213743-31-8
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- CAS号:
- 213743-31-8
- 英文名:
- 7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR
- 英文别名:
- RK-24466;KIN001-051;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;RK-24466,Src,Inhibitor,inhibit,RK 24466,RK24466;7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine;4-Amino-7-cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidine
- 中文名:
- 213743-31-8
- 中文别名:
- 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;4-氨基-7-环戊基-5-(4-苯氧基苯基)-7H-吡咯并[2,3-D]嘧啶
- CBNumber:
- CB6497372
- 分子式:
- C23H22N4O
- 分子量:
- 370.45
- MOL File:
- 213743-31-8.mol
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213743-31-8化学性质
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沸点:
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605.1±55.0 °C(Predicted)
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密度:
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1.30±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: 17 mg/mL at ≤60 °C, soluble
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酸度系数(pKa):
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5.75±0.30(Predicted)
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形态:
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White solid
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颜色:
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white
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213743-31-8性质、用途与生产工艺
RK-24466 (KIN 001-51, Lck inhibitor C 8863, C8863)是一种有效的、选择性的 Lck 抑制剂，可抑制人Lck激酶的两种构建体，lck (64-509)和lckcd，对应的IC50值分别为小于0.001 μM和0.002 μM。
| Target | Value |
Lck (64-509)
(Cell-free assay)
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0.001 μM
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Lckcd
(Cell-free assay)
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0.002 μM
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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.
213743-31-8
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-108318 | 213743-31-8
RK-24466 | 213743-31-8 | 1mg | 818元 |
| 2024/04/30 | HY-108318 | 213743-31-8
RK-24466 | 213743-31-8 | 5mg | 1800元 |
213743-31-8, 213743-31-8 相关搜索:
- Protein Kinase Inhibitors
- L to
- Kinase/Phosphatase Biology
- Enzyme Inhibitors by Enzyme
- Non-Receptor Tyrosine Kinase Inhibitors
- Lymphocyte Specific Kinase (Lck)Cell Signaling and Neuroscience
- LckNon-Receptor Tyrosine Kinase Biology
- 合成有机化合物配体
- 标准品
- 4-氨基-7-环戊基-5-(4-苯氧基苯基)-7H-吡咯并[2,3-D]嘧啶
- 7-环戊基-5-(4-苯氧基苯基)-7H-吡咯并[2,3-D]嘧啶-4-胺
- 化合物RK-24466
- 213743-31-8
- 4-Amino-7-cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidine
- RK-24466,Src,Inhibitor,inhibit,RK 24466,RK24466
- KIN001-051
- 7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-cyclopentyl-5-(4-phenoxyphenyl)-
- KIN 001-51
- RK-24466
- d]pyrimidin-4-ylamine
- Lck Inhibitor - CAS 213743-31-8 - Calbiochem
- RK-24466 ;RK 24466 ;RK24466
- 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
- 7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR