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JNJ-38877605

产品号 S1114 公司名称 Selleck Chemicals
CAS号 943540-75-8 公司网站 http://www.selleckchem.com
分子式 C19H13F2N7 电 话 (877) 796-6397
分子量 377.3502264 传 真 (832) 582-8590
纯 度 电子邮件 sales@selleckchem.com
保 存 -20°C Chembase数据库ID: 72520

产品价格信息

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产品别名

标题
JNJ-38877605
IUPAC标准名
6-{difluoro[6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline
IUPAC传统名
6-{difluoro[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline

产品登记号

CAS号 943540-75-8

产品性质

作用靶点 c-Met
成盐信息 Free Base
溶解度 DMSO
保存条件 -20°C

产品详细信息

详细说明 (English)
Research Area
Description Cancer
Biological Activity
Description JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM.
Targets c-Met
IC50 4 nM [1]
In Vitro 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. [1] 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. [2] A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells. [3]
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. [3]
Clinical Trials JNJ-38877605 is currently in Phase I clinical trials in patients with Neoplasms.
Features
Protocol
Animal Study [3]
Animal Models GTL16 cells are inoculated subcutaneously into the right posterior flank (or both right and left posterior flanks, for determination of uPAR and IL-6) of 6-week-old immunodeficient nu/nu female mice on Swiss CD1 background.
Formulation JNJ-38877605 is dissolved in PBS.
Doses ≤40 mg/kg/day
Administration Administered via p.o.
References
[1] Perera T, et al. Presented at the 99th AACR Annual Meeting; 2008 Apr 12-16; San Diego (CA): Abst
[2] De Bacco F, et al. J Natl Cancer Inst. 2011 Apr, 103(8), 645-661.
[3] Torti D, et al. Int J Cancer. 2012, 130(6), 1357-1366.