Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JNJ-38877605 is an ATP-competitive c-Met inhibitor (IC50: 4 nM), 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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2 mg | 在庫あり | ¥ 8,000 | |||
5 mg | 在庫あり | ¥ 12,500 | |||
10 mg | 在庫あり | ¥ 19,500 | |||
25 mg | 在庫あり | ¥ 35,500 | |||
50 mg | 在庫あり | ¥ 57,000 | |||
100 mg | 在庫あり | ¥ 93,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 13,000 |
説明 | JNJ-38877605 is an ATP-competitive c-Met inhibitor (IC50: 4 nM), 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. |
ターゲット&IC50 | c-Met:4 nM |
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. 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 (40 mg/kg/day, p.o., total 3day) results in a statistically marked decrease in the plasma levels of human IL-8 (0.150-0.050 ng/mL) and GROα (0.080-0.030 ng/mL). While concentrations of uPAR in the blood become reduced to more than 50% at the same dose. |
動物実験 | 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 immuno-deficient nu/nu female mice on Swiss CD1 background. Formulation: JNJ-38877605 is dissolved in PBS. Dosages: ≤40 mg/kg/day. Administration: Administered via p.o. |
分子量 | 377.35 |
分子式 | C19H13F2N7 |
CAS No. | 943540-75-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 35 mg/mL (92.8 mM)
You can also refer to dose conversion for different animals. 詳細
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JNJ-38877605 943540-75-8 Tyrosine Kinase/Adaptors c-Met/HGFR Inhibitor inhibit JNJ38877605 JNJ 38877605 inhibitor