| 中文名称: | GSK2334470 | ||||
|---|---|---|---|---|---|
| 英文名称: | GSK2334470 | ||||
| 别名: | GSK2334470 抑制剂;GSK2334470 国华试剂 (3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)pyrimidin-4-yl]-N-cyclohexyl-6-methylpiperidine-3-carboxamide | ||||
| CAS No: | 1227911-45-6 | 分子式: | C25H34N8O | 分子量: | 462.59 |
| CAS No: | 1227911-45-6 | ||||
| 分子式: | C25H34N8O | ||||
| 分子量: | 462.59 | ||||
基本信息
|
产品编号： |
G10774 |
||||
|
产品名称： |
GSK2334470 |
||||
|
CAS: |
1227911-45-6 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
|
|
||||
|
分子式： |
溶于液体 |
-80℃ |
6个月 |
||
|
分子量： |
462.59 |
-20℃ |
1个月 |
||
|
化学名： |
(3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)pyrimidin-4-yl]-N-cyclohexyl-6-methylpiperidine-3-carboxamide |
||||
|
Solubility (25°C)： |
|||||
|
体外:
|
DMSO |
92mg/mL (198.88mM) |
|||
|
Ethanol |
92mg/mL (198.88mM) |
||||
|
Water |
Insoluble |
||||
|
体内(现配现用): |
1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.5mg/mL(5.40mM);Clear solution |
||||
|
此⽅案可获得 ≥ 2.5 mg/mL (5.40 mM，饱和度未知) 的澄清溶液。 以 1 mL ⼯作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加⼊ 50 μ L Tween-80，混合均匀；然后继续加⼊ 450 μL ⽣理盐⽔定容⾄ 1 mL。 |
|||||
|
2.请依序添加每种溶剂：10% DMSO→90%(20% SBE-β-CD in saline) Solubility:≥2.5mg/mL(5.40mM);Clear solution |
|||||
|
此⽅案可获得 ≥ 2.5 mg/mL (5.40 mM，饱和度未知) 的澄清溶液。 以 1 mL ⼯作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均 匀。 |
|||||
|
3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2.5mg/mL(5.40mM);Clear solution |
|||||
|
此⽅案可获得 ≥ 2.5 mg/mL (5.40 mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1 mL ⼯作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ⽟⽶油中，混合均匀。 |
|||||
|
＜1mg/ml表示微溶或不溶。 |
|||||
|
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
|||||
|
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
|||||
制备储备液
|
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
|
1mM |
2.1617mL |
10.8087mL |
21.6174mL |
|
5mM |
0.4323mL |
2.1617mL |
4.3235mL |
|
10mM |
0.2162mL |
1.0809mL |
2.1617mL |
生物活性
|
产品描述 |
一种高效特异性的PDK1抑制剂，IC50值为10nM。 |
|
靶点 |
IC50:10nM(PDK1) |
|
体外研究 |
Small molecule GSK2334470 inhibits PDK1 with an IC50 of ~10nM,but does not suppress the activity of 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 500-fold higher concentrations.Addition of GSK2334470 ablates Tloop residue phosphorylation and activation of SGK isoforms and S6K1 induced by serum or IGF-1 (insulin-like growth factor 1).GSK2334470 and AZD8055 effectively inhibite phosphorylation of PDK1 and mTOR,respectively,and induce higher G0–G1 ratio in LAN-1-MK than that in LAN-1 as well.PDK1 and mTOR inhibitors effecte on phosphorylation of GSK3β in some of resistant sublines. |
|
体内研究 |
The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 is tested in newborn BrafV600E::Pten−/−mice subjected to systemic administration of 4-HT. Twice weekly administration of PDK1 results in marked inhibition of pigmented lesions and concomitant melanomagenesis,as well as significant inhibition of lung metastases,seen by H&E staining-based quantification (~80%),and lymph node metastases as by S100 immunostaining, similar to the phenotype seen upon genetic ablation of Pdk1. |
推荐实验方法(仅供参考)
|
细胞实验: |
|
|
GSK2334470 is dissolved in DMSO and diluted with appropriate medium before use.To study the inhibitory effect of GSK2334470 on mTOR-S6K pathway, non-resistant cells and the resistant sublines are treated with GSK2334470 at 5μM for 1.5 and 12h in 10 % FBS medium with/without MK-2206 (5μM). |
|
|
动物实验: |
|
|
Mice is dissolved in DMSO and then diluted with PBS or saline.BrafV600E:Pten−/−are generated as previously described.Cohorts of six animals per group are used in each experimental group.GSK2334470 is administered through IP injection (100mg/kg) 3 times per week starting the same day of topical administration of 4-hydroxytamoxifen and ending at the time of mouse collection,based on earlier studies. |
|
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
