research use only
Cat.No.S1188
| Related Targets | Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR |
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| Other Aromatase Inhibitors | Obacunone (AI3-37934) Fadrozole (CGS16949A) alpha-Naphthoflavone |
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In vitro |
DMSO
: 59 mg/mL
(201.11 mM)
Ethanol : 59 mg/mL Water : Insoluble |
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In vivo |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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| Molecular Weight | 293.37 | Formula | C17H19N5 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 120511-73-1 | Download SDF | Storage of Stock Solutions |
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| Synonyms | ZD-1033 | SMILES | CC(C)(C#N)C1=CC(=CC(=C1)CN2C=NC=N2)C(C)(C)C#N | ||
Read more about storage stability stock solution CAS number SMILES
| Targets/IC50/Ki |
Aromatase
(human placental microsomes) 15 nM
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|---|---|
| In vitro |
Anastrozole has high intrinsic potency in vitro and inhibits human placental aromatase with an IC50 of 15 nM. This compound is 200 times as potent as AG, twice as potent as 4-OHA and one third as potent as fadrozole. . This chemical inhibits aromatase by binding competitively to the hem group of the CYP unit of the enzyme thereby reducing estrogen biosynthesis in the periphery and the breast. It has little or no effect on other steroid hormones.
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| In vivo |
Anastrozole (0.1 mg/kg) given orally to mature rats on Day 2 or 3 of the estrous cycle, blocked ovulation in mature females; in pubertal rats, the same dose given for 3 days completely blocks androstenedione-stimulated uterine development. These effects may be attributes to inhibition of the normal preovulatory rise in ovarian follicular estrogen synthesis in mature females and to inhibition of metabolism of the exogenous androstenedione by the immature ovary in prepubertal females. Twice-daily administration of >9.1 mg/kg of this compound given orally to male pigtailed monkeys inhibits peripheral aromatase, thereby reducing circulating estradiol concentrations by 50% to 60%.
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References |
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(data from https://clinicaltrials.gov, updated on 2025-09-29)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT07190443 | RECRUITING | Breast Cancer; Locoregional Recurrence; Abemaciclib; Endocrine Therapy |
Japanese Foundation for Cancer Research |
2025-02-07 | PHASE3 |
| NCT05512364 | RECRUITING | ER-positive Breast Cancer; HER2-negative Breast Cancer; Stage IIB Breast Cancer; Stage III Breast Cancer |
European Organisation for Research and Treatment of Cancer - EORTC |
2023-12-15 | PHASE3 |
| NCT06223698 | NOT_YET_RECRUITING | Breast Cancer |
Region Örebro County |
2025-05-02 | PHASE3 |
| NCT07729046 | NOT_YET_RECRUITING | Metastatic Invasive Breast Cancer; Resistant Breast Cancer; ER+, HER2-, Metastatic Breast Cancer |
University of California, San Diego |
2027-07 | PHASE2 |
| NCT07581834 | RECRUITING | Breast Diseases; Breast Neoplasms; Dalpiciclib; Endocrine Breast Diseases; CDK4/6 Inhibitor; HR+/HER2- Breast Cancer |
Fujian Cancer Hospital |
2026-01-21 | PHASE2 |
| NCT07179939 | NOT_YET_RECRUITING | HER2-positive Breast Cancer |
Fudan University |
2025-09-10 | PHASE2 |
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