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Genistein EGFR remmer

Name: Genistein
Brand: Selleck Chemicals
SKU: S1342
Rating: 5 (35 reviews)

Cat.nr.S1342

Genistein, een fyto-oestrogeen dat voorkomt in sojaproducten, is een zeer specifieke remmer van protein tyrosine kinase (PTK) die het mitogene effect, gemedieerd door EGF op NIH-3T3 cellen, blokkeert met een IC50 van 12μM.

Genistein EGFR remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 270.24

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Kwaliteitscontrole

Batch: Zuiverheid: 99.88%

99.88

Gerelateerde doelwitten	VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Overig EGFR Inhibitoren	Lazertinib (YH25448) Icotinib Hydrochloride Sunvozertinib AG-490 AG-1478 Canertinib (CI-1033) WZ4002 Rociletinib (CO-1686) Poziotinib (NOV120101, HM781-36B) Allitinib tosylate

Celkweek, behandeling & werkzame concentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
BxPC3	Proliferation assay			Antiproliferative activity against human BxPC3 cell line by MTT assay, IC50=30 μM	16789737
BT20	Proliferation assay			Antiproliferative activity against human BT20 cell line by MTT assay, IC50=46 μM	16789737
ANN-1	Cytotoxic assay			Cytotoxic effect on v-abl transformed murine ANN-1 cells, IC50=8μM	8201603
breast carcinoma cells	Cytotoxic assay			Cytotoxic effect on MCF-7 human breast carcinoma cells, IC50=15.1μM	8201603
3T3	Cytotoxic assay			Cytotoxic effect on 3T3 cells, IC50=24μM	8201603
colon cells	Cytotoxic assay			Cytotoxic effect on WiDr human colon cells, IC50=27.7μM	8201603
Hepa1clc7	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse Hepa1clc7 cells after 72 hrs, IC50=11μM	10075742
MCF7	Function assay		6 hrs	Inhibition of phorbol ester-induced ornithine decarboxylase in human MCF7 cells after 6 hrs, IC50=26μM	10075742
3T3/A31	Cytotoxicity assay	1 to 100 ug/mL	72 hrs	Cytotoxicity against BALB/c mouse cloned 3T3/A31 cells at 1 to 100 ug/mL after 72 hrs by nigrosin assay	10096863
SH-SY5Y	Function assay			Agonist activity in transcriptional activation assay in SH-SY5Y neuroblastoma cells expressing Estrogen receptor beta, EC50=0.0017μM	11906280
HeLa	Function assay			Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor beta., EC50=0.0041μM	11906280
HeLa	Function assay			Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor alpha., EC50=0.048μM	11906280
Ishikawa	Estrogenic assay		4 days	Estrogenic activity in human Ishikawa cells assessed as induction of alkaline phosphatase activity after 4 days by para-nitrophenol release assay, IC50=0.51μM	12502307
Hepa-1c1c7	Function assay			Induction of NADPH:quinone reductase in mouse Hepa-1c1c7 cells assessed as drug level required to double enzyme activity by MTT assay, CD=22.9μM	14510590
Hepa-1c1c7	Function assay			Inhibition of mouse Hepa-1c1c7 cells by MTT assay, IC50=45.2μM	14510590
T47D	Estrogenic assay			Estrogenic activity in human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol by alamar blue assay, Activity=0.001μM	15787436
MCF7	Estrogenic assay			Estrogenic activity in human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol by alamar blue assay, Activity=0.003μM	15787436
T47D	Estrogenic assay			Estrogenic activity in human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 100 pM estradiol by alamar blue assay, Activity=0.009μM	15787436
MCF7	Estrogenic assay			Estrogenic activity in human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 100 pM estradiol by alamar blue assay, Activity=0.013μM	15787436
293T	Function assay			Displacement of [3H]17beta-estradiol from recombinant human ERbeta expressed in 293T cells, IC50=0.0013μM	16219463
293T	Function assay			Displacement of [3H]17beta-estradiol from recombinant human ERalpha expressed in 293T cells, IC50=0.0294μM	16219463
Vero	Cytotoxicity assay			Cytotoxicity against african green monkey Vero cells, IC50=32.9μM	16441066
U937	Antiproliferative assay		72 hrs	Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay, IC50=48μM	17158054
RAW 264	Function assay		24 hrs	Inhibition of 1 ug/ml LPS-stimulated TNFalpha accumulation in RAW 264 cells after 24 hrs, IC50=18.1μM	17320246
K562	Growth inhibition assay		5 days	Growth inhibition of K562 cells by XTT assay after 5 days, IC50=17.56μM	17411092
HUVE12	Function assay			Reversal of hydrogen peroxide-induced LDH activity in human HUVE12 cells	18068980
HL60	Antileukemic assay		24 hrs	Antileukemic activity against human HL60 cells after 24 hrs by clonogenic assay, LC50=6.3μM	18163589
L1210	Antileukemic assay		24 hrs	Antileukemic activity against mouse L1210 cells after 24 hrs by clonogenic assay, LC50=6.5μM	18163589
MOLT3	Antileukemic assay		24 hrs	Antileukemic activity against human MOLT3 cells after 24 hrs by clonogenic assay, LC50=7.5μM	18163589
MOLT3	Growth inhibition assay		48 hrs	Growth inhibition of human MOLT3 cells after 48 hrs, IG50=12.7μM	18163589
Raji	Antileukemic assay		24 hrs	Antileukemic activity against human Raji cells after 24 hrs by clonogenic assay, LC50=13.7μM	18163589
HL60	Growth inhibition assay		48 hrs	Growth inhibition of human HL60 cells after 48 hrs, IG50=18.2μM	18163589
L1210	Growth inhibition assay		24 hrs	Growth inhibition of mouse L1210 cells after 24 hrs, IG50=18.5μM	18163589
Raji	Growth inhibition assay		48 hrs	Growth inhibition of human Raji cells after 48 hrs, IG50=18.6μM	18163589
KG1a	Growth inhibition assay		48 hrs	Growth inhibition of human KG1a cells after 48 hrs, IG50=23μM	18163589
L1210	Function assay	1 to 20 uM	24 hrs	Induction of p15CDKN2B re-expression in mouse L1210 cells at 1 to 20 uM after 24 hrs by RT-PCR	18163589
HEK293	Function assay			Antagonist activity at human recombinant LXRbeta expressed in HEK293 cells by luciferase reporter gene assay, IC50=22μM	18343126
HEK293	Function assay			Antagonist activity at human recombinant LXRalpha expressed in HEK293 cells by luciferase reporter gene assay, IC50=31μM	18343126
NIH3T3	Function assay			Agonist activity at CFTR-deltaF508 mutant expressed in NIH3T3 cells assessed as increase in forskolin-stimulated current, EC50=4.4μM	18595696
NHEM	Function assay		72 hrs	Inhibition of melanin synthesis in NHEM cells assessed as [14C]thiouracil incorporation after 72 hrs by liquid scintillation counting, IC50=29.2μM	19132934
RAW264.7	Function assay			Inhibition of LPS-induced TNFalpha release in mouse RAW264.7 cells pretreated 1 hr before LPS challenge by enzyme immunoassay, IC50=26.5μM	19278854
MDA-kb2	Function assay			Agonist activity at androgen receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150=4.4μM	19592245
MDA-kb2	Function assay			Agonist activity at glucocorticoid receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150=4.4μM	19592245
MCF7	Antiproliferative assay			Antiproliferative activity against estrogen receptor expressing human MCF7 cells, GI50=10μM	19818612
MDA-MB-436	Antiproliferative assay			Antiproliferative activity against estrogen receptor expressing human MDA-MB-436 cells, GI50=17μM	19818612
FRT	Function assay			Binding affinity to CFTR deltaF508 mutant expressed in FRT cells coexpressing halide sensitive YFP-H148Q/I152L mutant protein by iodide influx assay, Kd=16.7μM	19880323
T47D	Estrogenic assay		96 hrs	Estrogenic activity in human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol after 96 hrs by alamar blue assay, Activity=0.01μM	19928832
MCF7	Estrogenic assay		96 hrs	Estrogenic activity in human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol after 96 hrs by alamar blue assay, Activity=0.01μM	19928832
MCF7	Estrogenic assay			Estrogenic activity in luciferase transfected human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol by luciferase reporter gene assay, Activity=0.01μM	19928832
MCF7	Estrogenic assay			Estrogenic activity in luciferase transfected human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 100 pM estradiol by luciferase reporter gene assay, Activity=0.01μM	19928832
T47D	Estrogenic assay			Estrogenic activity in luciferase transfected human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol by luciferase reporter gene assay, Activity=0.01μM	19928832
T47D	Estrogenic assay		96 hrs	Estrogenic activity in human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 100 pM estradiol after 96 hrs by alamar blue assay, Activity=0.08μM	19928832
