Art. -Nr.: HY-16950

4-Hydroxytamoxifen

(Synonyms: (Z)-4-Hydroxytamoxifen; trans-4-Hydroxytamoxifen; (Z)-Afimoxifene)

59 Cited Publications

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Based on 59 publication(s) in Google Scholar

4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM). 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is also the active metabolic form of Tamoxifen (HY-13757A) in vivo and can be used to induce gene knockout in transgenic mice expressing CreER.

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Reinheit: 99.86%
CAS. Nr.: 68047-06-3
Formel: C₂₆H₂₉NO₂
Molecular Weight:387.52

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

4-Hydroxytamoxifen Chemical Structure

CAS. Nr.: 68047-06-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (59)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
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Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]

Estrogen receptor

3.3 nM (IC₅₀)

ERα

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	EC₅₀	10 μM Compound: OH-TAM	Antiproliferative activity against human prostate, androgen receptor positive DU145 cells after 24 hrs by MTT assay Antiproliferative activity against human prostate, androgen receptor positive DU145 cells after 24 hrs by MTT assay	[PMID: 25198997]
DU-145	IC₅₀	15.3 μM Compound: 4OHT	Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 33965842]
HEK293	IC₅₀	0.07 μM Compound: 4-OHT	Antagonist activity at luciferase-fused ERalpha in human HEK293 cells expressing eYFP assessed as reduction of E2-induced estrogenic activity after 2 hrs by BRET assay Antagonist activity at luciferase-fused ERalpha in human HEK293 cells expressing eYFP assessed as reduction of E2-induced estrogenic activity after 2 hrs by BRET assay	[PMID: 26613635]
HEK293	IC₅₀	0.79 nM Compound: 4-OHT	Antagonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as reduction in E2-induced ER-alpha-mediated transcriptional activity by luciferase reporter gene assay Antagonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as reduction in E2-induced ER-alpha-mediated transcriptional activity by luciferase reporter gene assay	[PMID: 30940565]
Ishikawa	EC₅₀	11.5 μM Compound: OH-TAM	Antiproliferative activity against human ER-positive Ishikawa cells after 24 hrs by MTT assay Antiproliferative activity against human ER-positive Ishikawa cells after 24 hrs by MTT assay	[PMID: 25198997]
Ishikawa	IC₅₀	1.27 nM Compound: 4-OHT	Antiproliferative activity against human Ishikawa cells Antiproliferative activity against human Ishikawa cells	[PMID: 34710747]
Ishikawa	IC₅₀	3.57 μg/mL Compound: 4-Hydroxy-Tamoxifen	Inhibition of estradiol-induced proliferation in human Ishikawa cells after 72 hrs by Cell-titer-Glo assay Inhibition of estradiol-induced proliferation in human Ishikawa cells after 72 hrs by Cell-titer-Glo assay	[PMID: 28442256]
MCF-10A	IC₅₀	10 μM Compound: OH-TAM	Cytotoxicity against human MCF10A cells after 72 hrs by MTT assay Cytotoxicity against human MCF10A cells after 72 hrs by MTT assay	[PMID: 25198997]
MCF-10A	IC₅₀	21 μM Compound: 4-OHT	Anti-proliferative activity against human MCF-10A cells incubated for 96 hrs by CCK8 assay Anti-proliferative activity against human MCF-10A cells incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
MCF-10A	IC₅₀	21.5 μM Compound: 4OHT	Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability measured after 72 hrs by Cell Counting Kit-8 assay Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability measured after 72 hrs by Cell Counting Kit-8 assay	[PMID: 35611405]
MCF-10A	IC₅₀	21.5 μM Compound: 4-OHT	Cytotoxicity against human MCF-10A cells incubated for 72 hrs by CCK8 assay Cytotoxicity against human MCF-10A cells incubated for 72 hrs by CCK8 assay	[PMID: 37037140]
MCF-10A	IC₅₀	21.5 μM Compound: 4-OHT	Cytotoxicity against human MCF-10A cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human MCF-10A cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 37584263]
MCF-10A	IC₅₀	21.51 μM Compound: 1b; 4-OHT	Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37161783]
MCF7	EC₅₀	3.5 nM Compound: 2a; 4OH-T	Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay	[PMID: 34251202]
MCF7	EC₅₀	7.4 μM Compound: OH-TAM	Antiproliferative activity against human ER-negative MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human ER-negative MCF7 cells after 72 hrs by MTT assay	[PMID: 25198997]
MCF7	EC₅₀	8.8 μM Compound: OH-TAM	Antiproliferative activity against human ER-negative MCF7 cells after 24 hrs by MTT assay Antiproliferative activity against human ER-negative MCF7 cells after 24 hrs by MTT assay	[PMID: 25198997]
