213743-31-8
基本信息
KIN 001-51
d]pyrimidin-4-ylamine
RK-24466
RK 24466
RK24466
7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR
Lck Inhibitor - CAS 213743-31-8 - Calbiochem
7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3‑
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)-
7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3‑:d]pyrimidin-4-ylamine
物理化学性质
| 沸点 | 605.1±55.0 °C(Predicted) |
| 密度 | 1.30±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | DMSO: 17 mg/mL at ≤60 °C, soluble |
| 酸度系数(pKa) | 5.75±0.30(Predicted) |
| 形态 | 白色固体 |
| 颜色 | white |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319-H335 |
| 防范说明 | P261-P305+P351+P338 |
| WGK Germany | 3 |
213743-31-8价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 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 |
| 2024/11/08 | S0020 | 213743-31-8 RK 24466 | 213743-31-8 | 5mg | 2370元 |
常见问题列表
| 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.