MCF7	Estrogenic assay		96 hrs	Estrogenic activity in human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 100 pM estradiol after 96 hrs by alamar blue assay, Activity=0.11μM	19928832
T47D	Estrogenic assay			Estrogenic activity in luciferase transfected human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 100 pM estradiol by luciferase reporter gene assay, Activity=0.6μM	19928832
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production after 24 hrs by Griess reagent, IC50=26μM	20363145
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=1μM	20813524
LoVo	Cytotoxicity assay		72 hrs	Cytotoxicity against human LoVo cells after 72 hrs by MTT assay, IC50=15.88μM	21129977
LNCAP	Cytotoxicity assay		72 hrs	Cytotoxicity against human LNCAP cells after 72 hrs by SRB assay, IC50=30.65μM	21129977
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=34.9μM	21129977
AGS	Cytotoxicity assay		72 hrs	Cytotoxicity against human AGS cells after 72 hrs by MTT assay, IC50=41.67μM	21129977
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by SRB assay, IC50=43.09μM	21129977
DU145	Cytotoxicity assay		72 hrs	Cytotoxicity against human DU145 cells after 72 hrs by MTT assay, IC50=47.29μM	21129977
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production treated 2 hrs before LPS challenge measured after 24 hrs by ELISA, IC50=19.1μM	21288727
MDCK	Function assay			Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=6.9μM	21354800
MCF-7 MX	Function assay			Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining, IC50=8.8μM	21354800
NCI-ADR-RES	Antiproliferative assay		48 hrs	Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=16.9824μM	21513275
MCF12A	Antiproliferative assay		48 hrs	Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=21.8776μM	21513275
NCI-ADR-RES	Antiproliferative assay		48 hrs	Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=26.9154μM	21513275
MCF12A	Antiproliferative assay		48 hrs	Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=30.1995μM	21513275
NCI-ADR-RES	Antiproliferative assay		48 hrs	Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50=32.3594μM	21513275
MCF12A	Antiproliferative assay		48 hrs	Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50=32.3594μM	21513275
LNCAP	Antiproliferative assay		48 hrs	Antiproliferative activity against human LNCAP cells expressing androgen receptor incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50=38.9045μM	21513275
PC3	Antiproliferative assay		48 hrs	Antiproliferative activity against androgen receptor-deficient human PC3 cells incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50=42.6579μM	21513275
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=45.7088μM	21513275
FRT	Function assay		24 hrs	Binding affinity to CFTR F508 deletion mutant expressed in forskolin-stimulated FRT cells assessed as increase in iodine influx measured as YFP quenching rate after 24 hrs by fluorescence assay, Kd=9.4μM	21568323
MCF7	Antiestrogenic assay	1 to 20 uM	48 hrs	Antiestrogenic activity in human ER-positive MCF7 cells assessed as inhibition of 17beta estradiol-induced secreted alkaline phosphatase activity at 1 to 20 uM after 48 hrs by phospha-light reporter chemiluminescence assay	21800859
Jurkat T	Apoptosis assay		36 hrs	Induction of apoptosis in human Jurkat T cells overexpressing Neo after 36 hrs by flow cytometry	22197393
FRT	Function assay			Potentiation activity at human CFTR delta F508 mutant-mediated iodine flux expressed in rat FRT cells coexpressing fluorescent protein YFP-H148Q/1152L by fluorescence assay, EC50=7μM	22281185
Human Huh7.5.1	Antiviral assay		72 hrs	Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay, EC50=14.4μM	22445328
CHO	Function assay			Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells, Ki=2.96μM	23571415
CHO	Function assay			pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells, IC50=3.89045μM	23571415
CHO	Function assay			Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells, Ki=5μM	23571415
CHO	Function assay			pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells, IC50=9.12011μM	23571415
