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    Membrane Transporter/Ion Channel
  2. Estrogen Receptor/ERR
    Potassium Channel
  3. Endoxifen Z-isomer hydrochloride

Endoxifen Z-isomer hydrochloride 

Cat. No.: HY-18719A Purity: 99.31%
Handling Instructions

Endoxifen Z-isomer hydrochloride is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα).

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

Endoxifen Z-isomer hydrochloride Chemical Structure

Endoxifen Z-isomer hydrochloride Chemical Structure

CAS No. : 1032008-74-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 144 In-stock
Estimated Time of Arrival: December 31
1 mg USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 160 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

Other Forms of Endoxifen Z-isomer hydrochloride:

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Description

Endoxifen Z-isomer hydrochloride is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen inhibits hERG tail currents at 50 mV in a concentration-dependent manner with IC50 values of 1.6 μM. IC50 value: 1.6 μM [1] Target: hERG Potassium Channel, Estrogen Receptor/ERR Endoxifen is considered a prodrug, since it has a much higher potency for the estrogen receptor than its parent drug. Endoxifen inhibits the hERG channel protein trafficking to the plasma membrane in a concentration-dependent manner with Endoxifen being more potent than Tamoxifen. [1] Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. Additionally, low concentrations of Endoxifen observed in Tamoxifen treated patients with deficient CYP2D6 activity (20 to 40 nM) markedly inhibit estrogen-induced cell proliferation rates in the presence of ERβ, whereas much higher Endoxifen concentrations are needed when ERβ is absent.[2]

Molecular Weight

409.95

Formula

C₂₅H₂₈ClNO₂

CAS No.

1032008-74-4

SMILES

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

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 : 12.5 mg/mL (30.49 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

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    90% corn oil

    Solubility: ≥ 1.25 mg/mL (3.05 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.31%

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Product Name:
Endoxifen Z-isomer hydrochloride
Cat. No.:
HY-18719A
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