产品
编 号：F055266
分子式：C23H22FN7O3
分子量：463.46
分子式：C23H22FN7O3
分子量：463.46
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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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: 1173699-31-4
产品详情
生物活性：
AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC50 values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis.
体内研究：
AMG 337 (0-30 mg/kg; p.o.; daily, for 28 d) inhibits MET signaling in tumor xenografts and inhibits tumor growth in MET-dependent tumor xenograft models.AMG 337 (0-3 mg/kg; p.o.; once, for 3 or 24 h) is associated with increased necrosis in the MET-dependent SNU-620 tumor xenograft model.Animal Model:Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts
Dosage:0, 0.3, and 1 mg/kg (SNU-620 xenograft); 0, 0.3, 1, 3, and 10 mg/kg (SNU-5 xenograft); 0, 3, 10 and 30 mg/kg (U-87 xenograft)
Administration:Oral administration; daily, for 28 days
Result:Inhibited tumor growth in MET-dependent tumor xenograft models.
Animal Model:Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts
Dosage:0.1, 0.5, 0.75, 1, 2, and 3 mg/kg
Administration:Oral administration; once, for 3 hours
Result:Inhibited Gab-1 phosphorylation in a dose-dependent manner.
Animal Model:Female CD1 nu/nu mice with SNU-620 xenograft model (6-11 weeks of age; 20-26 g)
Dosage:0, 0.3, 1, and 3 mg/kg
Administration:Oral administration; once, for 3 or 24 hours
Result:Increased immunohistochemical staining with anti-caspase-3 antibody and decreased immunohistochemical staining with anti-BrdU antibody.
体外研究：
AMG 337 (0-3 μM; 72 h) inhibits proliferation in MET-dependent cancer cell lines.AMG 337 (0-300 nM; 0-24 h; MKN-45, SNU-620, and SNU-5 cells) inhibits signaling through the PI3K and MAPK pathways in MET-amplified gastric cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis.
AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC50 values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis.
体内研究：
AMG 337 (0-30 mg/kg; p.o.; daily, for 28 d) inhibits MET signaling in tumor xenografts and inhibits tumor growth in MET-dependent tumor xenograft models.AMG 337 (0-3 mg/kg; p.o.; once, for 3 or 24 h) is associated with increased necrosis in the MET-dependent SNU-620 tumor xenograft model.Animal Model:Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts
Dosage:0, 0.3, and 1 mg/kg (SNU-620 xenograft); 0, 0.3, 1, 3, and 10 mg/kg (SNU-5 xenograft); 0, 3, 10 and 30 mg/kg (U-87 xenograft)
Administration:Oral administration; daily, for 28 days
Result:Inhibited tumor growth in MET-dependent tumor xenograft models.
Animal Model:Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts
Dosage:0.1, 0.5, 0.75, 1, 2, and 3 mg/kg
Administration:Oral administration; once, for 3 hours
Result:Inhibited Gab-1 phosphorylation in a dose-dependent manner.
Animal Model:Female CD1 nu/nu mice with SNU-620 xenograft model (6-11 weeks of age; 20-26 g)
Dosage:0, 0.3, 1, and 3 mg/kg
Administration:Oral administration; once, for 3 or 24 hours
Result:Increased immunohistochemical staining with anti-caspase-3 antibody and decreased immunohistochemical staining with anti-BrdU antibody.
体外研究：
AMG 337 (0-3 μM; 72 h) inhibits proliferation in MET-dependent cancer cell lines.AMG 337 (0-300 nM; 0-24 h; MKN-45, SNU-620, and SNU-5 cells) inhibits signaling through the PI3K and MAPK pathways in MET-amplified gastric cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis.
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