Lck Inhibitor
(Synonyms: 6-(2,6-二甲基苯基)-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-嘧啶并[5',4':5,6]嘧啶并[1,2-A]苯并咪唑-5(6H)-酮) 目录号 : GC13117
A selective inhibitor of lymphocyte-specific protein tyrosine kinase
Cas No.:847950-09-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Lck Inhibitor is a small-molecule inhibitor of with IC50 value of 7 nM [1].
The lymphocyte specific kinase which expressed in NK cells and T-cells is a member of the Src kinase family. It takes participate in the T-cell receptor (TCR) signal transduction and affects the expression of genes associated with cell proliferation, cytokine release and T-cell survival. Therefore small-molecule inhibitors of Lck with potent activities and bioavailable efficacies have been designed and developed as therapeutic agents for the treatment for T-cell-mediated autoimmune and organ transplant rejection [1].
Lck Inhibitor showed high selectivity against Lck over another Src family kinase Src and the kinases related to inflammation and angiogenesis such as p38 and VEGFR-2 with IC50 values of 0.12, > 10 and 5.1 μM, respectively. Lck Inhibitor also showed more than 1000-fold greater selectivity over CDK, MAPK and the RSK family. In cultured human mixed lymphocytes, the inhibitor significantly suppressed the activation of T-cells with IC50 value of 47 nM. Besides that, this compound inhibited IL-2 secretion induced by T-cell receptor with IC50 value of 0.46 μM. The good potency and selectivity of the Lck Inhibitor were due to the critical aniline side chain within a N-methylpiperazine moiety. It extended to the ATP-binding pocket of the enzyme and formed hydrogen bond interactions with the linker region [1].
In rats model with arthritis induced by the injection of porcine type II collagen, oral administration of the compound dose-dependently suppressed the inflammation with ED50 value of 3.2 mg/kg. While in the adjuvant-induced arthritis model, oral administration of Lck Inhibitor also displayed significant anti- arthritis effects with ED50 value of 24 mg/kg [1].
References:
[1] Martin M W, Newcomb J, Nunes J J, et al. Structure-Based Design of Novel 2-Amino-6-phenyl-pyrimido [5', 4': 5, 6] pyrimido [1, 2-a] benzimidazol-5 (6 H)-ones as Potent and Orally Active Inhibitors of Lymphocyte Specific Kinase (Lck): Synthesis, SAR, and In Vivo Anti-Inflammatory Activity. Journal of medicinal chemistry, 2008, 51(6): 1637-1648.
| Cas No. | 847950-09-8 | SDF | |
| 别名 | 6-(2,6-二甲基苯基)-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-嘧啶并[5',4':5,6]嘧啶并[1,2-A]苯并咪唑-5(6H)-酮 | ||
| 化学名 | 6-(2,6-dimethylphenyl)-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)benzo[4,5]imidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one | ||
| Canonical SMILES | O=C1N(C2=C(C([H])([H])[H])C([H])=C([H])C([H])=C2C([H])([H])[H])C3=NC4=C([H])C([H])=C([H])C([H])=C4N3C5=NC(N([H])C6=C([H])C([H])=C(C([H])=C6[H])N7C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C7([H])[H])=NC([H])=C51 | ||
| 分子式 | C31H30N8O | 分子量 | 530.62 |
| 溶解度 | DMF: 12 mg/ml,DMF:PBS(pH7.2) (1:2): 0.33 mg/ml,DMSO: 2.5 mg/ml,Ethanol: 0.33 mg/ml | 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。 |
||
| 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 | 1.8846 mL | 9.4229 mL | 18.8459 mL |
| 5 mM | 0.3769 mL | 1.8846 mL | 3.7692 mL |
| 10 mM | 0.1885 mL | 0.9423 mL | 1.8846 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。