AZD9496
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
对ERα结合、ERα下调、ERα拮抗作用,IC50分别为0.82、0.14和0.28 nM。
AZD9496是一种口服活性雌激素受体抑制剂。
雌激素受体(ER)是一组存在于细胞内和细胞上的蛋白质,是被激素雌激素活化的受体。研究发现ER在约70%的乳腺癌病例中过表达,称为“ER阳性”。
体外:经鉴定,AZD9496是ERα的非甾体小分子抑制剂,是一种强效的和选择性的ERα拮抗剂和下调剂。此外,AZD9496可以结合和下调临床相关的ESR1突变体[1]。
体内:动物研究报道,在雌激素依赖性MCF-7异种移植模型中观察到低至0.5 mg/kg剂量的AZD9496显著的肿瘤生长抑制,并且这种效用伴随PR蛋白水平的剂量依赖性降低,提供强效的拮抗剂活性。此外,与单一疗法相比,AZD9496与PI3K途径和CDK4/6抑制剂联合用药导致进一步的生长抑制作用。此外,在长期雌激素剥夺的乳腺模型中还观察到肿瘤消退,其中发现显著的ERα蛋白下调[1]。
临床试验:AZD9496目前正在I期临床试验中,以评估不同形式和制剂的PK和安全性[2]。
参考文献:
[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/NCT02780713term=AZD9496&rank=2
Storage | Store at -20°C |
M.Wt | 442.47 |
Cas No. | 1639042-08-2 |
Formula | C25H25F3N2O2 |
Solubility | Soluble in DMSO |
Chemical 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 |
SDF | Download SDF |
Canonical SMILES | O=C(O)/C=C/C1=CC(F)=C([C@H]2N(CC(C)(F)C)[C@H](C)CC3=C2NC4=CC=CC=C34)C(F)=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |