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).
Plant J. 2022 Jun;110(6):1636-1650.
Small molecule RHP1 promotes root hair tip growth by acting upstream of the RHD6-RSL4-dependent transcriptional pathway and ROP signaling in plants
Formestane purchased from AbMole
| 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 |
| 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.
[1] Rajeev Kharb, et al. Aromatase inhibitors: Role in postmenopausal breast cancer
[3] Xavier de la Torre, et al. Detection of formestane abuse by mass spectrometric techniques
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