Endoxifen (Z-isomer hydrochloride) [CAS 1032008-74-4]
Endoxifen (Z-isomer hydrochloride) [CAS 1032008-74-4]
SKU:QM-0155099-01
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Product Details
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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]
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CAS Number
[1032008-74-4]
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Molecular Formula
C25H28ClNO2
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Molecular Weight
409.95
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Smiles
OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)\CC)C=C1.[H]Cl
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Target
Estrogen Receptor/ERR; Potassium Channel
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Concentration
10mM
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Purity
99.67
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Solubility
DMSO : 100 mg/mL (ultrasonic)
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Storage Conditions
4°C (Powder, sealed storage, away from moisture)
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Shipping Conditions
Room Temperature
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Hazard Statement
H350, H360, H410
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Precautions
H350, H360, H410
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Endoxifen (Z-isomer hydrochloride) [CAS 1032008-74-4]
Endoxifen (Z-isomer hydrochloride) is a premium-grade research compound supplied by Quantimol for laboratory and scientific applications.