首页 工具
登录
购物车
LY-2584702 hydrochloride

LY-2584702 hydrochloride

产品编号 T11900   CAS 1082948-81-9

Ly-2584702 hydrochloride is a p70S6K selective ATP competitive inhibitor with IC50 of 4 nM.In the S6K1 enzyme assay, the IC50 of LY-2584702 was 2 nM.

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
LY-2584702 hydrochloride Chemical Structure
LY-2584702 hydrochloride, CAS 1082948-81-9
规格 价格/CNY 货期 数量
25 mg ¥ 10,600 6-8周
50 mg ¥ 13,800 6-8周
100 mg ¥ 17,500 6-8周

LY-2584702 hydrochloride 的其他形式现货产品:

LY-2584702 free base
其他形式的 LY-2584702 hydrochloride:
产品目录号及名称: LY-2584702 hydrochloride (T11900)
点击图片重新获取验证码
该分子属于定制产品。陶术拥有优秀的合成团队,经验和能力,可以为您提供高性价比的产品。但由于客观因素,研发中会存在小概率合成不成功的情况,还请理解,如您有任何问题,欢迎咨询,我们将竭诚为您服务。
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Ly-2584702 hydrochloride is a p70S6K selective ATP competitive inhibitor with IC50 of 4 nM.In the S6K1 enzyme assay, the IC50 of LY-2584702 was 2 nM.
靶点活性 S6K1:2 nM, p70 S6K:4 nM
体外活性 LY-2584702 has some activity against the S6K-related kinases MSK2 and RSK at high concentrations (enzyme assay IC50=58-176 nM).?LY-2584702 inhibits S6K activity in EOMA cells, as determined by the phosphorylation of its downstream effector S6, in a dose-dependent manner[2].?Proliferation of A549 is significantly inhibited by LY-2584702 ?treating over 24 h at 0.1 μM (P<0.05);?and the trend of decline is more conspicuous with longer treatment and/or with the increased drug concentration (all P<0.05).?Similar results are also observed in SK-MES-1, although the obvious inhibition is led by LY-2584702 at 0.6 μM (P<0.05), much higher than that of A549[3].LY-2584702 ?inhibits phosphorylation of the S6 ribosomal protein (pS6) in HCT116 colon cancer cells with an IC50 of 0.1-0.24 μM[1].?In S6K1 enzyme assay, the IC50 of LY-2584702 ?is 2 nM.?For pS6 inhibition in cells, the IC50=100 nM.
体内活性 LY-2584702 demonstrates significant single-agent efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models at two dose levels of 2.5 mg/kg twice daily (BID) and 12.5 mg/kg BID.?LY-2584702 demonstrates statistically significant tumour growth reduction at TMED50 (threshold minimum effective dose 50%) (2.3 mg/kg) and TMED90 (10 mg/kg) in the HCT116 colon carcinoma xenograft model[1].?To examine the role of S6K in vivo, EOMA cells expressing shAkt3 are implanted in nu/nu mice, then treated for 14 days with LY-2584702 or Rapamycin.?Analysis of tumors removed after 14 days shows that LY-2584702 inhibits S6 phosphorylation almost as effectively as Rapamycin.?Loss of Akt3 increases tumor growth as compared with pLKO.?LY-2584702 treatment alone does not significantly affect the growth of pLKO tumors.?However, LY-2584702 significantly reduces the growth of tumors with shAkt3[2].
分子量 481.88
分子式 C21H20ClF4N7
CAS No. 1082948-81-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Tolcher A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumors. Eur J Cancer. 2014 Mar;50(5):867-75. 2. Phung TL, et al. Akt1 and akt3 exert opposing roles in the regulation of vascular tumor growth. Cancer Res. 2015 Jan 1;75(1):40-50. 3. Chen B, et al. Hyperphosphorylation of RPS6KB1, rather than overexpression, predicts worse prognosis in non-small cell lung cancer patients. PLoS One. 2017 Aug 9;12(8):e0182891.
Sodium salicylate Eudesmin AT13148 CKI-7 H-89 dihydrochloride BI-D1870 LJH685 Carnosol

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

LY-2584702 hydrochloride 1082948-81-9 MAPK PI3K/Akt/mTOR signaling S6 Kinase LY 2584702 hydrochloride LY2584702 Hydrochloride LY 2584702 Hydrochloride LY2584702 hydrochloride LY-2584702 Hydrochloride Inhibitor inhibitor inhibit

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