1. Others
    Cell Cycle/DNA Damage
    Autophagy
  2. Estrogen Receptor/ERR
    CRISPR/Cas9
    Autophagy

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

Cat. No.: HY-16950 Purity: 99.27%
Handling Instructions

4-Hydroxytamoxifen, an active metabolite of tamoxifen, is a selective estrogen receptor antagonist, with an IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor, widely used to treat breast cancer; also increases CRISPR/Cas9-mediated editing frequency.

For research use only. We do not sell to patients.
4-Hydroxytamoxifen Chemical Structure

4-Hydroxytamoxifen Chemical Structure

CAS No. : 68047-06-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 102 In-stock
2 mg USD 60 In-stock
5 mg USD 120 In-stock
10 mg USD 168 In-stock
25 mg USD 360 In-stock
50 mg USD 660 In-stock
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

4-Hydroxytamoxifen, an active metabolite of tamoxifen, is a selective estrogen receptor antagonist, with an IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor, widely used to treat breast cancer; also increases CRISPR/Cas9-mediated editing frequency.

IC50 & Target[1][2]

Estrogen receptor

3.3 nM (IC50)

CRISPR/Cas9

 

In Vitro

4-Hydroxytamoxifen (Monohydroxytamoxifen) is a selective oestrogen 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, reduces off-target CRISPR-mediated gene editing. In human cells, conditionally active Cas9s modify target genomic sites with up to 25-fold higher specificity than wild-type Cas9[2].

In Vivo

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].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.5806 mL 12.9029 mL 25.8058 mL
5 mM 0.5161 mL 2.5806 mL 5.1612 mL
10 mM 0.2581 mL 1.2903 mL 2.5806 mL
Please refer to the solubility information to select the appropriate solvent.
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]

4-Hydroxytamoxifen is formulated in sesame oil[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
Molecular Weight

387.51

Formula

C₂₆H₂₉NO₂

CAS No.

68047-06-3

SMILES

CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN(C)C)C=C2)\C3=CC=C(O)C=C3.[(Z)]

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 28 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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4-Hydroxytamoxifen
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HY-16950
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