Afimoxifene

 CAS No.: 68392-35-8  Cat No.: BP-300053  Purity: ≥95% 4.5  

Afimoxifene (4-hydroxytamoxifen) is a selective estrogen receptor modulator which is the active metabolite of tamoxifen. Afimoxifene is a transdermal gel formulation and is being developed by Ascend Therapeutics, Inc. under the trademark TamoGel. Afimoxifene has completed a phase II clinical trial for the treatment of cyclical mastalgia.

Afimoxifene

Structure of 68392-35-8

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Category
Ligand for Target Protein
Molecular Formula
C26H29NO2
Molecular Weight
387.51
Appearance
White to Off-white Solid

* For research and manufacturing use only. Not for human or clinical use.

SizePriceStockQuantity
100 mg $390 In stock
1 g $1290 In stock

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Purity
≥95%
Solubility
Soluble in Dichloromethane (Slightly), Methanol (Slightly)
Appearance
White to Off-white Solid
Application
Estrogen Antagonists
Storage
Store at 2-8°C
IUPACName
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol
Synonyms
(E/Z)-4-Hydroxytamoxifen; 4-[1-[4-[2-(Dimethylamino)ethoxy]phenyl]-2-phenyl-1-butenyl]phenol; TamoGel; Phenol, 4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]-
Boiling Point
514.4±50.0°C (Predicted)
Melting Point
135-144°C
Density
1.092±0.1 g/cm3 (Predicted)
InChI Key
TXUZVZSFRXZGTL-UHFFFAOYSA-N
InChI
InChI=1S/C26H29NO2/c1-4-25(20-8-6-5-7-9-20)26(21-10-14-23(28)15-11-21)22-12-16-24(17-13-22)29-19-18-27(2)3/h5-17,28H,4,18-19H2,1-3H3
Canonical SMILES
CCC(=C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3
1.Sulfation of afimoxifene, endoxifen, raloxifene, and fulvestrant by the human cytosolic sulfotransferases (SULTs): A systematic analysis.
Hui Y1, Luo L2, Zhang L3, Kurogi K4, Zhou C2, Sakakibara Y4, Suiko M4, Liu MC5. J Pharmacol Sci. 2015 Jul;128(3):144-9. doi: 10.1016/j.jphs.2015.06.004. Epub 2015 Jun 25.
Previous studies demonstrated that sulfate conjugation is involved in the metabolism of three commonly used breast cancer drugs, tamoxifen, raloxifene and fulvestrant. The current study was designed to systematically identify the human cytosolic sulfotransferases (SULTs) that are capable of sulfating raloxifene, fulvestrant, and two active metabolites of tamoxifen, afimoxifene and endoxifen. A systematic analysis using 13 known human SULTs revealed SULT1A1 and SULT1C4 as the major SULTs responsible for the sulfation of afimoxifene, endoxifen, raloxifene and fulvestrant. Kinetic parameters of these two human SULTs in catalyzing the sulfation of these drug compounds were determined. Sulfation of afimoxifene, endoxifen, raloxifene and fulvestrant under metabolic conditions was examined using HepG2 human hepatoma cells and MCF-7 breast cancer cells. Moreover, human intestine, kidney, liver, and lung cytosols were examined to verify the presence of afimoxifene/endoxifen/raloxifene/fulvestrant-sulfating activity.
ConcentrationVolumeMass1 mg5 mg10 mg
1 mM2.5806 mL12.9029 mL25.8058 mL
5 mM0.5161 mL2.5806 mL5.1612 mL
10 mM0.2581 mL1.2903 mL2.5806 mL
50 mM0.0516 mL0.2581 mL0.5161 mL

what is the functional group of Afimoxifene?

Afimoxifene is a triphenylethylene derivative, which means that it has three phenyl groups attached to an ethylene group. The phenyl groups are aromatic rings, and the ethylene group is a double bond. The functional groups in afimoxifene are: Aromatic rings: The three phenyl groups are aromatic rings. Aromatic rings are planar, conjugated, and cyclic systems that are stabilized by resonance. Double bond: The ethylene group is a double bond. Double bonds are unsaturated bonds that contain two pi electrons. The functional groups in afimoxifene are responsible for its biological activity. The aromatic rings are responsible for the binding of afimoxifene to estrogen receptors, and the double bond is responsible for the activation of estrogen receptors.

29/12/2018

Hello, can Afimoxifene be used in vitro?

Yes, Afimoxifene can be used in vitro. It is a selective estrogen receptor modulator (SERM) that is used to treat breast cancer. It can be used in vitro to study the effects of estrogen on cells and tissues.

16/5/2022

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* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2

* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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