| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| J409280-1ml |
1ml |
现货  |
|
| 英文别名 | 6-(difluoro(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)quinoline |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | JNJ-38877605 |
| 生化机理 | JNJ-38877605 是一种 ATP 竞争性 c-Met 抑制剂，IC50 为 4 nM，对 c-Met 的选择性是其他 200 种酪氨酸和丝氨酸-苏氨酸激酶的 600 倍。第一阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 肝细胞生长因子受体抑制剂 |
| 产品介绍 |
产品介绍： JNJ-38877605是一种ATP竞争性的c-Met抑制剂，IC50为4 nM，作用于c-Met比作用于200种其他酪氨酸和丝-苏氨酸激酶选择性高600倍。 Information JNJ-38877605 JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. Phase 1. JNJ-38877605 shows more than 600-fold selectivity for c-Met compared with more than 200 other diverse tyrosine and serine-threonine kinases and also potently inhibits HGF-stimulated and constitutively activated c-Met phosphorylation in vitro. In EBC1, GTL16, NCI-H1993, and MKN45 cells, JNJ-38877605 (500 nM) leads to a significant reduction of phosphorylation of Met and RON, another key player in invasive growth. A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells. In vivo In mice bearing established GTL16 xenografts, JNJ-38877605, dosed orally with 40 mg/kg/day for 72 hours, results in a statistically significant decrease in the plasma levels of human IL-8 (from 0.150 ng/mL to 0.050 ng/mL) and GROα (from 0.080 ng/mL to 0.030 ng/mL). While concentrations of uPAR in the blood become reduced to more than 50% at the same dose. cell lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| ALogP | 2.1 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CN1C=C(C=N1)C2=NN3C(=NN=C3C(C4=CC5=C(C=C4)N=CC=C5)(F)F)C=C2 |
| 分子量 | 377.35 |
| Reaxy-Rn | 12928078 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12928078&ln= |
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