MCF7	IC₅₀	0.0033 μM Compound: 4-OHT	Antiproliferative activity against human MCF7 cells after 5 days by coulter counter analysis Antiproliferative activity against human MCF7 cells after 5 days by coulter counter analysis	[PMID: 27529700]
MCF7	IC₅₀	0.0034 μM Compound: 4-hydroxytamoxifen	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 5 days by Coulter counting method Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 5 days by Coulter counting method	[PMID: 28105283]
MCF7	IC₅₀	0.15 μM Compound: 4-OHT	Antiproliferative activity against human MCF7 cells treated for 48 hrs followed by refreshed every 96 hrs measured on day 10 by Lowry assay Antiproliferative activity against human MCF7 cells treated for 48 hrs followed by refreshed every 96 hrs measured on day 10 by Lowry assay	[PMID: 26613635]
MCF7	IC₅₀	0.67 μM Compound: 4OHT	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by Cell Counting Kit-8 assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by Cell Counting Kit-8 assay	[PMID: 35611405]
MCF7	IC₅₀	0.67 μM Compound: 1b; 4-OHT	Antiproliferative activity against human tamoxifen-sensitive MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human tamoxifen-sensitive MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37161783]
MCF7	IC₅₀	0.67 μM Compound: 4-OHT	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay	[PMID: 37037140]
MCF7	IC₅₀	0.67 μM Compound: 4-OHT	Antiproliferative activity against ERalpha positive human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against ERalpha positive human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 37584263]
MCF7	IC₅₀	0.67 μM Compound: 4-OHT	Anti-proliferative activity against ERalpha positive human MCF7 cells incubated for 96 hrs by CCK8 assay Anti-proliferative activity against ERalpha positive human MCF7 cells incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
MCF7	IC₅₀	0.95 μg/mL Compound: 4-Hydroxy-Tamoxifen	Inhibition of estradiol-induced proliferation in human MCF7 cells after 72 hrs by Cell-titer-Glo assay Inhibition of estradiol-induced proliferation in human MCF7 cells after 72 hrs by Cell-titer-Glo assay	[PMID: 28442256]
MCF7	IC₅₀	1.2 nM Compound: 4-OHT	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 34710747]
MCF7	IC₅₀	10.1 μM Compound: 4-OHT	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay	[PMID: 30939353]
MCF7	IC₅₀	11 μM Compound: 4-OHT	Antiproliferative activity against human resistant MCF7 cells harboring ERalpha Y537S mutant at LBD assessed as cell viability incubated for 96 hrs by CCK8 assay Antiproliferative activity against human resistant MCF7 cells harboring ERalpha Y537S mutant at LBD assessed as cell viability incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
MCF7	IC₅₀	15.6 μM Compound: 4OHT	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 33965842]
MCF7	IC₅₀	17.5 μM Compound: 4-hydroxytamoxifen	Antiproliferative activity against human MCF7 cells measured after 72 hrs by sulforhodamine B assay Antiproliferative activity against human MCF7 cells measured after 72 hrs by sulforhodamine B assay	[PMID: 31465222]
MCF7	IC₅₀	2.45 x 10^-5μM Compound: 4-Hydroxytamoxifen	Antiproliferative activity against human MCF7 cells incubated for 5 days by MTT assay Antiproliferative activity against human MCF7 cells incubated for 5 days by MTT assay	[PMID: 38870830]
MCF7	IC₅₀	20 μM Compound: 4-hydroxytamoxifen	Cytotoxicity against tamoxifen-resistant human MCF7 cells assessed as reduction in cell viability after 5 days by Coulter counting method Cytotoxicity against tamoxifen-resistant human MCF7 cells assessed as reduction in cell viability after 5 days by Coulter counting method	[PMID: 28105283]
MCF7	IC₅₀	22 μM Compound: 4-OHT	Antiproliferative activity against human tamoxifen-resistant MCF7 cells after 5 days by coulter counter analysis Antiproliferative activity against human tamoxifen-resistant MCF7 cells after 5 days by coulter counter analysis	[PMID: 27529700]
MCF7	IC₅₀	3.2 μM Compound: 4-OHT	Antiproliferative activity against human resistant MCF7 cells harboring EGFR assessed as cell viability incubated for 96 hrs by CCK8 assay Antiproliferative activity against human resistant MCF7 cells harboring EGFR assessed as cell viability incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
MCF7	IC₅₀	5.2 μM Compound: 4-Hydroxytamoxifen	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 39026643]
MCF7	IC₅₀	5.8 μM Compound: 4-OHT	Antiproliferative activity against human resistant MCF7 cells harboring ERalpha D538G mutant at LBD assessed as cell viability incubated for 96 hrs by CCK8 assay Antiproliferative activity against human resistant MCF7 cells harboring ERalpha D538G mutant at LBD assessed as cell viability incubated for 96 hrs by CCK8 assay	[PMID: 38809993]
