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MedKoo Cat#: 561177 | Name: Endoxifen mesylate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is a chemical that is under development for estrogen receptor-positive breast cancer. It is also being evaluated as an antipsychotic for treatment of mania and other psychotic disorders. Endoxifen is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group. It is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromatase inhibitors, and fulvestrant). The prodrug tamoxifen is metabolized by the CYP2D6 enzyme to produce afimoxifene (4-hydroxytamoxifen) and endoxifen.

Chemical Structure

Endoxifen mesylate
Endoxifen mesylate
CAS#1032008-71-1 (mesylate)

Theoretical Analysis

MedKoo Cat#: 561177

Name: Endoxifen mesylate

CAS#: 1032008-71-1 (mesylate)

Chemical Formula: C26H31NO5S

Exact Mass: 0.0000

Molecular Weight: 469.60

Elemental Analysis: C, 66.50; H, 6.65; N, 2.98; O, 17.03; S, 6.83

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
1032008-74-4 (HCl) 112093-28-4 (free base) 1372937-28-4 (citrate) 1032008-66-4 (acetate) 1032008-71-1 (mesylate) 1197194-61-8 (E-isomer HCl)
Synonym
Endoxifen HCl; Endoxifen hydrochloride; Z-Endoxifen HCl; 4-Hydroxy-N-desmethyltamoxifen; N-Desmethyl-4-hydroxytamoxifen;
IUPAC/Chemical Name
4-[(Z)-1-[4-[2-(Methylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol mesylate
InChi Key
NZSNFFJPXQBVFG-BJFQDICYSA-N
InChi Code
InChI=1S/C25H27NO2.CH4O3S/c1-3-24(19-7-5-4-6-8-19)25(20-9-13-22(27)14-10-20)21-11-15-23(16-12-21)28-18-17-26-2;1-5(2,3)4/h4-16,26-27H,3,17-18H2,1-2H3;1H3,(H,2,3,4)/b25-24-;
SMILES Code
OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)\CC)C=C1.OS(=O)(C)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 469.60 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Barginear MF, Jaremko M, Peter I, Yu C, Kasai Y, Kemeny M, Raptis G, Desnick RJ. Increasing tamoxifen dose in breast cancer patients based on CYP2D6 genotypes and endoxifen levels: effect on active metabolite isomers and the antiestrogenic activity score. Clin Pharmacol Ther. 2011 Oct;90(4):605-11. doi: 10.1038/clpt.2011.153. Epub 2011 Sep 7. PubMed PMID: 21900890. 2: Lin FI, Gonzalez EM, Kummar S, Do K, Shih J, Adler S, Kurdziel KA, Ton A, Turkbey B, Jacobs PM, Bhattacharyya S, Chen AP, Collins JM, Doroshow JH, Choyke PL, Lindenberg ML. Utility of (18)F-fluoroestradiol ((18)F-FES) PET/CT imaging as a pharmacodynamic marker in patients with refractory estrogen receptor-positive solid tumors receiving Z-endoxifen therapy. Eur J Nucl Med Mol Imaging. 2017 Mar;44(3):500-508. doi: 10.1007/s00259-016-3561-8. Epub 2016 Nov 21. PubMed PMID: 27872957. 3: de Krou S, Rosing H, Nuijen B, Schellens JH, Beijnen JH. Fast and Adequate Liquid Chromatography-Tandem Mass Spectrometric Determination of Z-endoxifen Serum Levels for Therapeutic Drug Monitoring. Ther Drug Monit. 2017 Apr;39(2):132-137. doi: 10.1097/FTD.0000000000000372. PubMed PMID: 28045782. 4: Reid JM, Goetz MP, Buhrow SA, Walden C, Safgren SL, Kuffel MJ, Reinicke KE, Suman V, Haluska P, Hou X, Ames MM. Pharmacokinetics of endoxifen and tamoxifen in female mice: implications for comparative in vivo activity studies. Cancer Chemother Pharmacol. 2014 Dec;74(6):1271-8. doi: 10.1007/s00280-014-2605-7. Epub 2014 Oct 16. PubMed PMID: 25318936; PubMed Central PMCID: PMC4343319. 5: Ding S, Bierbach U. Linker design for the modular assembly of multifunctional and targeted platinum(ii)-containing anticancer agents. Dalton Trans. 2016 Aug 16;45(33):13104-13. doi: 10.1039/c6dt01399f. PubMed PMID: 27251881; PubMed Central PMCID: PMC4987242.