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  3. Endoxifen hydrochloride

Endoxifen hydrochloride 

Cat. No.: HY-18719B Purity: 98.32%
Handling Instructions

Endoxifen hydrochloride, the active metabolite of Tamoxifen, is a potent antiestrogen that targets estrogen receptor.

For research use only. We do not sell to patients.

Endoxifen hydrochloride Chemical Structure

Endoxifen hydrochloride Chemical Structure

CAS No. : 1197194-41-4

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10 mM * 1 mL in DMSO USD 116 In-stock
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10 mg USD 105 In-stock
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50 mg USD 310 In-stock
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100 mg USD 550 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Endoxifen hydrochloride:

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Description

Endoxifen hydrochloride, the active metabolite of Tamoxifen, is a potent antiestrogen that targets estrogen receptor.

IC50 & Target

Estrogen receptor[1]

In Vitro

Endoxifen blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. These studies reveal that Endoxifen concentrations between 10 and 1000 nM enhance ERα protein degradation. Lower concentrations of Endoxifen (≤1 nM) do not affect ERα protein levels[1].

In Vivo

GLAST::Cre(ERT);ROSA26loxP/loxP mice are injected intraventricularly with 5 μL 5 mM Endoxifen, and mice injected with 4 μL Adeno-Cre virus [109 plaque-forming units (pfu)] serve as positive control. At 7-10 days after ICV injection, mice are sacrificed and the SVZ dissected to isolate and derive stem and progenitor cells. These stem/progenitor cells are then cultured in permissive medium to form neurospheres and assayed for recombination. In our unpassaged preparations is found derived from Endoxifen-injected GLAST::CreERT2;ROSA26loxP/loxP mice that 1.9% of neurospheres show recombination, compared to a higher rate of 4.3% of neurospheres in Adeno-Cre-recombined ROSA26loxP/loxP mice[2].

Molecular Weight

409.95

Formula

C₂₅H₂₈ClNO₂

CAS No.

1197194-41-4

SMILES

OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)\CC)C=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 35 mg/mL (85.38 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4393 mL 12.1966 mL 24.3932 mL
5 mM 0.4879 mL 2.4393 mL 4.8786 mL
10 mM 0.2439 mL 1.2197 mL 2.4393 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

MCF7 and Ishikawa cells are grown in 10% triple charcoal-stripped serum-containing medium for 3 d. The cells are then plated at a density of 2,000 cells per well in 96-well tissue culture plates and treated as indicated every 48 h. Cell proliferation assays are conducted 8 days after the first treatment using a CellTiter-Glo Luminescent Cell Viability kit[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
GLAST::CreERT2 mice are used. Tamoxifen is injected as active metabolite 4-hydroxytamoxifen (4-OH-TAM), or 4-hydroxy-N-desmethyltamoxifen (Endoxifen). 4-OH-TAM is dissolved at 1 mM concentration in 2% ethanol/PBS and 5 μL injected into the ventricles. Endoxifen has not been used before for the induction of the ERT2 system. Endoxifen hydrochloride hydrate has a recommended solubility of over 10 mg/mL (25 mM) in 100% DMSO, corresponding to a maximum concentration of 25 mM or a dose of 125 nmol in a 5 μL volume. At this concentration, a proportion of mice developed neurological signs suggestive of neurotoxicity. Subsequently, concentrations of 2.5, 5, 10, 12.5 and 25 mM, dissolved in 10, 20, 40, 50 and 100% DMSO, respectively, corresponding to a drug dose of 12.5, 25, 50, 62.5 and 125 nmol are used. For testing DMSO toxicity, groups of three mice are injected with 5 uL PBS, 50% DMSO in PBS or 100% DMSO in PBS. Mice are culled 9 days after injection and coronally sectioned brains are stained for cleaved caspase 3, GFAP and Iba1.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 98.32%

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Keywords:

EndoxifenEstrogen Receptor/ERRParasiteDrug MetaboliteInhibitorinhibitorinhibit

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Endoxifen hydrochloride
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