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编 号:F197830
分子式:C21H17N9O2S
分子量:459.48
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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:
Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity.

体内研究:
Glumetinib (2.5-10 mg/kg; p.o.; once daily for 2-3 weeks) significantly inhibits c-Met–driven tumor growth in cancer CDX models.Glumetinib shows significant antitumor efficiency in NSCLC and HCC tumor PDX models with MET aberration.Animal Model:Female nude mice (4-6 weeks old) (MKN-45 model)
Dosage:10, 5, 2.5 mg/kg
Administration:P.o.; once daily for 2-3 weeks
Result:Significantly inhibited tumor growth with inhibitory rates of 99.3%, 88.6%, and 63.6% at doses of 10, 5, and 2.5 mg/kg, respectively.

体外研究:
Glumetinib (SCC244) (0-10 nM; 72 hours) elicits selective and profound effects against c-Met–driven cancer cell proliferation.Glumetinib (0-50 nM; 24 hours) induces G1–S phase cell-cycle arrest in c-Met–addicted human cancer cells.
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