A non-steroidal aromatase inhibitor
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Fadrozole (hydrochloride)

Item No. 24272

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)-benzonitrile, monohydrochloride
CAS Number
102676-31-3
Synonyms
  • CGS 16949A
Molecular Formula
C14H13N3 • HCl
Formula Weight
259.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 10 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.3 mg/mlEthanol: 2 mg/ml
λmax
229 nm
SMILES
N#CC(C=C1)=CC=C1C(CCC2)N3C2=CN=C3.Cl
InChi Code
InChI=1S/C14H13N3.ClH/c15-8-11-4-6-12(7-5-11)14-3-1-2-13-9-16-10-17(13)14;/h4-7,9-10,14H,1-3H2;1H
InChi Key
UKCVAQGKEOJTSR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $70

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    10 mg

    $120

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    Product Description

    Fadrozole is a non-steroidal aromatase inhibitor (IC50s = 5 and 1.4 nM for human placental and rat ovarian microsomal aromatase, respectively).1,2 It selectively inhibits estrogen over progesterone production induced by luteinizing hormone (LH) in hamster ovarian tissue as well as corticosterone and aldosterone production induced by adrenocorticotropic hormone (ACTH; Item No. 24257) in rat adrenal tissue (IC50s = 0.03, 160, 100, and 1 μM, respectively).1 It also decreases ovarian estrogen levels in rats when administered at a dose of 0.26 mg/kg.2 Fadrozole inhibits conversion of cholesterol to 27-hydroxycholesterol by the cytochrome P450 (CYP) isomer 27A1 (Ki = 4.6 μM).3 It inhibits growth of androstenedione-stimulated mammary D2 cells implanted into thoracic mammary fat pads of mice by 95% when administered at a dose of 0.5 mg per animal per day.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bhatnagar, A.S., Häusler, A., Schieweck, K., et al. Highly selective inhibition of estrogen biosynthesis by CGS 20267, a new non-steroidal aromatase inhibitor. J. Steroid Biochem. Mol. Biol. 37(6), 1021-1027 (1990).

    2. Steele, R.E., Mellor, L.B., Sawyer, W.K., et al. In vitro and in vivo studies demonstrating potent and selective estrogen inhibition with the nonsteroidal aromatase inhibitor CGS 16949A. Steroids 50(1-3), 147-161 (1987).

    3. Mast, N., Lin, J.B., and Pikuleva, I.A. Marketed drugs can inhibit cytochrome P450 27A1, a potential new target for breast cancer adjuvant therapy. Mol. Pharmacol. 88(3), 428-436 (2015).

    4. Tekmal, R.R., and Durgam, V.R. A novel in vitro and in vivo breast cancer model for testing inhibitors of estrogen biosynthesis and its action using mammary tumor cells with an activated int-5/aromatase gene. Cancer Lett. 118(1), 21-28 (1997).