213743-31-8
中文名稱 | 213743-31-8 |
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中文同義詞 | 化合物RK-24466;7-環(huán)戊基-5-(4-苯氧基苯基)-7H-吡咯并[2,3-D]嘧啶-4-胺;4-氨基-7-環(huán)戊基-5-(4-苯氧基苯基)-7H-吡咯并[2,3-D]嘧啶 |
英文名稱 | 7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR |
英文同義詞 | 7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR;7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine;RK-24466 ;RK 24466 ;RK24466;Lck Inhibitor - CAS 213743-31-8 - Calbiochem;d]pyrimidin-4-ylamine;RK-24466;KIN 001-51;7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-cyclopentyl-5-(4-phenoxyphenyl)- |
CAS號(hào) | 213743-31-8 |
分子式 | C23H22N4O |
分子量 | 370.45 |
EINECS號(hào) | |
相關(guān)類別 | 標(biāo)準(zhǔn)品;LckNon-Receptor Tyrosine Kinase Biology;Lymphocyte Specific Kinase (Lck)Cell Signaling and Neuroscience;Non-Receptor Tyrosine Kinase Inhibitors;Enzyme Inhibitors by Enzyme;Kinase/Phosphatase Biology;L to;Protein Kinase Inhibitors |
Mol文件 | 213743-31-8.mol |
結(jié)構(gòu)式 |
213743-31-8 性質(zhì)
沸點(diǎn) | 605.1±55.0 °C(Predicted) |
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密度 | 1.30±0.1 g/cm3(Predicted) |
儲(chǔ)存條件 | 2-8°C |
溶解度 | 在DMSO中的溶解度為17 mg/mLat ≤60 °C |
酸度系數(shù)(pKa) | 5.75±0.30(Predicted) |
形態(tài) | 白色固體 |
顏色 | 白色 |
Target | Value |
Lck (64-509)
(Cell-free assay) | 0.001 μM |
Lckcd
(Cell-free assay) | 0.002 μM |
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).
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.
安全信息
WGK Germany | 3 |
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更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
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2024/11/08 | HY-108318 | 213743-31-8 RK-24466 | 213743-31-8 | 1mg | 600元 |
2024/11/08 | HY-108318 | 213743-31-8 RK-24466 | 213743-31-8 | 5mg | 1500元 |