Afimoxifene
- Product Name
- Afimoxifene
- CAS No.
- 68392-35-8
- Chemical Name
- Afimoxifene
- Synonyms
- 4-HT;C016601;Alfecifene;AFIMOXIFENE;4-OHT 4-hydroxy;4-Oht hydrotamoxifen;4-Monohydroxytamoxifen;Tamoxifen metabolite B;Afimoxifene cas 68392-35-8;(E/Z)-4-Hydroxy Tamoxifen
- CBNumber
- CB91353793
- Molecular Formula
- C26H29NO2
- Formula Weight
- 387.51
- MOL File
- 68392-35-8.mol
Afimoxifene Property
- Melting point:
- 135-144°C
- Boiling point:
- 514.4±50.0 °C(Predicted)
- Density
- 1.092
- storage temp.
- 2-8°C
- solubility
- methanol: soluble10mg/mL
- form
- solution
- pka
- 9.38±0.15(Predicted)
- color
- white to off-white
- Appearance
- white solid
- biological source
- synthetic
Safety
- Hazard Codes
- Xn
- Risk Statements
- 63-20/21/22
- Safety Statements
- 22-23-36
- RIDADR
- UN1170 - class 3 - PG 2 - Ethanol, solution
- WGK Germany
- 3
- RTECS
- SL1210000
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H361Suspected of damaging fertility or the unborn child
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P308+P313IF exposed or concerned: Get medical advice/attention.
N-Bromosuccinimide Price
- Product number
- H6278
- Product name
- 4-Hydroxytamoxifen
- Purity
- ≥70% Z isomer (remainder primarily E-isomer)
- Packaging
- 10mg
- Price
- $98
- Updated
- 2025/07/31
- Product number
- 94873
- Product name
- 4-Hydroxytamoxifen
- Purity
- (
- Packaging
- 10mg
- Price
- $210.9
- Updated
- 2025/07/31
- Product number
- 17308
- Product name
- (E/Z)-4-hydroxy Tamoxifen
- Purity
- ≥98% (E) and (Z) isomers (50:50)
- Packaging
- 5mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 17308
- Product name
- (E/Z)-4-hydroxy Tamoxifen
- Purity
- ≥98% (E) and (Z) isomers (50:50)
- Packaging
- 10mg
- Price
- $61
- Updated
- 2024/03/01
- Product number
- T176
- Product name
- 4-Hydroxytamoxifen
- Purity
- analytical standard, (
- Packaging
- 10mg
- Price
- $90.6
- Updated
- 2025/07/31
Afimoxifene Chemical Properties,Usage,Production
Description
(E/Z)-4-Hydroxytamoxifen (4-OHT, cis/trans-4-hydroxytamoxifen, afimoxifene) is a selective estrogen receptor (ER) modulator, an active metabolite of tamoxifen. 4-Hydroxytamoxifen is widely used as a research tool for inducible genome manipulation.
4-Hydroxytamoxifen is used in the inducible Cre-LoxP system to control CreER/CreERT2 recombinase activity and trigger tissue-specific gene expression or genome/genetic modification (e.g., gene deletion). 4-Hydroxytamoxifen is a part of the TRAP/TRAP2 (targeted recombination in active populations) systems providing genetic access to neuron activity. It is also used in CRISPR/Cas9 gene editing to activate inactivated Cas9 nuclease.
Also, 4-Hydroxytamoxifen was reported to be an intramembranous lipid peroxidation inhibitor, exhibiting peroxyl radical scavenging activity.
Chemical Properties
Off-White Solid
Uses
A selective estrogen receptor modulator.
Uses
(E/Z)-4-Hydroxy Tamoxifen is selective estrogen receptor modulator.
Definition
ChEBI: Afimoxifene is a tertiary amino compound that is tamoxifen in which the phenyl group which is in a Z- relationship to the ethyl substituent is hydroxylated at the para- position. It is the active metabolite of tamoxifen. It has a role as an antineoplastic agent, an estrogen receptor antagonist and a metabolite. It is a tertiary amino compound and a member of phenols. It is functionally related to a tamoxifen.
brand name
TamoGel (Ascend Therapeutics).
General Description
4-Hydroxytamoxifen is a first generation, selective estrogen receptor modulator (SERM) that functions as an antagonist in breast cancer cells but can display estrogen-like activities in the uterus and bone.
Biological Activity
4-hydroxytamoxifen is an estrogen receptor modulator.estrogen receptor can be selectively stimulated or inhibited, providing promising therapeutic opportunities for auto-immune diseases, prostate and breast cancer, as well as depression.
Biochem/physiol Actions
Metabolite of the chemotherapeutic drug tamoxifen, exhibiting more potent estrogen agonist/antagonist activity than the parent drug. Also active as intra-membranous inhibitor of lipid peroxidation.
in vitro
previous study was conducted to evaluate the effects of tamoxifen and its active metabolite 4-hydroxytamoxifen on isolated rat cardiac myocyte mechanical function and calcium handling. results showed that myocytes treated with 4-hydroxytamoxifen had similarly to tamoxifen-treated cells to both calcium handling and contractility [1].
in vivo
previous animal study compared the extent of dna adduct formation in sd rats treated with seven tamoxifen or 4-hydroxytamoxifen. results showed that the liver weights and microsomal rates were not changed by tamoxifen or 4-hydroxytamoxifen treatment. moreover, the uterine weights were significantly decreased and uterine peroxidase activity was marginally decreased in tamoxifen or 4-hydroxytamoxifen treated rats. in addition, hepatic dna adduct levels in rats treated with 4-hydroxytamoxifen did not differ from control rats. similaryly, the adduct levels in uterus dna from rats treated with tamoxifen or 4-hydroxytamoxifen were not different from those in control rats [2].
IC 50
27 and 18 μm for mcf-7 and mda-mb-231 cell proliferation
storage
-20°C
References
[1] asp ml,martindale jj,metzger jm. direct, differential effects of tamoxifen, 4-hydroxytamoxifen, and raloxifene on cardiac myocyte contractility and calcium handling. plos one.2013 oct 24;8(10):e78768.
[2] beland fa,mcdaniel lp,marques mm. comparison of the dna adducts formed by tamoxifen and 4-hydroxytamoxifen in vivo. carcinogenesis.1999 mar;20(3):471-7.
[3] lee o et al. a randomized phase ii presurgical trial of transdermal 4-hydroxytamoxifen gel versus oral tamoxifen in women with ductal carcinoma in situ of the breast. clin cancer res.2014 jul 15;20(14):3672-82.
Afimoxifene Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Afimoxifene manufacturers
- Product
- Afimoxifene 68392-35-8
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 98%-99.9%HPLC
- Supply Ability
- 100KG
- Release date
- 2020-02-04