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213743-31-8

213743-31-8

中文名稱213743-31-8
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 結(jié)構(gòu)式

213743-31-8 性質(zhì)

沸點(diǎn)605.1±55.0 °C(Predicted)
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

213743-31-8 用途與合成方法

RK-24466 (KIN 001-51, Lck inhibitor C 8863, C8863)是一種有效的、選擇性的 Lck 抑制劑,可抑制人Lck激酶的兩種構(gòu)建體,lck (64-509)和lckcd,對(duì)應(yīng)的IC50值分別為小于0.001 μM和0.002 μM。
TargetValue
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 Germany3

MSDS信息

更新日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-108318213743-31-8
RK-24466
213743-31-81mg600元
2024/11/08HY-108318213743-31-8
RK-24466
213743-31-85mg1500元

213743-31-8 上下游產(chǎn)品信息

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