MCF7	IC₅₀	9.5 μM Compound: 4OHT	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30053783]
MCF7	IC₅₀	9.5 μM Compound: 4-OHT	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32283297]
MCF7	IC₅₀	9.9 nM Compound: 2	Antiproliferative activity against human MCF7 cells after 6 days in presence of estradiol by CellTiter-Glo assay Antiproliferative activity against human MCF7 cells after 6 days in presence of estradiol by CellTiter-Glo assay	[PMID: 29562737]
MDA-MB-231	EC₅₀	7.8 μM Compound: OH-TAM	Antiproliferative activity against human ER-positive MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human ER-positive MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25198997]
MDA-MB-231	EC₅₀	8 μM Compound: OH-TAM	Antiproliferative activity against human ER-positive MDA-MB-231 cells after 24 hrs by MTT assay Antiproliferative activity against human ER-positive MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 25198997]
MDA-MB-231	IC₅₀	17.25 μM Compound: 4-OHT	Antiproliferative activity against ERalpha negative human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against ERalpha negative human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 37584263]
MDA-MB-231	IC₅₀	18.43 μM Compound: 4OHT	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by Cell Counting Kit-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by Cell Counting Kit-8 assay	[PMID: 35611405]
MDA-MB-231	IC₅₀	18.43 μM Compound: 1b; 4-OHT	Antiproliferative activity against triple negative human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against triple negative human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37161783]
MDA-MB-231	IC₅₀	36.76 nM Compound: 4-OHT	Antiproliferative activity against human MDA-MB-231 cells Antiproliferative activity against human MDA-MB-231 cells	[PMID: 34710747]
MDA-MB-231	IC₅₀	6.51 μg/mL Compound: 4-Hydroxy-Tamoxifen	Inhibition of estradiol-induced proliferation in human MDA-MB-231 cells after 72 hrs by Cell-titer-Glo assay Inhibition of estradiol-induced proliferation in human MDA-MB-231 cells after 72 hrs by Cell-titer-Glo assay	[PMID: 28442256]
MRC5	IC₅₀	>100 nM Compound: 4-OHT	Antiproliferative activity against human MRC5 cells Antiproliferative activity against human MRC5 cells	[PMID: 34710747]
T47D	IC₅₀	0.01 μM Compound: 4-OHT	Antagonist activity at ERalpha in human T47D-KBLuc cells assessed as inhibition of E2-induced transcriptional activity by luciferase reporter gene assay Antagonist activity at ERalpha in human T47D-KBLuc cells assessed as inhibition of E2-induced transcriptional activity by luciferase reporter gene assay	[PMID: 26613635]
T47D	IC₅₀	0.024 μM Compound: 4-OHT	Antiproliferative activity against human T47D cells after 5 days by coulter counter analysis Antiproliferative activity against human T47D cells after 5 days by coulter counter analysis	[PMID: 27529700]
T47D	IC₅₀	0.54 μM Compound: 4-OHT	Antiproliferative activity against human tamoxifen-resistant T47D cells over-expressing PKC-alpha after 5 days by coulter counter analysis Antiproliferative activity against human tamoxifen-resistant T47D cells over-expressing PKC-alpha after 5 days by coulter counter analysis	[PMID: 27529700]
T47D	IC₅₀	1.95 μM Compound: 1b; 4-OHT	Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37161783]
T47D	IC₅₀	1.95 μM Compound: 4-OHT	Antiproliferative activity against ERalpha positive human T47D cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against ERalpha positive human T47D cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 37584263]
T47D	IC₅₀	11.59 μM Compound: 1b; 4-OHT	Antiproliferative activity against human T47D cells harboring ERalpha D538G mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells harboring ERalpha D538G mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37161783]
T47D	IC₅₀	8.9 μM Compound: 4-OHT	Antiproliferative activity against human T47D cells harboring ERalpha Y537S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human T47D cells harboring ERalpha Y537S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 37584263]
T47D	IC₅₀	9.13 μM Compound: 4-OHT	Antiproliferative activity against human T47D cells harboring ERalpha D538G mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human T47D cells harboring ERalpha D538G mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 37584263]
T47D	IC₅₀	9.89 μM Compound: 1b; 4-OHT	Antiproliferative activity against human T47D cells harboring ERalpha Y537S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells harboring ERalpha Y537S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37161783]
Vero	IC₅₀	15.1 μM Compound: 4OHT	Antiproliferative activity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 33965842]

In Vitro

4-Hydroxytamoxifen (Monohydroxytamoxifen) is a selective ostrogen receptor antagonist, with an IC₅₀ of 3.3 nM for the [³H]oestradiol binding to oestrogen receptor. 4-Hydroxytamoxifen (10, 100 nM) enables to inhibit the binding of [³H]oestradiol to the human 8 S oestrogen receptor^[1].
4-Hydroxytamoxifen activates intein-linked inactive Cas9. In human cells, conditionally active Cas9s modify target genomic sites with up to 25-fold higher specificity than wild-type Cas9^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

4-Hydroxytamoxifen (0.2, 1 and 5 μg/day, p.o.) causes a dose-related decrease in uterine wet weight of immature rats^[1].
4-Hydroxytamoxifen (6 μg/0.1 mL sesame oil/day, s.c.) effectively attenuates methamphetamine-induced nigrostriatal dopamine depletions in bothsexes of intact and gonadectomized C57BL/6 J mice. 4-Hydroxytamoxifen does not alter the dopamine content levels in the striatum^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 68047-06-3
Appearance Solid
Molecular Weight 387.52
Formel C₂₆H₂₉NO₂
Color White to off-white
SMILES

CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN(C)C)C=C2)\C3=CC=C(O)C=C3
Synonyms

(Z)-4-Hydroxytamoxifen; trans-4-Hydroxytamoxifen; (Z)-Afimoxifene
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (59)

All IHCRT-PCRWBIn Vivo Efficacy StudyBio/Physico-chemical Assay

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Journal Impact Factor

Nature

Fasting boosts breast cancer therapy efficacy via glucocorticoid activation. [Abstract]

2026 Jan;649(8098):1013-1021. PMID: 41372410

4-Hydroxytamoxifen purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1013-1021. [Abstract]

Representative immunohistochemistry stainings for Ki-67 in MCF7 xenografts from mice treated with ad-libitum diet, tamoxifen (TMX, 45 mg/kg, daily, oral), fasting and combination (TMX+Fasting).

4-Hydroxytamoxifen purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1013-1021. [Abstract]

MCF7 xenograft tumour growth in six/eight-week-old female athymic nude mice in the different treatment arms (TMX, 45 mg/kg, daily, oral).
Cancer Cell

Myofibroblast programming blocks differentiation of TLS-organizing fibroblastic reticular cells in pancreatic cancer. [Abstract]

2026 Mar 26:S1535-6108(26)00156-X. PMID: 41895277
Cancer Cell

In vivo models of subclonal oncogenesis and dependency in hematopoietic malignancy. [Abstract]

2024 Nov 11;42(11):1955-1969.e7. PMID: 39532065

4-Hydroxytamoxifen purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 Nov 11;42(11):1955-1969.e7. [Abstract]

Lin ^- bone marrow from WT or Ubc:CreERT2 Flt3^GL-ITD was infected with MSCV:Dre-IRES-GFP retrovirus or mock infection. Cells were treated ± 4-hydroxytamoxifen (400 nM, 48 h) to activate Cre, and DNA was isolated 72 hours post treatment. PCR was used to evaluate Dre-inversion and Cre-deletion, visualized by capillary electrophoresis (Qiaxcel).

