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- 2026年07月07日
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- CAS号：
1082948-81-9
- 规格：
25mg/50mg/100mg
| 规格： | 25mg | 产品价格： | ￥8480.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥11040.0 |
| 规格： | 100mg | 产品价格： | ￥14000.0 |
Product Introduction
Bioactivity
| 名称 | LY-2584702 hydrochloride |
| 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. |
| 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]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 关键字 | S6Kinase | S6K1 | S6 Kinase | p70S6K | LY-2584702 Hydrochloride | LY2584702 Hydrochloride | LY 2584702 hydrochloride |
| 相关产品 | MBM-55S | Carnosol | Prexasertib dihydrochloride | Sodium salicylate | RMC-7977 | CHIR-98014 | Bimiralisib | SB 699551 dihydrochloride | Quercitrin | GSK269962A | Gossypin | FMK |
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文献和实验使用它的拮抗剂或抑制剂去反复证明，LY就是其中之一，而这些保护药的拮抗剂或抑制剂当然是不会用于人身上的，要不然细胞实验和动物实验还有什么意义呢？ shaaou tom88339 wrote: 很奇怪很多人总是用DMSO来作溶剂来做药理的实验。 不溶的化合物要用乳化剂、助悬剂或增溶剂来分散或溶解。乳化剂可用泊洛沙姆、助悬剂常用CMCNa，增溶剂可选用吐温８０或CO40。
以及活化过程中，出现或消失的细胞表面标记。它们大都是穿膜的蛋白或糖蛋白，含胞膜外区、穿膜区和胞浆区。有些白细胞分化抗原是以磷脂酰肌醇（inositol phospholipids,IP）连接方式“锚”在细胞膜上。少数白细胞分化抗原是碳水化合物半抗原。白细胞分化抗原参与机体重要的生理和病理过程。例如：①免疫应答过程中免疫细胞的相互识别，免疫细胞抗原识别、活化、增殖和分化，免疫效应功能的发挥；②造血细胞的分化和造血过程的调控；③炎症发生；④细胞的迁移如肿瘤细胞的转移。 一、人白细胞分化抗原
区。有些白细胞分化抗原是以磷脂酰肌醇（inositol phospholipids,IP）连接方式“锚”在细胞膜上。少数白细胞分化抗原是碳水化合物半抗原。白细胞分化抗原参与机体重要的生理和病理过程。例如：①免疫应答过程中免疫细胞的相互识别，免疫细胞抗原识别、活化、增殖和分化，免疫效应功能的发挥；②造血细胞的分化和造血过程的调控；③炎症发生；④细胞的迁移如肿瘤细胞的转移。 一、人白细胞分化抗原 80年代以来，由于单克隆抗体、分子克隆、基因转染细胞系等技术在白细胞分化抗原研究中
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