Fadrozole is a nonsteroidal aromatase inhibitor. Fadrozole is a very potent and highly selective inhibitor of the aromatase enzyme system in vitro and estrogen biosynthesis in vivo. It inhibited the conversion of [4-14C]androstenedione to [4-14C]estrone by human placental microsomes in a competitive manner (Ki = 1.6 nM). At a substrate concentration 3-fold the Km, Fadrozole was 180 times more potent, as an inhibitor, than aminoglutethimide (Cat. No. A9657), exhibiting half-maximal inhibition at 1.7 nM as compared to 0.3 μM. In vivo, Fadrozole lowered ovarian estrogen synthesis by gonadotropin-primed, androstenedione treated, immature rats by 90% at a dose of 260 μg/kg (PO). In vivo, Fadrozole leads to sequelae of estrogen deprivation (e.g. regression of DMBA-induced mammary tumors) without causing adrenal hypertrophy in adult rats. It blocked aromatase by 50% in human breast cancer homogenates, live breast cancer cells, human placental microsomes, and porcine ovarian microsomes at concentrations of 0.008 to 0.02 μM.
| Molecular Weight | 259.73 |
| Formula | C14H13N3·HCl |
| CAS Number | 102676-31-3 |
| Solubility (25°C) | DMSO: ≥20 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
| Related Products |
|---|
| Isothiuronium
Isothiouronium is a functional group, it is the acid salt of isothiourea. |
| Sultosilic acid, piperazine salt
Sultosilic acid piperazine salt is a compound with lowering lipid activity. It causes significant shortening of the euglobulin lysis time and a significant diminution of platelet adhesiveness, as well as statistically significant decrease of triglycerides, total cholesterol, beta- and pre-beta-cholesterol and an increase of alpha-cholesterol. |
| Ipamorelin
Ipamorelin (NNC-26-0161) is a a novel and potent ghrelin mimetic peptide compound that counteracts glucocorticoid-induced decrease in bone formation of adult rats. |
| PRGL493
PRGL493 is a potent and selective long-chain acyl-CoA synthetase 4 (ACSL4) inhibitor. PRGL493 blocks cell proliferation and tumor growth in both breast and prostate cellular and animal models. |
| Hercynine
Hercynine is a natural product, found in the fine leaf algae, Schizosaccharomyces cerevisiae and honey bees, and is a precursor of L-(+)-ergothioneine. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
