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Glumetinib

CAS No. : 1642581-63-2

產(chǎn)品活性：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.

研究領(lǐng)域：Protein Tyrosine Kinase/RTK

作用靶點(diǎn)：c-Met/HGFR

In Vitro: 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.

In Vivo: 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.

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