1642581-63-2

Glumetinib (1642581-63-2) is a highly selective (2400-fold selectivity against a panel of 312 kinases) and potent (IC50 = 0.42 nM) inhibitor of c-Met kinase.? It induced tumor regression in MET-driven CDX (MKN-45, SNU-5, EBC-1) and PDX (4 NSCLC, 5 HCC) tumor models.

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].

Ai et al. (2018), Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models; Cancer Res., 17 751