Name: AZD9496
Price: 276.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    IC50: 0.82, 0.14 and 0.28 nM for ERα binding, ERα downregulation, ERα antagonism, respectivelyAZD9496 is an orally active estrogen receptor inhibitor. Estrogen receptors (ERs) are a group of proteins presented inside and on cells, and they are receptors that are activated by the hormoneestrogen. ERs are found to be over-expressed in about 70% of breast cancer cases, referred to as "ER-positive".In vitro: AZD9496 was identified as a nonsteroidal small-molecule inhibitor of ERα, which was a potent and selective antagonist and downregulator of ERα. In addition, AZD9496 could bind and downregulate clinically relevant ESR1 mutants [1]. In vivo: Animal study reported that significant tumor growth inhibition was observed as low as 0.5 mg/kg dose of AZD9496 in the estrogen-dependent MCF-7 xenograft model, and such effect was accompanied by a dose-dependent decrease in PR protein levels, providing potent antagonist activity. In addition, the combination of AZD9496 with PI3K pathway and CDK4/6 inhibitors resulted in further growth-inhibitory effects when compared with monotherapy alone. Furthermore, the tumor regression was also observed in a long-term estrogen-deprived breast model, in which significant ERα protein downregulation was found [1]. Clinical trial: AZD9496 is currently being evaluated in a phase I clinical trial to assess the PK and safety of different forms and formulations [2].
    
    [1] Weir HM et al. AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models. Cancer Res. 2016 Jun 1;76(11):3307-18.
    [2] https://clinicaltrials. gov/ct2/show/NCT02780713 term=AZD9496&rank=2
- Properties
  - Alternative Name
    
    (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic acid
    
    CAS Number
    
    1639042-08-2
    
    Molecular Formula
    
    C25H25F3N2O2
    
    Molecular Weight
    
    442.47
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

AZD9496

AZD9496

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