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Endoxifen Z-isomer hydrochloride

Cat. No. M6710
Endoxifen Z-isomer hydrochloride Structure
Synonym:

Endoxifen Z-isomer HCl

Size Price Availability
10mg USD 105  USD105 4-7 Days
25mg USD 215  USD215 4-7 Days
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Quality Control & Documentation
Biological Activity

Endoxifen Z-isomer 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.

Chemical Information
Molecular Weight 409.95
Formula C25H28ClNO2
CAS Number 1032008-74-4
Solubility (25°C) DMSO ≥ 33 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Chae YJ, et al. Eur J Pharmacol. Endoxifen, the active metabolite of tamoxifen, inhibits cloned hERG potassium channels.

[2] Ali SM, et al. Bioorg Med Chem Lett. Endoxifen is a new potent inhibitor of PKC: a potential therapeutic agent for bipolar disorder.

[3] Ahmad A, et al. Breast Cancer Res Treat. Orally administered endoxifen is a new therapeutic agent for breast cancer.

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