切换导航

LY2584702

现货
Catalog No.
B5815
P70 S6激酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,100.00
现货
5mg
¥ 750.00
现货
10mg
¥ 1,250.00
现货
25mg
¥ 2,500.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

LY2584702 is a potent and selective inhibitor of p70 S6 kinase with IC50 value of 4 nM [1].

P70 S6 kinase (p70S6K) is a serine/threonine protein kinase that acts downstream of the phosphatidylinositol-3-kinase (PI3K)/Akt/mTOR signalling pathway. p70S6K phosphorylates the eukaryotic initiation factor 4B (eIF4B), a regulator of protein synthesis, and phosphorylates and activates ribosomal protein S6 (S6), a component of the 40S ribosomal subunit [1] [2].

LY2584702 is an oral and selective ATP competitive p70S6K inhibitor. In HCT116 colon cancer cells, LY2584702 inhibits phosphorylation of S6 (pS6) with IC50 value of 0.1-0.24 μM [1].

In the HCT116 colon carcinoma xenograft model, LY2584702 significantly inhibited tumour growth with threshold minimum effective dose 50% (TMED50) and TMED90 of 2.3 mg/kg and 10 mg/kg, respectively. In both HCT116 colon carcinoma and U87MG glioblastoma xenograft models, LY2584702 at levels of 2.5 mg/kg twice daily (BID) and 12.5 mg/kg BID exhibited significant efficacy. Treatment patients with advanced solid tumours with LY2584702 orally on a 28-day cycle, the maximum tolerated dose (MTD) was 75 mg BID (twice-daily) or 100 mg QD (once-daily) [1].

References:
[1].  Tolcher A, Goldman J, Patnaik A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumours. Eur J Cancer, 2014, 50(5): 867-875.
[2].  Hollebecque A, Houédé N, Cohen EE, et al. A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours. Eur J Cancer, 2014, 50(5): 876-884.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt445.42
Cas No.1082949-67-4
FormulaC21H19F4N7
Solubility≥22.25mg/mL in DMSO
Chemical Name4-(4-(4-(4-fluoro-3-(trifluoromethyl)phenyl)-1-methyl-1H-imidazol-2-yl)piperidin-1-yl)-2H-pyrazolo[3,4-d]pyrimidine
SDFDownload SDF
Canonical SMILESCN(C(C1CCN(C2=NC=NC3=NNC=C32)CC1)=N4)C=C4C5=CC(C(F)(F)F)=C(F)C=C5
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

细胞实验[1]:

细胞系

HCT116结肠癌细胞

溶解方法

在DMSO中的溶解度>22.3mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

N/A

应用

在HCT116结肠癌细胞中,LY2584702抑制S6核糖体蛋白的磷酸化(pS6),IC50为0.1-0.24μM。

动物实验[1]:

动物模型

U87MG胶质母细胞瘤和HCT116结肠癌异种移植模型

剂量

2.5 mg/kg每天2次,12.5 mg/kg每天2次

应用

在U87MG胶质母细胞瘤和HCT116结肠癌异种移植模型中,LY2584702显示出显著的单一药效。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Tolcher A, Goldman J, Patnaik A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumours. Eur J Cancer, 2014, 50(5): 867-875.

质量控制

质量控制和MSDS

批次:

化学结构

LY2584702