HuH7	Antiplasmodial assay		24 hrs	Antiplasmodial activity against liver sporozoite stage of Plasmodium berghei ANKA expressing GFP infected in human HuH7 cells assessed as inhibition of parasite development after 24 hrs by qRT-PCR analysis, IC50=20μM	24125849
SKBR3	Cell cycle assay	50 to 75 uM	36 hrs	Cell cycle arrest in human SKBR3 cells assessed as decrease in accumulation at G0/G1 phase at 50 to 75 uM after 36 hrs by propidium iodide staining-based flow cytometric analysis	24456004
A431	Cell cycle assay	50 to 75 uM	36 hrs	Cell cycle arrest in human A431 cells assessed as decrease in accumulation at G0/G1 phase at 50 to 75 uM after 36 hrs by propidium iodide staining-based flow cytometric analysis	24456004
A431	Cell cycle assay	50 to 75 uM	36 hrs	Cell cycle arrest in human A431 cells assessed as accumulation at G2/M phase at 50 to 75 uM after 36 hrs by propidium iodide staining-based flow cytometric analysis relative to control	24456004
A431	Apoptosis assay	50 to 75 uM	72 hrs	Induction of apoptosis in human A431 cells overexpressing ErbB in complete medium assessed as late apoptotic/necrotic cells at 50 to 75 uM after 72 hrs by annexin V-FITC/7-AAD staining-based flow cytometric analysis	24456004
MCF7	Growth inhibition assay	0.1 to 20 uM	4 days	Stimulation of growth in human MCF7 cells at 0.1 to 20 uM after 4 days by MTT assay	25078314
MCF7	Growth inhibition assay	20 to 100 uM	4 days	Growth inhibition in human MCF7 cells at 20 to 100 uM after 4 days by MTT assay	25078314
RAW264.7	Function assay	26 uM		Inhibition of nitric oxide production in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as nitrites level at 26 uM by Griess method (Rvb = 6.4 +/- 0.5 uM), Activity=6.1μM	25127153
RAW264.7	Function assay	6.5 uM		Inhibition of nitric oxide production in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as nitrites level at 6.5 uM by Griess method (Rvb = 6.4 +/- 0.5 uM), Activity=6.3μM	25127153
RAW264.7	Function assay	13 uM		Inhibition of nitric oxide production in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as nitrites level at 13 uM by Griess method (Rvb = 6.4 +/- 0.5 uM), Activity=6.3μM	25127153
J774A1	Function assay	6.5 uM		Inhibition of nitric oxide production in LPS/IFNgamma-stimulated mouse J774A1 cells assessed as nitrites level at 6.5 uM by Griess method (Rvb = 16.5 +/- 1.4 uM), Activity=13.4μM	25127153
J774A1	Function assay	13 uM		Inhibition of nitric oxide production in LPS/IFNgamma-stimulated mouse J774A1 cells assessed as nitrites level at 13 uM by Griess method (Rvb = 16.5 +/- 1.4 uM), Activity=13.8μM	25127153
J774A1	Function assay	26 uM		Inhibition of nitric oxide production in LPS/IFNgamma-stimulated mouse J774A1 cells assessed as nitrites level at 26 uM by Griess method (Rvb = 16.5 +/- 1.4 uM), Activity=14.5μM	25127153
HEK293	Function assay			Inhibition of EGFR (unknown origin) expressed in HEK293 cells assessed as decrease in phosphorylation by chemiluminescence assay, IC50=25.12μM	25205190
Sf9	Function assay			Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintil, IC50=30μM	25406944
LNCAP	Cytotoxicity assay		3 days	Cytotoxicity against human androgen-dependent LNCAP cells assessed as inhibition of cell viability after 3 days by WST-1 cell proliferation assay, IC50=37.4μM	26341135
insect cells	Function assay		10 mins	Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells preincubated for 10 mins followed by addition of kynuramine as substrate, IC50=3.9μM	27575476
insect cells	Function assay		10 mins	Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells preincubated for 10 mins followed by addition of benzylamine as substrate, IC50=4.1μM	27575476
insect cells	Function assay		40 mins	Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells assessed as decrease in arbitrary light units preincubated for 40 mins followed by addition of luciferin derivative substrate measured after 2 hrs by MAO-Glow assay, IC50=6.8μM	27575476
insect cells	Function assay		40 mins	Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells assessed as decrease in arbitrary light units preincubated for 40 mins followed by addition of luciferin derivative substrate measured after 2 hrs by MAO-Glow assay, IC50=9.7μM	27575476
