AZD8186
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.
AZD8186对PI3Kβ和PI3Kδ的IC50值分别为0.003 μM和0.017 μM.
PI3K-Akt信号通路在细胞生长\增殖\运动以及存活方面起着关键作用.在人类癌症中,上述通路由多种机制激活,包括体细胞突变\缺失以及扩增.I类PI3K可进一步划分为IA类酶(PI3Kα\PI3Kβ和PI3Kδ)和IB类酶(PI3Kγ).AZD8186是一种有效的PI3Kβ和PI3Kδ选择性抑制剂.
体外:在PI3Kβ抑制敏感性细胞以及PI3Kδ抑制敏感性细胞中,AZD8186有效地抑制p-Akt,但对PI3Kα抑制敏感性细胞无效.使用多种重组蛋白和脂质激酶测定AZD8186的整体激酶选择性.在59种蛋白激酶中,1 μM的AZD8186没有显示出显著的抑制活性[1].
体内:在PTEN缺失的PC3前列腺肿瘤异种移植裸鼠模型中,评价AZD8186的抗肿瘤活性,给予100 mg/kg AZD8186(不给予ABT),每天2次,或给予60 mg/kg\30 mg/kg以及10 mg/kg AZD8186(同时给予ABT),每天2次.相对于100 mg/kg组(不同时给予ABT),60 mg/kg组和30 mg/kg组(同时给予ABT)具有较高的抑制作用[1].
临床试验:AZD8186有望用于治疗PTEN缺失的癌症,最近已进入I期临床试验[1].
参考文献:
[1] Barlaam B, Cosulich S, Degorce S, Fitzek M, Green S, Hancox U, Lambert-van der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Pasquet MJ, Péru A, Plé P, Saleh T, Vautier M, Walker M, Ward L, Warin N. Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl -2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers. J Med Chem. 2015 Jan 22;58(2):943-62.
[2] https://clinicaltrials. gov/ct2/show/NCT01884285term=AZD8186&rank=1
Storage | Store at -20°C |
M.Wt | 457.47 |
Cas No. | 1627494-13-6 |
Formula | C24H25F2N3O4 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥45.7 mg/mL in DMSO with ultrasonic |
Chemical Name | (R)-8-(1-((3,5-difluorophenyl)amino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide |
SDF | Download SDF |
Canonical SMILES | C[C@](NC1=CC(F)=CC(F)=C1)([H])C2=C3C(C(C=C(O3)N4CCOCC4)=O)=CC(C(N(C)C)=O)=C2 |
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。 |
质量控制和MSDS
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