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Fulvestrant

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(xì)胞試驗(yàn)中IC50為0.094 nM。Fulvestrant還可誘導(dǎo)自噬和凋亡并具有抗腫瘤的活性。

Fulvestrant Chemical Structure

Fulvestrant Chemical Structure

CAS: 129453-61-8

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 647.01 現(xiàn)貨
25mg 567.34 現(xiàn)貨
100mg 2233.34 現(xiàn)貨
500mg 7289.1 現(xiàn)貨
1g 10401.3 現(xiàn)貨
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Fulvestrant相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
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

產(chǎn)品描述 Fulvestrant是一種Estrogen receptor（ER）拮抗劑， 無細(xì)胞試驗(yàn)中IC50為0.094 nM。Fulvestrant還可誘導(dǎo)自噬和凋亡并具有抗腫瘤的活性。
靶點(diǎn)
ER [1]
(Cell-free assay)
0.94 nM
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(duì)ER陰性的的 BT-20人類乳腺癌細(xì)胞的生長沒有作用效果。Fulvestrant 使細(xì)胞在 G0/G1 期累積，也降低了能持續(xù)進(jìn)行DNA合成的細(xì)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(yùn)，而阻斷ER的核定位。由于Fulvestrant-ER復(fù)合體的不穩(wěn)定性，F(xiàn)ulvestrant與ER的結(jié)合最終會(huì)導(dǎo)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(xì)胞，提高TNFR1 和TRADD 穩(wěn)態(tài)的mRNA水平，這種作用具有時(shí)間依賴性。[4] Fulvestrant 作用于LNCaP人類前列腺癌細(xì)胞，可以下調(diào)雄激素受體的表達(dá)，也減少雄激素的反應(yīng)。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(xì)胞死亡。[6]
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 MCF-7 乳腺癌細(xì)胞
濃度 2.9 nM
孵育時(shí)間 5 天
方法 MCF-7細(xì)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(jìn)一步改變培養(yǎng)基，通過在實(shí)驗(yàn)處理開始和結(jié)束測量全部細(xì)胞蛋白，且與只用乙醇(0.1%)處理的對(duì)照組進(jìn)行比較后，測評(píng)生長狀況。
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 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
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(dá)，ERK1/2磷酸化，和細(xì)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]
動(dòng)物實(shí)驗(yàn) 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 --

化學(xué)信息&溶解度

分子量 606.77 分子式

C32H47F5O3S
CAS號(hào) 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(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (164.8 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 100 mg/mL (164.8 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)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(qǐng)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(jìn)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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常見問題及建議解決方法

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.

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