4-Hydroxytamoxifen purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 Nov 11;42(11):1955-1969.e7. [Abstract]

Lin^- HSPCs from fluorescent reporter mice (Lox, Ai14), or (Rox-RLTG) were infected with GFP+ retroviruses encoding CreER or DreSTAPL-ODC. Cultures were treated with DMSO, 4-OHT (400 nM, 48 h), or grazoprevir (GZV) (10 μM). Barplot depicts recombination in infected population (%TdTomato+ of GFP+ cells).
Nat Neurosci

A bottom-up septal inhibitory circuit mediates anticipatory control of drinking. [Abstract]

2025 Sep 22. PMID: 40983715
Mol Cell

Functional nutrient-genetic profiling reveals biotin and FBXW7 are essential to bypass glutamine addiction. [Abstract]

2026 Feb 25:S1097-2765(26)00097-3. PMID: 41747732
Mol Cell

METTL3 and N6-Methyladenosine Promote Homologous Recombination-Mediated Repair of DSBs by Modulating DNA-RNA Hybrid Accumulation. [Abstract]

2020 Aug 6;79(3):425-442.e7. PMID: 32615088
Sci Immunol

ILC3s promote intestinal tuft cell hyperplasia and anthelmintic immunity through RANK signaling. [Abstract]

2025 May 16;10(107):eadn1491. PMID: 40378237
Nat Commun

Lactate derived from macrophages drives skin dermal fibroblasts phenotypic remodeling via MCT1-primed histone H3 lysine 23 lactylation in hypertrophic scar. [Abstract]

2026 Feb 12;17(1):2694. PMID: 41680147
Nat Commun

Priming with LSD1 inhibitors promotes the persistence and antitumor effect of adoptively transferred T cells. [Abstract]

2024 May 21;15(1):4327. PMID: 38773088

4-Hydroxytamoxifen purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 May 21;15(1):4327. [Abstract]

On day 5, LSD1 immunoblot analysis was performed on Rosa26^Cre-ERT2Lsd1^f/f CD8⁺ T cells, which had been treated with 4-OHT (100 nM) during either the 2-day TCR activation phase (4OHT-A) or the 3-day IL-2 expansion phase (4OHT-E).
Nat Commun

DHX9 maintains epithelial homeostasis by restraining R-loop-mediated genomic instability in intestinal stem cells. [Abstract]

2024 Apr 9;15(1):3080. PMID: 38594251
Nat Commun

Persistent repair intermediates induce senescence. [Abstract]

2018 Sep 25;9(1):3923. PMID: 30254262
Neuron

Biased histamine signaling selectively gates fat preference. [Abstract]

2025 Nov 26:S0896-6273(25)00842-6. PMID: 41308645
Acta Pharm Sin B

Inhibition of ASCT2 induces hepatic stellate cell senescence with modified proinflammatory secretome through an IL-1 α/NF- κ B feedback pathway to inhibit liver fibrosis. [Abstract]

2022 Sep;12(9):3618-3638. PMID: 36176909
Adv Sci (Weinh)

AXL Promotes Ischemic Myelin Repair Through Alleviating Myelin Debris Deposition and Lipid Droplets Accumulation. [Abstract]

2026 Feb;13(10):e17825. PMID: 41524160
Adv Sci (Weinh)

Faecalibaculum rodentium Alleviates Ionizing Radiation-Induced Damage in Mice by Improving Intestinal Integrity and Hematopoiesis via Its Metabolite Butyrate. [Abstract]

2025 Oct 13:e09383. PMID: 41082369
Adv Sci (Weinh)

Conditional Overexpression of Serpine2 Promotes Hair Cell Regeneration from Lgr5+ Progenitors in the Neonatal Mouse Cochlea. [Abstract]

2025 May;12(18):e2412653. PMID: 40091489
Mol Ther

Estrogen-mediated NF-κB blockade enables breast cancer sensitivity to oncolytic VSV virotherapy. [Abstract]

2026 May 5:S1525-0016(26)00382-5. PMID: 42093158
J Neuroinflammation

Microglial NLRC5 drives lysosomal dysfunction to disrupt autophagic flux and promote post-stroke neuroinflammation. [Abstract]

2025 Oct 31;22(1):253. PMID: 41174779
Cell Death Dis

Sodium/glucose cotransporter 1-dependent metabolic alterations induce tamoxifen resistance in breast cancer by promoting macrophage M2 polarization. [Abstract]

