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Endoxifen hydrochloride

Cat. No. M6710
Endoxifen hydrochloride Structure
Synonym:

Endoxifen HCl

Size Price Availability
10mg USD 94.5  USD105 4-7 Days
25mg USD 193.5  USD215 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Endoxifen hydrochloride is a estrogen receptor α (ERα) ligand; potent antiestrogen. Metabolite of tamoxifen. Primary metabolite responsible for the effectiveness of tamoxifen in ER-positive breast cancer.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 409.95
Formula C25H28ClNO2
CAS Number 1032008-74-4
Purity >98%
Solubility DMSO ≥ 33 mg/mL
Storage at -20°C
References

Endoxifen, the active metabolite of tamoxifen, inhibits cloned hERG potassium channels.
Chae YJ, et al. Eur J Pharmacol. 2015 Apr 5;752:1-7. PMID: 25680947.

Endoxifen is a new potent inhibitor of PKC: a potential therapeutic agent for bipolar disorder.
Ali SM, et al. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2665-7. PMID: 20227879.

Orally administered endoxifen is a new therapeutic agent for breast cancer.
Ahmad A, et al. Breast Cancer Res Treat. 2010 Jul;122(2):579-84. PMID: 20052538.

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SAR439859 (Amcenestrant)

SAR439859 (Amcenestrant) is an orally active, nonsteroidal and selective degrader of estrogen receptor, it is also a potent antagonist of ER with EC50 of 0.2 nM for ERα degradation.

4-Hydroxytamoxifen

4-Hydroxytamoxifen is a selective estrogen receptor modulator.

Methylpiperidino pyrazole

Methylpiperidino pyrazole (MPP) is an agonist for estrogen receptor α and lacks any ligand functionality with estrogen receptor (ER)β.

Endoxifen E-isomer hydrochloride

Endoxifen E-isomer hydrochloride is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Endoxifen hydrochloride, Endoxifen HCl supplier, Estrogen Receptor, inhibitors

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