产品
编 号：F517203
分子式：C30H29N5O5
分子量：539.58
分子式：C30H29N5O5
分子量：539.58
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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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: 913376-83-7
产品详情
生物活性：
AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively.
体内研究：
AMG-458 (orally, 30, 100 mg/kg) significantly inhibits tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight.Animal Model:NIH-3T3/TPR-Met model and U-87 MG human glioblastoma xenograft model.
Dosage:10, 30, 100 mg/kg.
Administration:Orally q.d. or b.i.d.
Result:With an ED50 of ～12 mg/kg and an ED90 of ～ 34 mg/kg in NIH-3T3/TPR-Met model.With an ED50 of ～16 mg/kg and an ED90 of ～ 59 mg/kg in U-87 MG human glioblastoma xenograft model.Significantly inhibited tumor growth at 30 and 100 mg/kg q.d. and 30 mg/kg b.i.d. without adverse effect on body weight.
Animal Model:Balb/c mouse and SD rat.
Dosage:1 mg/kg (Pharmacokinetic Analysis).
Administration:IV dose: 1 mg/kg (20% Captisol with pH adjusted to 3.5 using methanesulfonic acid).
Result:Exhibited CL ((L/h)/kg) values of 0.16 and 0.73, Vss (L/kg) values of 0.31 and 0.62, t1/2 (h) values of 1.3 and 1.0 in mouse and rat, respectively.
AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively.
体内研究：
AMG-458 (orally, 30, 100 mg/kg) significantly inhibits tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight.Animal Model:NIH-3T3/TPR-Met model and U-87 MG human glioblastoma xenograft model.
Dosage:10, 30, 100 mg/kg.
Administration:Orally q.d. or b.i.d.
Result:With an ED50 of ～12 mg/kg and an ED90 of ～ 34 mg/kg in NIH-3T3/TPR-Met model.With an ED50 of ～16 mg/kg and an ED90 of ～ 59 mg/kg in U-87 MG human glioblastoma xenograft model.Significantly inhibited tumor growth at 30 and 100 mg/kg q.d. and 30 mg/kg b.i.d. without adverse effect on body weight.
Animal Model:Balb/c mouse and SD rat.
Dosage:1 mg/kg (Pharmacokinetic Analysis).
Administration:IV dose: 1 mg/kg (20% Captisol with pH adjusted to 3.5 using methanesulfonic acid).
Result:Exhibited CL ((L/h)/kg) values of 0.16 and 0.73, Vss (L/kg) values of 0.31 and 0.62, t1/2 (h) values of 1.3 and 1.0 in mouse and rat, respectively.
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