2021 May 18;12(6):509. PMID: 34006822
Cell Death Dis

TNFR2 induced priming of the inflammasome leads to a RIPK1-dependent cell death in the absence of XIAP. [Abstract]

2019 Sep 20;10(10):700. PMID: 31541082
NPJ Biofilms Microbiomes

Gut-resident Phascolarctobacterium succinatutens decreases fat accumulation via MYC-driven epigenetic regulation of arginine biosynthesis. [Abstract]

2025 Aug 2;11(1):150. PMID: 40753182
Proc Natl Acad Sci U S A

TRIM24 as a therapeutic target in endocrine treatment-resistant breast cancer. [Abstract]

2025 Aug 19;122(33):e2507571122. PMID: 40815626
Dev Cell

Conserved signals control self-organization and symmetry breaking of murine bilayered epithelia during development and regeneration. [Abstract]

2025 Jun 25:S1534-5807(25)00362-4. PMID: 40592344
Dev Cell

GRP75-dependent mitochondria-ER contacts ensure cell survival during early mouse thymocyte development. [Abstract]

2024 Jul 3:S1534-5807(24)00385-X. PMID: 38981469
Dev Cell

Setdb1 protects genome integrity in murine muscle stem cells to allow for regenerative myogenesis and inflammation. [Abstract]

2024 Jun 5:S1534-5807(24)00329-0. PMID: 38848717
Oncogene

BMAL1 collaborates with CLOCK to directly promote DNA double-strand break repair and tumor chemoresistance. [Abstract]

2023 Mar;42(13):967-979. PMID: 36725890
Cell Rep

The m6A reader IGF2BP2 promotes homologous recombination-mediated DNA repair by eliminating DNA-RNA hybrids. [Abstract]

2025 Oct 15;44(10):116438. PMID: 41100254
Cell Rep

Protein UFMylation regulates early events during ribosomal DNA-damage response. [Abstract]

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MRE11:p.K464R mutation mediates olaparib resistance by enhancing DNA damage repair in HGSOC. [Abstract]

2023 Sep 27;13(1):178. PMID: 37759323
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A Novel Long-range Excitatory Neural Circuit from the Magnocellular Red Nucleus to Spinal Dorsal Horn Facilitates Neuropathic Pain-like Behaviors in Male Mice. [Abstract]

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Chin Med-UK

Shikonin and 4-hydroxytamoxifen synergistically inhibit the proliferation of breast cancer cells through activating apoptosis signaling pathway in vitro and in vivo. [Abstract]

2020 Mar 10;15:23. PMID: 32175001
Biochem Pharmacol

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Biochem Pharmacol

Cabozantinib inhibits necroptosis by targeting MLKL oligomerization and alleviates psoriasis in vivo. [Abstract]

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Ependymal Yes-Associated Protein Promotes the Neural Regeneration Through Enhancing the Ependymal Cell-Derived Perilesional Glial Borders in Mice After Spinal Cord Injury. [Abstract]

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Repurposing of Ibrutinib and Quizartinib as potent inhibitors of necroptosis. [Abstract]

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Establishment of patient-derived organoids for guiding personalized therapies in breast cancer patients. [Abstract]

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Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

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iScience

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Breast Cancer Res Treat

Monopolar spindle 1 contributes to tamoxifen resistance in breast cancer through phosphorylation of estrogen receptor α. [Abstract]

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Mucinous breast cancer organoids: an in vitro research model. [Abstract]

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Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (129.03 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 20 mg/mL (51.61 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5805 mL

12.9026 mL

25.8051 mL

5 mM

0.5161 mL

2.5805 mL

5.1610 mL

10 mM

0.2581 mL

1.2903 mL

2.5805 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (5.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 5 mg/mL (12.90 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 0.5% HPMC/1% Tween-80 in Saline water

Solubility: 20 mg/mL (51.61 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

