4-hydroxytamoxifen

Modify Date: 2024-01-04 11:35:07

4-hydroxytamoxifen structure	Common Name	4-hydroxytamoxifen
	CAS Number	68047-06-3	Molecular Weight	387.514
	Density	1.1±0.1 g/cm3	Boiling Point	514.4±50.0 °C at 760 mmHg
	Molecular Formula	C₂₆H₂₉NO₂	Melting Point	105-107ºC
	MSDS	Chinese USA	Flash Point	264.9±30.1 °C
	Symbol	GHS07, GHS08	Signal Word	Warning

Use of 4-hydroxytamoxifen

4-Hydroxytamoxifen is a selective estrogen receptor modulator (SERM).

Name	afimoxifene
Synonym	More Synonyms

Description	4-Hydroxytamoxifen is a selective estrogen receptor modulator (SERM).
Related Catalog	Signaling Pathways >> Others >> Estrogen Receptor/ERR Research Areas >> Cancer
Target	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].
Kinase Assay	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].
Animal Admin	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].
References	[1]. Jordan VC, et al. A monohydroxylated metabolite of tamoxifen with potent antioestrogenic activity. J Endocrinol. 1977 Nov;75(2):305-16. [2]. Davis KM, et al. Small molecule-triggered Cas9 protein with improved genome-editing specificity. Nat Chem Biol. 2015 May;11(5):316-8. [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.

Density	1.1±0.1 g/cm3
Boiling Point	514.4±50.0 °C at 760 mmHg
Melting Point	105-107ºC
Molecular Formula	C₂₆H₂₉NO₂
Molecular Weight	387.514
Flash Point	264.9±30.1 °C
Exact Mass	387.219818
PSA	32.70000
LogP	7.34
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.597
Storage condition	2-8°C
Stability	Stable. Store cool. Incompatible with strong oxidizing agents.
Water Solubility	95% ethanol: 20 mg/mL

4-hydroxytamoxifen MSDS(Chinese)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SL1210000

CHEMICAL NAME :: Phenol, 4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenyl-1-b utenyl)-, (E)-

CAS REGISTRY NUMBER :: 68047-06-3

LAST UPDATED :: 199801

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C26-H29-N-O2

MOLECULAR WEIGHT :: 387.56

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 50 ug/kg

SEX/DURATION :: female 4 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

TYPE OF TEST :: DNA adduct

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 480 umol/kg/4D (Continuous)

REFERENCE :: CRNGDP Carcinogenesis (London). (Oxford Univ. Press, Pinkhill House, Southfield Road, Eynsham, Oxford OX8 1JJ, UK) V.1- 1980- Volume(issue)/page/year: 15,2087,1994

Symbol	GHS07, GHS08
Signal Word	Warning
Hazard Statements	H302-H312-H332-H361
Precautionary Statements	P280
Personal Protective Equipment	Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges
Hazard Codes	Xn
Risk Phrases	R20/21/22;R63
Safety Phrases	S22-S23-S36
RIDADR	NONH for all modes of transport
WGK Germany	3
RTECS	SL1210000

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MFCD00278780

4-hydroxytamoxifen

4-[(1Z)-1-{4-[2-(Dimethylamino)ethoxy]phenyl}-1-phenyl-1-buten-2-yl]phenol

Phenol, 4-[(1Z)-1-[[4-[2-(dimethylamino)ethoxy]phenyl]phenylmethylene]propyl]-

4-{(1Z)-1-[{4-[2-(dimethylamino)ethoxy]phenyl}(phenyl)methylidene]propyl}phenol

4-{(1Z)-1-[{4-[2-(dimethylamino)ethoxy]phenyl}(phenyl)methylene]propyl}phenol

4-hydroxy-tamoxifen

DC Chemicals Limited
China
Product Name: (Z)-4-hydroxy Tamoxifen
Price: $650.0/1g $1100.0/2g $2200.0/5g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 4-HYDROXYTAMOXIFEN
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

Zhejiang Hangyu API Co., Ltd
China
Product Name: 4-HYDROXYTAMOXIFEN
Price: ￥Inquiry/1kg
Purity: 99.5%
Stocking Period: Inquiry
Contact: Vinnie

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Price: $102/10mM*1mLinDMSO

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4-hydroxytamoxifen

Use of 4-hydroxytamoxifen

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