Glumetinib (Synonyms: SCC244) |
Katalog-Nr.GC64947 |
Glumetinib (SCC244) ist ein hochselektiver, oral bioverfÜgbarer, ATP-kompetitiver c-Met-Inhibitor mit einem IC50 von 0,42 nM. Glumetinib weist eine mehr als 2400-fache SelektivitÄt fÜr c-Met gegenÜber den 312 untersuchten Kinasen auf, einschließlich des c-Met-Familienmitglieds RON und der hochgradig homologen Kinasen Axl, Mer, TyrO3. Antitumor-AktivitÄt.
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Cas No.: 1642581-63-2
Sample solution is provided at 25 µL, 10mM.
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[1].
Glumetinib (SCC244) (0-10 nM; 72 hours) elicits selective and profound effects against c-Met-driven cancer cell proliferation[1].Glumetinib (0-50 nM; 24 hours) induces G1-S phase cell-cycle arrest in c-Met-addicted human cancer cells[1].
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[1].Glumetinib shows significant antitumor efficiency in NSCLC and HCC tumor PDX models with MET aberration[1].
[1]. Ai J, et al. Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models. Mol Cancer Ther. 2018 Apr;17(4):751-762.
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