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別名: ICI-182780, ZD 9238, ZM 182780 中文名稱:氟維司瓊,氟維司群
Fulvestrant是一種Estrogen receptor(ER)拮抗劑, 無細胞試驗中IC50為0.094 nM。Fulvestrant還可誘導自噬和凋亡并具有抗腫瘤的活性。
Fulvestrant Chemical Structure
CAS: 129453-61-8
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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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 | ||
點擊查看更多細胞系數(shù)據(jù) |
產(chǎn)品描述 | Fulvestrant是一種Estrogen receptor(ER)拮抗劑, 無細胞試驗中IC50為0.094 nM。Fulvestrant還可誘導自噬和凋亡并具有抗腫瘤的活性。 | ||
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靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | Fulvestrant 有效抑制ER陽性的MCF-7生長(IC50為 0.29 nM),而對ER陰性的的 BT-20人類乳腺癌細胞的生長沒有作用效果。Fulvestrant 使細胞在 G0/G1 期累積,也降低了能持續(xù)進行DNA合成的細胞比例。[1] Fulvestrant 競爭性地抑制雌二醇與雌激素受體結(jié)合。 Fulvestrant通過損害受體二聚化和能量依賴型核質(zhì)轉(zhuǎn)運,而阻斷ER的核定位。由于Fulvestrant-ER復合體的不穩(wěn)定性,F(xiàn)ulvestrant與ER的結(jié)合最終會導致 ER蛋白的加速退化。[2] Fulvestrant (10 nM) 不僅可降低IGF-IR mRNA水平,也降低半衰期。[3] 100 μM Fulvestrant 處理MCF-7細胞,提高TNFR1 和TRADD 穩(wěn)態(tài)的mRNA水平,這種作用具有時間依賴性。[4] Fulvestrant 作用于LNCaP人類前列腺癌細胞,可以下調(diào)雄激素受體的表達,也減少雄激素的反應。Fulvestrant也顯著降低R1881 刺激的生長,降低 70%。[5]Fulvestrant作用于未成熟的小腦神經(jīng)元,通過快速激活MAPK,可以調(diào)節(jié)有絲分裂和細胞死亡。[6] | |||
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細胞實驗 | 細胞系 | MCF-7 乳腺癌細胞 | ||
濃度 | 2.9 nM | |||
孵育時間 | 5 天 | |||
方法 | MCF-7細胞培養(yǎng)在多孔板中(24孔,按4 × 104密度為接種),孔中含基本必需培養(yǎng)基,培養(yǎng)基中包含酚紅,胰島素(10 μg/mL),和5%活性炭處理的胎牛血清,不含額外的雌二醇。接種2天后,在新鮮的培養(yǎng)基中加入Fulvestrant 和/或雌二醇。培養(yǎng)持續(xù)5天,且進一步改變培養(yǎng)基,通過在實驗處理開始和結(jié)束測量全部細胞蛋白,且與只用乙醇(0.1%)處理的對照組進行比較后,測評生長狀況。 | |||
實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
Western blot | MDM2 / ER p-ErbB3 Y1289 / ErbB3 / p-ErbB4 Y1056 / ErbB4 / p-AKT / AKT / p-ERK / ERK ErbB3 ERα |
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24747123 | |
Immunofluorescence | IGF-1R / Erα Snail / E-cadherin |
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19815064 | |
Growth inhibition assay | Cell viability |
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29787591 |
體內(nèi)研究(In Vivo) | ||
體內(nèi)研究活性 | Fulvestrant缺乏子宮活性,與雌二醇聯(lián)用皮下注射給藥未成熟的雌性大鼠,有效抑制雌二醇的子宮內(nèi)活性,ED50 為0.06 mg/kg/day。5 mg Fulvestrant懸浮液皮下注射到MCF-7移植瘤中,完全抑制腫瘤生長。10 μM Fulvestrant也有效抑制BrlO人類乳腺癌移植瘤的生長。[1] Fulvestrant (10 mg/rat) 皮下注射到大鼠前列腺腹側(cè),降低雄激素受體的表達,ERK1/2磷酸化,和細胞增殖。[7]Fulvestrant作用于雞胚絨毛尿囊膜還具有抗血管生成的作用效果。[8] | |
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動物實驗 | Animal Models | 攜帶人類乳腺癌移植瘤MCF-7的裸鼠 |
Dosages | 5 mg | |
Administration | 皮下注射 |
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 | -- |
分子量 | 606.77 | 分子式 | C32H47F5O3S |
CAS號 | 129453-61-8 | SDF | Download Fulvestrant SDF |
Smiles | CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 100 mg/mL ( (164.8 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Ethanol : 100 mg/mL (164.8 mM) Water : Insoluble |
摩爾濃度計算器 |
體內(nèi)溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 |
動物體內(nèi)配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結(jié)果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內(nèi)配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內(nèi)配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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問題 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.