Cytosol (200 μL) is incubated for 30 min at 4°C with different concentrations of oestradiol, tamoxifen and (4-Hydroxytamoxifen) or dihydroxytamoxifen administered in 10 μL methanol. Control tubes are incubated with 10 μL methanol alone and non-specific binding is determined in a parallel incubation of cytosol (200 μL) with methanol (10 μL) containing DES (5 × 10⁶ M). [2,4,6,7-³H]Oestradiol solution (50 μL) in TED buffer is added to each tube to give a final concentration of 2 × 10^-9 M. Incubation is continued for 4 h (4°C) and then 400 μL of a suspension of dextran-coated charcoal (250 mg % Norit A, 2.5 mg % dextran) in TED buffer are added and allowed to stand for 20 min. Tubes are centrifuged at 800 g for 10 min (4°C) and 400 μL samples of the supernatant are added to 10 mL tritium scintillator (6 g butyl PBD, 135 mL toluene, 720 ml dioxan, 100 g naphthalene, 45 mL absolute methanol). Samples are counted for 10 min in a liquid scintillation spectrometer. Counting efficiency is determined by external standardization (35-36 %). Results are represented as a percentage of the specifically bound radioactivity (c.p.m.) in the control tubes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]

Mice^[3]
Animals of each sex are divided into two groups: one group receives 4-Hydroxytamoxifen [6 μg/0.1 mL sesame oil/day, subcutaneously (s.c.) starting at 06.00 h] injections for three consecutive days, while the other group receives an equivalent amount of sesame oil injection for 3 days. Four hours following the third injection, each group is then subdivided into two groups: one receives four cumulative doses of methamphetamine hydrochloride (10 mg/kg, s.c.), and the other receives a comparable volume of saline at 2-h intervals. Bilateral gonadectomy is performed under pentobarbital anesthesia (50 mg/kg, intraperitoneally). Five weeks after surgery,gonadectomized mice of each sex are randomly divided into six groups. Five groups of each sex receive three daily injections ofvarious concentrations of 4-Hydroxytamoxifen (0, 1.5, 3.0, 6.0, and 12.0 μg/0.1 mL sesame oil/day). Four hours following the third injection, mice receive four doses of methamphetamine (MA, 10 mg/kg) at 2-h intervals. The remaining group of each sex receives sesame oil pretreatment for three consecutive days, followed by saline injections, and serves as the control group^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (622 KB)
- English - EN (622 KB)
- Français - FR (622 KB)
- Deutsch - DE (622 KB)
- Norwegian - NO (622 KB)
- Español - ES (622 KB)
- Swedish - SV (622 KB)
- Italian - IT (622 KB)
- Korean - KR (622 KB)
- Portuguese - PT (622 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Jordan VC, et al. A monohydroxylated metabolite of tamoxifen with potent antioestrogenic activity. J Endocrinol. 1977 Nov;75(2):305-16. [Content Brief]

[2]. Davis KM, et al. Small molecule-triggered Cas9 protein with improved genome-editing specificity. Nat Chem Biol. 2015 May;11(5):316-8. [Content Brief]

[3]. Kuo YM, et al. 4-Hydroxytamoxifen attenuates methamphetamine-induced nigrostriatal dopaminergic toxicity in intact and gonadetomized mice. J Neurochem. 2003 Dec;87(6):1436-43. [Content Brief]

[4]. Zhang J, et al. Drug Inducible CRISPR/Cas Systems. Comput Struct Biotechnol J. 2019;17:1171-1177. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.5805 mL	12.9026 mL	25.8051 mL	64.5128 mL
	5 mM	0.5161 mL	2.5805 mL	5.1610 mL	12.9026 mL
	10 mM	0.2581 mL	1.2903 mL	2.5805 mL	6.4513 mL
	15 mM	0.1720 mL	0.8602 mL	1.7203 mL	4.3009 mL
	20 mM	0.1290 mL	0.6451 mL	1.2903 mL	3.2256 mL
	25 mM	0.1032 mL	0.5161 mL	1.0322 mL	2.5805 mL
	30 mM	0.0860 mL	0.4301 mL	0.8602 mL	2.1504 mL
	40 mM	0.0645 mL	0.3226 mL	0.6451 mL	1.6128 mL
	50 mM	0.0516 mL	0.2581 mL	0.5161 mL	1.2903 mL
DMSO	60 mM	0.0430 mL	0.2150 mL	0.4301 mL	1.0752 mL
	80 mM	0.0323 mL	0.1613 mL	0.3226 mL	0.8064 mL
	100 mM	0.0258 mL	0.1290 mL	0.2581 mL	0.6451 mL

Keywords

4-Hydroxytamoxifen

59 Cited Publications

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4-Hydroxytamoxifen

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) 4-Hydroxytamoxifen

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (59)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

4-Hydroxytamoxifen

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) 4-Hydroxytamoxifen

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (59)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

4-Hydroxytamoxifen Related Classifications

HY-16950 Related Classifications