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

Endoxifen Z-isomer 

Cat. No.: HY-18719
Handling Instructions

Endoxifen Z-isomer 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 Chemical Structure

Endoxifen Z-isomer Chemical Structure

CAS No. : 112093-28-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 131 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
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Endoxifen Z-isomer:

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Description

Endoxifen Z-isomer 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 Z-isomer 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 Z-isomer 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 Z-isomer concentrations are needed when ERβ is absent.[2]

Molecular Weight

373.49

Formula

C₂₅H₂₇NO₂

CAS No.

112093-28-4

SMILES

OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)\CC)C=C1.[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 : 50 mg/mL (133.87 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6774 mL 13.3872 mL 26.7745 mL
5 mM 0.5355 mL 2.6774 mL 5.3549 mL
10 mM 0.2677 mL 1.3387 mL 2.6774 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 (6.69 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.69 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Endoxifen Z-isomer
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HY-18719
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