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

Name: 4-Hydroxytamoxifen
Brand: MedChemExpress
SKU: HY-16950
Rating: 5.0 (53 reviews)

Cat. No.: HY-16950 Purity: 99.86%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 68047-06-3

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 53 publication(s) in Google Scholar

Other Forms of 4-Hydroxytamoxifen:

53 Publications Citing Use of MCE 4-Hydroxytamoxifen

IHC

RT-PCR

In Vivo Efficacy Study

Bio/Physico-chemical Assay

: 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).

: 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).

: 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).

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]

Estrogen receptor

3.3 nM (IC₅₀)

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: 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	21.5 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	21.51 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: 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	0.67 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	0.95 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^-5 μM 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: 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	9.5 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	9.9 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: 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	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	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

Molecular Weight

387.52

Formula

C₂₆H₂₉NO₂

CAS No.

68047-06-3

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (281 KB) SDS (622 KB)

COA (250 KB) HNMR (226 KB) LCMS (123 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

4-Hydroxytamoxifen Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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4-Hydroxytamoxifen68047-06-3(Z)-4-Hydroxytamoxifen trans-4-Hydroxytamoxifen(Z)-AfimoxifeneEstrogen Receptor/ERRestrogen receptororalnucleus translocationInhibitorinhibitorinhibit

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

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