中文名 | RK-24466 (KIN 001-51) |
英文名 | 7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR |
别名 | 化合物RK-24466 7-环戊基-5-(4-苯氧基苯基)-7H-吡咯并[2,3-D]嘧啶-4-胺 |
英文别名 | RK24466 RK-24466 RK 24466 RK-24466 KIN 001-51 d]pyrimidin-4-ylamine RK-24466 (KIN 001-51) 7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine 7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-cyclopentyl-5-(4-phenoxyphenyl)- |
CAS | 213743-31-8 |
化学式 | C23H22N4O |
分子量 | 370.45 |
密度 | 1.30±0.1 g/cm3(Predicted) |
沸点 | 605.1±55.0 °C(Predicted) |
溶解度 | DMSO: 17mg/ml在 ≤ 60 °C,可溶 |
酸度系数 | 5.75±0.30(Predicted) |
存储条件 | 2-8°C |
外观 | 白色固体 |
颜色 | white |
体外研究 | RK-24466 is selective for Lck over a range of receptor, non-receptor tyrosine kinases and seronine/threonine kinases. RK-24466 are potent inhibitors of IL2 production in Jurkat cells stimulated with anti-CD3 antibody, being at least 100-fold more potent than PP1. RK-24466 displays remarkable cellular selectivity. RK-24466 significantly inhibits both VSMC proliferation and migration. RK-24466 suppresses VSMC proliferation and migration via down-regulating the protein kinase B (Akt) and extracellular signal regulated kinase (ERK) pathways, and it significantly decreases the expression of proliferating cell nuclear antigen (PCNA) and cyclin D1 and, the phosphorylation of retinoblastoma protein (pRb). |
体内研究 | RK-24466 inhibits T-cell receptor stimulated (a-CD3 mAb) IL-2 production in mice at low doses (ED 50 =4 mg/kg) after ip administration. However, efficacy is greatly reduced after oral administration (ED 50 =25 mg/kg) which is presumed to reflect poor intestinal absorption in the latter regimen. Inhibition of antigen specific T-cell immune responses is also seen for RK-24466. After administration of RK-24466 twice daily (100 mg/kg po) for 3 days during the in vivo priming phase, a 70% inhibition of IFNγ production is seen upon subsequent antigen-specific (KLH) challenge of lymphocytes from the draining lymph nodes in vitro . RK-24466 suppresses the migration of VSMCs from endothelium-removed aortic rings, as well as neointima formation following rat carotid balloon injury. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.699 ml | 13.497 ml | 26.994 ml |
5 mM | 0.54 ml | 2.699 ml | 5.399 ml |
10 mM | 0.27 ml | 1.35 ml | 2.699 ml |
5 mM | 0.054 ml | 0.27 ml | 0.54 ml |
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