RAW264.7	Antiosteoporotic assay		4 to 5 days	Antiosteoporotic activity in mouse RAW264.7 cells assessed as inhibition of RANKL-induced osteoclast differentiation after 4 to 5 days by TRAP assay, IC50=11.4μM	28169537
SK-MEL-2	Cytotoxicity assay		48 hrs	Cytotoxicity against human SK-MEL-2 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=36μM	28654265
MML1	Cytotoxicity assay		48 hrs	Cytotoxicity against human MML1 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=42μM	28654265
MDA-MB-231	Cytotoxicity assay		48 hrs	Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=43μM	28654265
LN229	Cytotoxicity assay		48 hrs	Cytotoxicity against human LN229 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=44μM	28654265
NCI-H460	Cytotoxicity assay		48 hrs	Cytotoxicity against human NCI-H460 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=47μM	28654265
T47D	Cytotoxicity assay		48 hrs	Cytotoxicity against human T47D cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=48μM	28654265
HepG2	Function assay		1 hr	Inhibition of IL-6-Induced STAT3 activation (unknown origin) expressed in human HepG2 cells expressing pSTAT3-luciferase pre-incubated for 1 hr before IL-6 stimulation for 6 hrs by luciferase reporter gene assay, IC50=24.8μM	29140705
UOCB1	Antiproliferative assay		72 hrs	Antiproliferative activity against human UOCB1 cells after 72 hrs by CelTiter-Glo assay, EC50=35.6958μM	29407975
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LNCAP	Antiproliferative assay			Antiproliferative activity against human LNCAP cells, IC50=10μM	29456113
LNCAP	Antiproliferative assay		72 hrs	Antiproliferative activity against human LNCAP cells after 72 hrs by MTS assay, IC50=24μM	29456113
LNCAP	Antiproliferative assay		72 hrs	Antiproliferative activity against human LNCAP cells after 72 hrs in presence of enzalutamide by MTS assay, IC50=31.7μM	29456113
LNCAP	Function assay	2.5 uM	24 hrs	Inhibition of HDAC6/HSP90 in human LNCAP cells assessed as downregulation of AR protein level at 2.5 uM after 24 hrs by Western blot method	29456113
BV2	Antiinflammatory assay			Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production, IC50=28.4μM	29482940
MDA-MB-231/beta41	Estrogenic assay		18 hrs	Estrogenic activity at ERbeta (unknown origin) expressed in human MDA-MB-231/beta41 cells after 18 hrs by renilla luciferase reporter gene assay, EC50=0.0024μM	29641206
Ishikawa	Estrogenic assay		96 hrs	Estrogenic activity at ERalpha in human Ishikawa cells assessed as induction of alkaline phosphatase activity using p-nitrophenol as substrate treated for 96 hrs followed by substrate addition by spectrophotometric method, EC50=0.24μM	29641206
HEK293	Function assay		48 hrs	Agonist activity at human ER-beta transfected in HEK293 cells after 48 hrs by luciferase reporter gene assay, EC50=0.01995μM	ChEMBL
HEK293	Function assay		48 hrs	Agonist activity at human ER-alpha transfected in HEK293 cells after 48 hrs by luciferase reporter gene assay, EC50=0.50119μM	ChEMBL
HT-29	Growth inhibition assay			Growth inhibition of Homo sapiens (human) HT-29 cells by MTT assay, GI=4.11μM	ChEMBL
HL60	Growth inhibition assay			Growth inhibition of Homo sapiens (human) HL60 cells by MTT assay, GI=4.82μM	ChEMBL
SGC7901	Growth inhibition assay			Growth inhibition of Homo sapiens (human) SGC7901 cells by MTT assay, GI=5.78μM	ChEMBL
HL60	Function assay			Competitive inhibition of GLUT1 in human HL60 cells assessed as reduction in 2-[1,2-3H]deoxy-D-glucose uptake measured for 30 secs by double reciprocal plot analysis, Ki=7μM	ChEMBL
CHO	Function assay			Competitive inhibition of GLUT1 (unknown origin) expressed in CHO cells assessed as reduction in 2-[1,2-3H]deoxy-D-glucose uptake measured for 30 secs by double reciprocal plot analysis, Ki=7μM	ChEMBL
3T3L1	Function assay			Inhibition of GLUT4 in mouse 3T3L1 cells assessed as reduction in insulin-stimulated 2-deoxy-D-[14C]glucose uptake, IC50=20μM	ChEMBL
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Chemische informatie, opslag en stabiliteit

Molecuulgewicht	270.24	Formule	C₁₅H₁₀O₅	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	446-72-0	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	NPI 031L			Smiles	C1=CC(=CC=C1C2=COC3=CC(=CC(=C3C2=O)O)O)O

Oplosbaarheid

In vitro
Batch:

DMSO : 54 mg/mL (199.82 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	2.700mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 54 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	0.340mg/ml (1.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 6.8 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.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	EGFR topo II
In vitro	Genistein is een ATP-competitieve remmer. Deze verbinding remt tyrosinefosforylering in geïsoleerde enzym- en receptorpreparaten en in hele cellen, inclusief bloedplaatjes, lymfocyten en een verscheidenheid aan gekweekte cellen. Het remt ook EGF-gestimuleerde fosforylering in gekweekte cellen, evenals de remming van Topo II (topoisomerase II). Deze chemische stof remt EGF-gestimuleerde tyrosinefosforylering in gekweekte A431 epidermoïde carcinoomcellen. De remming is competitief met ATP en niet-competitief met het substraat. Het blokkeert het mitogene effect gemedieerd door EGF en trombine op NIH-3T3 cellen. Deze verbinding fungeert ook als een agonist voor de GPR30-receptor en bindt aan PPARγ en oestrogeenreceptoren. Het bindt ook aan PPARγ, fungerend als een agonist voor deze receptor met een K_i van 5,7 μM.
In vivo	Genistein heeft chemopreventieve effecten op borst-, prostaat- en andere hormoonafhankelijke tumoren bij volwassen dieren. Deze verbinding in het dieet verminderde de incidentie van slecht gedifferentieerde prostaatadenocarcinomen op een dosisafhankelijke manier en downreguleerde androgeenreceptor, oestrogeenreceptor-alfa, epidermale groeifactorreceptor en extracellulaire signaal-gereguleerde kinase-1, maar niet de mRNA-expressies van oestrogeenreceptor-beta en transformerende groeifactor-alfa. Voedingsgenisteïne beschermt tegen borst- en prostaatkanker door specifieke geslachtssteroïdreceptoren en groeifactor-signaalroutes te reguleren. Deze chemische stof, gecombineerd met bestraling van prostaattumoren, veroorzaakt een grotere remming van de primaire tumorgroei en verhoogt de controle over spontane metastase naar para-aortale lymfeklieren, waardoor de overleving van muizen toeneemt. Paradoxaal genoeg verhoogt behandeling met deze verbinding alleen de metastase naar lymfeklieren.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/3106339/ [2] https://pubmed.ncbi.nlm.nih.gov/2153378/ [3] https://pubmed.ncbi.nlm.nih.gov/12421816/ [4] https://pubmed.ncbi.nlm.nih.gov/11880592/ [5] https://pubmed.ncbi.nlm.nih.gov/16808622/

Toepassingen

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	PPARγ / C/EBPα / αP2 p-ERK Foxo3 CIP2A / PARP / Cleaved PARP / Caspase-3 / Cleaved Caspase-3 p-AKT / AKT DNMT-1 / DNMT-3a / DNMT-3b		18384126
Immunofluorescence	ER-β / pS87 ER-β		25931004

Informatie over klinische proeven

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
NCT05073523	Completed	Healthy	Chalmers University of Technology	September 27 2021	Not Applicable
NCT04650555	Completed	Acute Radiation Syndrome	Humanetics Corporation\|United States Department of Defense\|Joint Warfighter Medical Research Program	December 8 2020	Phase 1
NCT01982578	Completed	Alzheimer''s Disease	Fundación para la Investigación del Hospital Clínico de Valencia\|University of Valencia	September 1 2017	Not Applicable
NCT02499861	Completed	Cancer	St. Justine''s Hospital	July 2015	Phase 1\|Phase 2
NCT01628471	Completed	Non Small Cell Lung Cancer	Uman Pharma\|DSM Nutritional Products Inc.\|MDEIE Ministry Québec Government\|INRS-Institut Armand Frappier Université du Québec	November 2012	Phase 1\|Phase 2

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

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