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Formestane

Cat. No. M3409

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Formestane Structure
Synonym:

4-hydroxyandrostenedione

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 30 In stock
25mg USD 50 In stock
50mg USD 75 In stock
100mg USD 110 In stock
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Quality Control & Documentation
Biological Activity

Formestane (Lentaron (R)) is a second generation selective aromatase inhibitor with an IC50 of 80 nM. Formestane (Lentaron (R)) is used in the treatment of estrogen-receptor positive breast cancer in post-menopausal women. Formestane (Lentaron (R)) is often used to suppress estrogen production from anabolic steroids or prohormones. Formestane (Lentaron (R)) also acts as a prohormone to 4-hydroxytestosterone, an active steroid which displays weak androgenic activity in addition to acting as a mild aromatase inhibitor. Formestane has poor oral bioavailability and as such is no longer popular as many orally active aromatase inhibitors have been identified. Cells were treated with different aromatase inhibitors anastrozole, formestane, exemestane, and letrozole, or antiestrogens tamoxifen and fulvestrant. UMB-1Ca cells showed significant growth inhibition in response to fulvestrant (100 nM, P < 0.0005) and partial growth inhibition in response to letrozole (100 nM, P < 0.005).

Product Citations
Chemical Information
Molecular Weight 302.41
Formula C19H26O3
CAS Number 566-48-3
Solubility (25°C) DMSO 55 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Rajeev Kharb, et al. Aromatase inhibitors: Role in postmenopausal breast cancer

[2] X de la Torre, et al. Metabolism of formestane in humans: Identification of urinary biomarkers for antidoping analysis

[3] Xavier de la Torre, et al. Detection of formestane abuse by mass spectrometric techniques

[4] L R Wiseman, et al. Formestane. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the management of breast cancer and prostatic cancer

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Keywords: Formestane, 4-hydroxyandrostenedione supplier, inhibitors, activators

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