产品说明书
RK-24466
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同义名 : | KIN 001-51;LCK Inhibitor;KIN001 051, Lck Inhibitor;KIN001-051;RK-24466;Lymphocyte-specific Protein Tyrosine Kinase;C8863;Lck inhibitor C 8863 |
| CAS号 : | 213743-31-8 | |
| 货号 : | A724479 | |
| 分子式 : | C23H22N4O | |
| 纯度 : | 99%+ | |
| 分子量 : | 370.45 | |
| MDL号 : | MFCD04974490 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 45 mg/mL(121.47 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Lck is a src-family tyrosine kinase that predominantly expressed in T lymphocytes. The inhibition of lck activity prevents the activation of T cells, which might be used for the treatment of T-cell-dependent diseases. RK 24466 is a pyrrolopyrimidine that inhibits the activity of two forms of lck kinase, lck (64-509) and lckcd, with IC50 values of <1 nM and 2 nM, respectively. It also blocks kinases scr, kdr, and tie-2 with IC50 values of 0.07, 1.57, and 1.98 µM, respectively. RK 24466 showed much less inhibitory effect on the activities of EGFR, Zap70, PKC, and CDC2/CyB with IC50s values of 3.2 µM, >50 µM, >33 µM, and >50 µM, respectively[1]. The i.p. administration of RK 24466 at low doses (ED50 = 4 mg/kg) inhibited T-cell receptor-stimulated IL-2 production in mice, while the efficacy was remarkably decreased after the oral administration (ED50 = 25 mg/kg)[2]. | ||
| 作用机制 | RK 24466 is a potent and selective inhibitor of lck kinase. The hydrophobic pocket in lck (64-509) is occupied by the phenoxyphenyl moiety of RK 24466, resulting in an increased potency against lck (64-509). | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.70mL 0.54mL 0.27mL |
13.50mL 2.70mL 1.35mL |
26.99mL 5.40mL 2.70mL |
| 参考文献 |
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