Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TP3654是一种Pim 激酶抑制剂,对Pim-1和Pim-3的Ki 值分别为5和42 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 259 | 现货 | ||
5 mg | ¥ 589 | 现货 | ||
10 mg | ¥ 885 | 现货 | ||
25 mg | ¥ 1,790 | 现货 | ||
50 mg | ¥ 2,790 | 现货 | ||
100 mg | ¥ 4,230 | 现货 | ||
500 mg | ¥ 9,170 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 663 | 现货 |
产品描述 | TP-3654 is a second-generation Pim kinase inhibitor (Ki values against Pim-1/3: 5/42 nM). |
靶点活性 | Pim1:5 nM (Ki), Pim3:42 nM (Ki), Pim2:239 nM (Ki) |
体外活性 | TP-3654 shows potent PIM-1 specific cellular activity in the PIM-1/BAD overexpression system with an average EC50 of 67 nM. TP-3654 treatment reduces levels of phospho-BAD in vitro using the bladder cancer cell line UM-UC-3. TP-3654 reduces colony growth of T24 and UM-UC3 cells, confirming the PIM-1–dependent growth for both cell lines [1]. |
体内活性 | TP-3654 (200 mg/kg, i.g.) significantly reduces both UM-UC-3 and PC-3 tumour growth measured by volume (calliper) and by final tumour weight, with no significant changes in body weight or gross adverse toxicity[1]. |
细胞实验 | 1 μM TP-3654 is tested against 336 kinases at a concentration of 10 μM ATP. IC50 determinations of phosphoinositide 3-kinase (PI3K) (α, β, δ, and γ) and all kinases inhibited by >50% from the initial screen are performed using 10-dose, three-fold serial dilutions of TP-3654 starting with 10 μM at Km ATP concentrations for each kinase[1]. |
动物实验 | When tumours of mice reach 100 to 200 mm3 by calliper measurement, mice are randomized and oral dosing of TP-3654 or vehicle control began and continued every day for 5 days with 2 days off for 18 to 21 days. Tumour volumes and body weights were determined twice a week[1]. |
分子量 | 418.46 |
分子式 | C22H25F3N4O |
CAS No. | 1361951-15-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (131.43 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3897 mL | 11.9486 mL | 23.8971 mL | 59.7429 mL |
5 mM | 0.4779 mL | 2.3897 mL | 4.7794 mL | 11.9486 mL | |
10 mM | 0.239 mL | 1.1949 mL | 2.3897 mL | 5.9743 mL | |
20 mM | 0.1195 mL | 0.5974 mL | 1.1949 mL | 2.9871 mL | |
50 mM | 0.0478 mL | 0.239 mL | 0.4779 mL | 1.1949 mL | |
100 mM | 0.0239 mL | 0.1195 mL | 0.239 mL | 0.5974 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
TP-3654 1361951-15-6 Chromatin/Epigenetic JAK/STAT signaling Pim inhibit Pim kinases TP 3654 Inhibitor TP3654 inhibitor