AZD9496 |
Katalog-Nr.GC14405 |
AZD9496 ist ein potenter und selektiver Östrogenrezeptor (ERα)-Antagonist mit einem IC50 von 0,28 nM. AZD9496 ist ein oral bioverfÜgbarer selektiver Östrogenrezeptorabbauer (SERD).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1639042-08-2
Sample solution is provided at 25 µL, 10mM.
IC50: 0.82, 0.14 and 0.28 nM for ERα binding, ERα downregulation, ERα antagonism, respectively
AZD9496 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].
References:
[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
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