货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T95801-1ml促销	10mM in DMSO	￥720.00 ￥648.00 T95801-1ml ￥648.00 现货	5 5	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T95801-1ml促销

10mM in DMSO

￥720.00 ￥648.00

产品描述：

DNA-PK 抑制剂;DNA-PK Inhibitors;;InformationSamotolisib (LY3023414) Samotolisib (LY3023414, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK .Targetsclass I PI3K isoforms ; mTOR kinase ; DNA-PKIn vitroLY3023414 shows high solubility across a wide pH range. inhibition of PI3K/AKT/mTOR signaling by LY3023414 causes G1 cell-cycle arrest and resulted in broad antiproliferative activity in cancer cell panel screens. In cell-based assays, LY3023414 inhibition of PI3K and mTOR is assessed in the PTEN-deficient U87 MG glioblastoma cell line. LY3023414 inhibits the phosphorylation ofAKT at position T308 downstream of PI3K at an IC50 of 106 nM. Similarly, LY3023414 inhibits phosphorylation of AKT at position S473 (IC50 = 94.2 nM) by mTORC2 as well as phosphorylation of mTORC1 kinase targets p70S6K (position T389; IC50 =10.6 nM) and 4E-BP1 (positions T37/46; IC50 = 187 nM). The downstream phosphorylation of S6RP at positions pS240/244 (IC50 = 19.1 nM) by p70S6K was inhibited as well, indicating target inhibition along the entire PI3K/AKT/mTOR pathway by LY3023414.In vivoLY3023414 demonstrates high bioavailability and dose-dependent dephosphorylation of PI3K/AKT/mTOR pathway downstream substrates such as AKT, S6K, S6RP, and 4E-BP1 for 4 to 6 hours, reflecting the drug\'s half-life of 2 hours. Intermittent target inhibition is sufficient for its antitumor activity. LY3023414 shows time- and dose-dependent target inhibition in vivo. It is currently being evaluated in phase 1 and 2 trials for the treatment of human malignancies.

体内研究：

Samotolisib (LY3023414) 抑制肿瘤生长的能力在几种表现出激活 PI3K/Akt/mTOR 通路的突变或缺失的异种移植模型中进行了研究。在 PTEN 缺失的 U87 MG 异种移植模型中，每天两次口服 Samotolisib，剂量为 3、6 或 10 mg/kg，持续 28 天，导致肿瘤生长出现剂量反应性抑制。这种处理在表现出 PTEN 截断 (786-O)、激活 PI3Kα 突变 (NCI-H1975) 和转基因 Eu-myc 突变体 PI3Kα 驱动的白血病模型的模型中产生相似的 TGI。

保存条件：

避光,-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.46 ml	12.301 ml	24.601 ml
5 mM	0.492 ml	2.46 ml	4.92 ml
10 mM	0.246 ml	1.23 ml	2.46 ml
50 mM	0.049 ml	0.246 ml	0.492 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

质检证书(COA)

输入产品批号：

如何获取质检证书(COA)?

请输入货号和一个与之匹配的批号。
例如:
批号：JS298415 货号：S20001-25g
在货品标签上如何找到货号和批号?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置