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编 号:F532478
分子式:C19H13F2N7
分子量:377.35
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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生物活性:
JNJ-38877605 is an orally active ATP-competitive inhibitor of c-Met with an IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. JNJ-38877605 inhibits c-Met phosphorylation and regulates lipid accumulation. JNJ-38877605 can be used for tumor and metabolic disease reseach.

体内研究:
JNJ-38877605 (50 mg/kg,口服,每日 1 次,持续 13 天) 在异种移植肿瘤中抵消辐射诱导的侵袭,促进细胞凋亡。JNJ-38877605 (40 mg/kg,口服,每日 1 次,持续 3 天) 使 Met 依赖的 GTL16 肿瘤异种移植小鼠模型的血浆中 IL8、GROa、uPAR 浓度下降。Animal Model:U251 human glioma cells and MDA-MB-231 human breast cancer cells transplanted tumor xenografts
Dosage:50 mg/kg
Administration:Oral gavage (p.o.) once daily for 13 days
Result:Counteracted radiation-induced invasiveness, promoted apoptosis.
Animal Model:Met-addicted GTL16 xenografts mice model
Dosage:40 mg/kg
Administration:Oral gavage (p.o.) once daily for 3 days
Result:Decreased in the plasma levels of human IL-8 (from 0.150 to 0.050 ng/ml) and GROa (from 0.080 to 0.030 ng/ml).Diminished The blood concentration of uPAR also by more than 50% .Inhibited Met-addicted xenografts induced consistent changes in plasma concentration of IL8, GROa, uPAR and IL-6.

体外研究:
JNJ-38877605 (0.5 μΜ,24 小时) 抑制 A549 细胞中 CPNE1 (HY-P70097) 诱导的 MET 信号通路的激活。JNJ-38877605 (JNJ) (5,10,20 μΜ,2,,5,8 天) 抑制 MET 磷酸化,减少 3T3-L1 细胞中脂质积累和甘油三酯 (TG) 含量,且无细胞毒性。
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