TTP 22
(Synonyms: TTP22;TTP-22) 目录号 : GC10649A CK2 inhibitor
Cas No.:329907-28-0
Sample solution is provided at 25 µL, 10mM.
IC50= 0.1 μM; Ki= 40 nM
TTP 22 is a high affinity, ATP-competitive casein kinase 2 (CK2) inhibitor.
Casein kinase 2 (CK2) noticeably stands out against a background of the kinase family due to its constitutive catalytic activity with the ability to phosphorylate more than 300 physiological substrates. These features make CK2 appear greatly diverse points of cell signaling pathways and be involved in processes leading to the development of various disorders, especially cancer. Thus, currently CK2 is regarded as druggable protein kinase target and can be used for the development of antitumor, anti-inflammatory and antiviral drugs.
In vitro: Kinetic studies of TTP 22 showed that activity of (thieno[2,3-d]pyrimidin-4-ylthio)carboxylic acids moiety was a result of its competition with ATP molecule for the binding site. Inhibition constant (Ki) for TTP 22 was 40 nM. Initial in vitro tests of TTP 22 and it analog on four serine/threonine (ASK1, JNK3, Aurora A and Rock 1) and three tyrosine protein kinases (FGFR1, Met and Tie2) revealed their remarkable specificity towards CK2 [1].
In vivo: So far, no animal in vivo study has been conducted for TTP 22.
Clinical trial: N/A
Reference:
[1] Golub AG,Bdzhola VG,Briukhovetska NV,Balanda AO,Kukharenko OP,Kotey IM,Ostrynska OV,Yarmoluk SM. Synthesis and biological evaluation of substituted (thieno[2,3-d]pyrimidin-4-ylthio)carboxylic acids as inhibitors of human protein kinase CK2. Eur J Med Chem.2011 Mar;46(3):870-6.
Cas No. | 329907-28-0 | SDF | |
别名 | TTP22;TTP-22 | ||
化学名 | 3-[5-(4-methylphenyl)thieno[2,3-d]pyrimidin-4-yl]sulfanylpropanoic acid | ||
Canonical SMILES | CC1=CC=C(C=C1)C2=CSC3=C2C(=NC=N3)SCCC(=O)O | ||
分子式 | C16H14N2O2S2 | 分子量 | 330.42 |
溶解度 | ≥ 16.5 mg/mL in DMSO, ≥ 7.85 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
General tips | 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。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.0265 mL | 15.1323 mL | 30.2645 mL |
5 mM | 0.6053 mL | 3.0265 mL | 6.0529 mL |
10 mM | 0.3026 mL | 1.5132 mL | 3.0265 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet