产品
编 号：F212525
分子式：C18H22FN9O2
分子量：415.42
分子式：C18H22FN9O2
分子量：415.42
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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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结构图
CAS No: 1776112-90-3
产品详情
生物活性：
Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).
体内研究：
Mavelertinib exhibits low to moderate oral bioavailability (mouse 60%, rat 11%, dog 66%) following oral administration (mouse 1, rat 30, dog 3 mg/kg).Mavelertinib exhibits short plasma half-lives (mouse 0.56, rat 0.28, dog 1.3 h) due to moderate to high plasma clearance (mouse 53, rat 49, dog 12 mL/min/kg) and low steady-state volume of distribution (mouse 1.48, rat 0.66, dog 0.94 L/kg) following intravenous administration (1 mg/kg to mouse, rat and dog).Animal Model:Female Nu/Nu mice
Dosage:1 mg/kg (Pharmacokinetic Analysis)
Administration:P.o. and i.v. administration
Result:Oral bioavailability (60%), T1/2 (1.48 h).
体外研究：
Mavelertinib exhibits selectivity over wild-type EGFR (IC50=307 nM).Mavelertinib (10 μM) exhibits less than 50% e?ect or inhibition against all nonkinase targets.Mavelertinib inhibits the hERG26 current with an IC50 > 100 μM.
Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).
体内研究：
Mavelertinib exhibits low to moderate oral bioavailability (mouse 60%, rat 11%, dog 66%) following oral administration (mouse 1, rat 30, dog 3 mg/kg).Mavelertinib exhibits short plasma half-lives (mouse 0.56, rat 0.28, dog 1.3 h) due to moderate to high plasma clearance (mouse 53, rat 49, dog 12 mL/min/kg) and low steady-state volume of distribution (mouse 1.48, rat 0.66, dog 0.94 L/kg) following intravenous administration (1 mg/kg to mouse, rat and dog).Animal Model:Female Nu/Nu mice
Dosage:1 mg/kg (Pharmacokinetic Analysis)
Administration:P.o. and i.v. administration
Result:Oral bioavailability (60%), T1/2 (1.48 h).
体外研究：
Mavelertinib exhibits selectivity over wild-type EGFR (IC50=307 nM).Mavelertinib (10 μM) exhibits less than 50% e?ect or inhibition against all nonkinase targets.Mavelertinib inhibits the hERG26 current with an IC50 > 100 μM.
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