d inhibits cell growth in a dose-dependent manner 23399957
MMQ  Function Assay 0-625 nM 72 h down-regulates the expression of estrogen receptor-α (ERα) 23523357
MCF-7L Function Assay 100 nM  24 h induces EGFR phosphorylation required HB-EGF function 23686416
C4-12  Function Assay 100 nM  48 h induces EGFR family member activation required ER 23686416
MCF-7L Function Assay 100 nM  48 h induces EGFR family member activation required ER 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  10 min/24 h/48 h results in EGFR, HER2 and HER3 phosphorylation at prolonged exposure 23686416
HepG2  Function Assay 0.01-10 μM 18 h  activates the ERE-mediated transcription of AF2ER 23733188
MCF-7-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
BT474-tet-shMED1 Growth Inhibition Assay 0.1-5 μM 7 d increases +Dox induced cell death in a dose-dependent manner 23936234
MCF-7  Function Assay 100 nM  24/48 h facilitates invasion through MMPs' modulation 23936773
MCF-7  Function Assay 100 nM  72 h reverses the protective effect of E2 in cell invasion 23936773
H1975 Function Assay 3 μM 1 m upregulates the level of Let-7c 24268810
H1975  Growth Inhibition Assay 3 μM 1 m increases the gefitinib sensitivity of H1975 cells  24268810
MCF-7  Function Assay 10 nM  72 h reverses the estrogen effect(IC50 1.9 × 10−9 M) 24908652
Mesangial Function Assay 0.1-100 nM 0.5 h inhibits TGF-β1-induced Smad2 phosphorylation via GPER 24793639
mesangial  Function Assay 0.1-100 nM 48 h suppresses TGF-β1-induced type IV collagen 24793639
MCF-7  Growth Inhibition Assay 100 nM 5 d inhibits cell growth to 10％ 24819550
LCC9 Function Assay 100 nM 48-144 h activates UPR signaling 24858277
LCC1 Function Assay 100 nM 48-144 h activates UPR signaling 24858277
HCC1428/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
MCF-7/LTED Growth Inhibition Assay 1.3-1000 nM 48 h inhibits cell growth in a dose-dependent manner 24979294
MCF-7 Growth Inhibition Assay 1.3-1000 nM 48 h inhibits cell growth in a dose-dependent manner 24979294
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 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 10 uM 3 days Inhibition of increase in proliferation of estrogen receptor expressing MCF7 cells at 10 uM after 3 days 17275315
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
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
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
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: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
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 6 h attenuates the fludioxonil- or fenhexamid-induced increase in miR-21 expression 23052036
ER+ MCF-7 Growth Inhibition Assay 200 h IC50=0.21 nM 15324884
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 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 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 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
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
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
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
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
MCF-7  Growth Inhibition Assay IC50 of approximately 2 nM 23448346
ER+ MCF-7/2a Growth Inhibition Assay IC50=0.004 μM 15324884
MCF7 Function assay Antagonist activity at ERalpha receptor in human MCF7 cells, IC50 = 0.0000631 μM. 26407012
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 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
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
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
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生物活性

製品説明 フルベストラント (Fulvestrant (ICI-182780, ZD 9238, ZM 182780)) はエストロゲン受容体 (estrogen receptor, ER) アンタゴニストであり、cell-free assay における IC50 は 0.94 nM です。フルベストラントはまたオートファジー (autophagy) とアポトーシス (apoptosis) を誘導し、抗腫瘍活性を呈します。
Targets
ER [1]
(Cell-free assay)
0.94 nM
In Vitro
In vitro Fulvestrant is an effective inhibitor of the growth of ER-positive MCF-7 (with IC50 of 0.29 nM) but with no effect on the growth of ER-negative BT-20 human breast cancer cells. Fulvestrant causes accumulation of cells in G0/G1 and also reduces the proportion of cells capable of continued DNA synthesis. [1] Fulvestrant competitively inhibits binding of oestradiol to the estrogen receptor. Fulvestrant blocks nuclear localization of the ER through impairing receptor dimerisation, and energy-dependent nucleo-cytoplasmic shuttling. Because of the instability of fulvestrant-ER complex, the binding of Fulvestrant with ER finally results in accelerated degradation of the ER protein. [2] Fulvestrant (10 nM) not only decreases IGF-IR mRNA levels but also decreases the half-life. [3] Treatment with 100 μM Fulvestrant leads to a time dependent increase of TNFR1 and TRADD steady-state mRNA levels in MCF-7 cells. [4] Fulvestrant is capable of down-regulating androgen receptor expression and diminishes androgenic responses in LNCaP human prostate cancer cells. Fulvestrant also significantly attenuates R1881-stimulated growth by 70%. [5] Fulvestrant is able to modulate mitosis and cell death in immature cerebellar neurons via rapid activation of MAPK. [6]
細胞実験 細胞株 MCF-7 breast cancer cells
濃度 2.9 nM
反応時間 5 days
実験の流れ MCF-7 cells are cultured in multiwell plates (24-well, seeding density 4 × 104) in minimal essential medium containing phenol red, insulin (10 μg/mL), and 5% charcoal-stripped fetal calf serum without additional estradiol. Fulvestrant and/or estradiol are added in fresh medium 2 days after seeding. Cultures are maintained for 5 days with one further medium change and growth is assessed by measurement of total cell protein at the beginning and end of treatment and compared with that of controls treated with ethanol (0.1%) alone.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot MDM2 / ER p-ErbB3 Y1289 / ErbB3 / p-ErbB4 Y1056 / ErbB4 / p-AKT / AKT / p-ERK / ERK ErbB3 ERα 24747123
Immunofluorescence IGF-1R / Erα Snail / E-cadherin 19815064
Growth inhibition assay Cell viability 29787591
In Vivo
In Vivo Fulvestrant is devoid of uterotropic activity, and when co-administered with estradiol, it effectively blocks the uterotropic action of estradiol with ED50 of 0.06 mg/kg/day s.c. in immature female rats. A single s.c. injection of 5 mg of Fulvestrant suspension blocks completely the growth of MCF-7 xenografts. The growth of transplants of the BrlO human breast tumor is also suppressed effectively by 10 μM Fulvestrant. [1] Fulvestrant (10 mg/rat, s.c.) reduces the androgen receptor expression, ERK1/2 phosphorylation and cell proliferation in the rat ventral prostate. [7] Fulvestrant also displays anti-angiogenesis in the chick egg chorioallantoic membrane. [8]
動物実験 動物モデル The human breast cancer xenografts MCF-7 in nude mice
投与量 5 mg/mouse
投与経路 s.c. injection
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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 --

化学情報

分子量 606.77 化学式

C32H47F5O3S
CAS No. 129453-61-8 SDF Download Fulvestrant SDFをダウンロードする
Smiles CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (164.8 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 100 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

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よくある質問（FAQ）

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

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

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