产品
编 号：F011480
分子式：C18H13N7S
分子量：359.41
分子式：C18H13N7S
分子量：359.41
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规格
价格
是否有货
10mM*1mL in DMSO
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2mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1022150-57-7
产品详情
生物活性：
SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC50 of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity.
体内研究：
SGX523 exhibits antitumor activity in vivo. SGX523 inhibits MET-dependent tumor growth.Animal Model:Female Harlan nude mice (athymic nu/nu) were s.c. implanted with U87 cells
Dosage:10 or 30 mg/kg
Administration:Oral gavage; twice daily starting at day 5 for 22 days
Result:Potently inhibited U87MG tumor growth at a dose of 10 mg/kg administered twice daily.Led to clear regression of U87MG tumors at 30 mg/kg dosed twice daily.
体外研究：
SGX523 shows ATP-competitive inhibition with higher apparent affinity for the less active, unphosphorylated form of MET [MET-KD(0P), Ki=2.7 nM] versus the more active phospho-enzyme [MET-KD(3P), Ki=23 nM].SGX523 inhibits the growth of gastric and lung cancer cell lines with amplification of the MET gene but has no effect, even at high micromolar concentration, on cell lines with normal MET gene copy number. TheIC50s of 0.02, 0.113, and 0.035 μM for NSCLC H1993, gastric cncer MKN45, and gastric cancer Hs746T cells, respectively.The IC50 value for the inhibition of MET autophosphorylation is 0.040 μM in GTL16 cells. SGX523 (0.5, 1.5, 4.6, 13.7, 41, 123, 370, 1100, 3300, 10000 nM; 1 hour) inhibits MET autophosphorylation without affecting total MET or extracellular signal-regulated kinase protein levels in HGF-stimulated A549 cells.
SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC50 of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity.
体内研究：
SGX523 exhibits antitumor activity in vivo. SGX523 inhibits MET-dependent tumor growth.Animal Model:Female Harlan nude mice (athymic nu/nu) were s.c. implanted with U87 cells
Dosage:10 or 30 mg/kg
Administration:Oral gavage; twice daily starting at day 5 for 22 days
Result:Potently inhibited U87MG tumor growth at a dose of 10 mg/kg administered twice daily.Led to clear regression of U87MG tumors at 30 mg/kg dosed twice daily.
体外研究：
SGX523 shows ATP-competitive inhibition with higher apparent affinity for the less active, unphosphorylated form of MET [MET-KD(0P), Ki=2.7 nM] versus the more active phospho-enzyme [MET-KD(3P), Ki=23 nM].SGX523 inhibits the growth of gastric and lung cancer cell lines with amplification of the MET gene but has no effect, even at high micromolar concentration, on cell lines with normal MET gene copy number. TheIC50s of 0.02, 0.113, and 0.035 μM for NSCLC H1993, gastric cncer MKN45, and gastric cancer Hs746T cells, respectively.The IC50 value for the inhibition of MET autophosphorylation is 0.040 μM in GTL16 cells. SGX523 (0.5, 1.5, 4.6, 13.7, 41, 123, 370, 1100, 3300, 10000 nM; 1 hour) inhibits MET autophosphorylation without affecting total MET or extracellular signal-regulated kinase protein levels in HGF-stimulated A549 cells.
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