Endoxifen Chemical Properties

Melting point:

127-129°C

Boiling point:

519.3±50.0 °C(Predicted)

Density 

1.099±0.06 g/cm3(Predicted)

storage temp. 

Amber Vial, -86°C Freezer, Under Inert Atmosphere

solubility 

DMSO : 50 mg/mL (133.87 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)

form 

Powder

pka

10.36±0.15(Predicted)

color 

White to off-white

Stability:

Light Sensitive, Temperature Sensitive

Endoxifen Usage And Synthesis

Chemical Properties

Off-White to Pink Solid

Uses

A novel active metabolite of the anti-cancer drug Tamoxifen. It showed potent ER binding property, blocked estrogen stimulated growth of breast cancer cell and half maximal inhibition of estrogen responsive gene expression in ER pos. human breast ca

Uses

A novel active metabolite of the anti-cancer drug Tamoxifen (T006000). It showed potent ER binding property, blocked estrogen stimulated growth of breast cancer cell and half maximal inhibition of estrogen responsive gene expression in ER pos. human breast cancer cell line.

Definition

ChEBI: 4-Hydroxy-N-desmethyltamoxifen is a stilbenoid.

Biological Activity

(Z)-Endoxifen (endoxifen) is an active tamoxifen metabolite generated via actions of cytochrome P450 (CYP) enzymes CYP3A4/5 and CYP2D6. Endoxifen is more potent than tamoxifen as a selective estrogen receptor modulator (SERM) both in vitro and in vivo with good pharmacokinetics and oral availability (∼80% MCF-7 tumor growth inhibition with 4-8 mg/kg/day endoxifen or 20 mg/kg/day tamoxifen in mice via p.o.). Endoxifen also exhibits 4-fold higher PKC inhibitory potency than tamoxifen and can overcome tamoxifen resistance due to cytochrome CYP2D6 polymorphism.

Endoxifen(112093-28-4)Related Product Information

• Endoxifen HCl
• Tamoxifen Impurity 3
• 4-Benzyloxy β-Hydroxy TaMoxifen
• TaMoxifen DiMer
• 1-(4-(2-Dimethylamino)-2-ethoxyphenyl butanone
• N-Desmethyl-4-hydroxy Tamoxifen β-D-Glucuronide (E/Z Mixture)
• 4Hydroxy Tamoxifen
• Tamoxifen EP Impurity D
• (E)-4-Alloxycarboxyl Tamoxifen
• desdimethyltamoxifen
• TAMOXIFEN-N-OXIDE
• Droloxifene
• (E)-4-Acetoxy Tamoxifen
• N-Desmethyl Tamoxifen Methanethiosulfonate
• 2-[4-[(E)-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethyl-ethanamine
• alpha-[4-[2-(dimethylamino)ethoxy]phenyl]-beta-ethyl-alpha-phenylphenethyl alcohol
• (E)-4-Hydroxy-N-desmethyl Tamoxifen
• 4-HYDROXYTAMOXIFEN