LY3023414
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.
作用于Akt1(pT308)、Akt1(pS473)、P70S6(pT389)和S6RP(pS240/242),IC50分别为64.9、42.1、10.6和19.1 nM。
LY3023414是I类PI3K亚型、mTOR和DNA-PK的ATP竞争性抑制剂。
磷酸肌醇-3激酶(PI3K)/AKT / mTOR通路是癌细胞生长和存活中最常改变的通路之一。
体外:在针对约266种激酶的生化测试中发现,低浓度LY3023414强效地和选择性地抑制I类PI3K亚型、mTORC1/2以及DNA-PK。此外,LY3023414抑制PI3K/AKT/mTOR信号传导导致G1细胞周期停滞,并导致癌细胞板中的广泛抗增殖活性[1]。
体内:LY3023414表现出对PI3K/AKT/mTOR途径下游底物的高生物利用度和剂量依赖性去磷酸化达4至6小时,表明LY3023414的半衰期为2小时。此外,在多种异种移植模型中每日一次或两次的LY3023414等效总日剂量给药可以抑制肿瘤生长至相似程度,证明间歇性靶标抑制对抗肿瘤活性是有效的[1]。
临床试验:LY3023414作为单剂量以高达325 mg QD或200 mg BID施用时是安全的。目前,LY3023414在乳腺癌、间皮瘤、非霍奇金淋巴瘤以及NSCLC的肿瘤特异性扩增队列中进行研究(临床试验信息:NCT01655225)。
参考文献:
[1] Smith MC,Mader MM,Cook JA,et al. Characterization of LY3023414, a Novel PI3K/mTOR Dual Inhibitor Eliciting Transient Target Modulation to Impede Tumor Growth. Mol Cancer Ther.2016 Oct;15(10):2344-2356.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 406.48 |
Cas No. | 1386874-06-1 |
Formula | C23H26N4O3 |
Solubility | ≥40.6 mg/mL in DMSO; insoluble in H2O; ≥28.9 mg/mL in EtOH |
Chemical Name | (S)-8-(5-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-(2-methoxypropyl)-3-methyl-1H-imidazo[4,5-c]quinolin-2(3H)-one |
SDF | Download SDF |
Canonical SMILES | O=C(N(C1=C2C3=CC(C4=CC(C(O)(C)C)=CN=C4)=CC=C3N=C1)C)N2C[C@H](C)OC |
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
- 批次: