c-Met-IN-14 

c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC₅₀ value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner^[1].

IC50: 2.89 nM (c-Met); 4.26 nM (c-kit); 7.28 nM (Flt-3)^[1]

c-Met-IN-14 (compound 26af) is a relatively selective inhibitor of c-Met kinase (IC₅₀=2.89 nM), because of high inhibitory effects against c-Kit (IC₅₀=4.26 nM) and Flt-3 (IC₅₀=7.28 nM)^[1].
c-Met-IN-14 (0.28-0.72 μM; 24 h) exhibits the remarkable anti-proliferative activities against cancer cell lines (A549, HT-29, MKN-45 and MDA-MB-231), with IC₅₀s of 0.28-0.72 μM^[1].
c-Met-IN-14 (0.25, 0.5, and 1.0 μM; 12 h) induces the late apoptotic and early apoptotic and (0.25, 0.5, and 1.0 μM; 24 h) shows anti-proliferative of A549 cells by arresting cell cycle at G2/M phase and apoptosis induction^[1].
c-Met-IN-14 (1.35, or 6.12 μM, respectively; 24 h) has moderate selectivity towards cancer cells over normal cells, with the selectivity index of 4.2 and 19.1 to HUVEC (IC₅₀=1.35 μM) and FHC cells (IC₅₀=6.12 μM), respectively^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

c-Met-IN-14 (compound 26af) (p.o.; 8 mg/kg) exhibits safety profile and favorable pharmacokinetic properties in BALB/c mouse, with rapid absorption (T_max=2.5 h), high maximum concentration (C_max=1228.4 ng/mL), high plasma exposure (AUC_0-∞=6.8 µg.h.mL^-1), accepted elimination half-life (T_1/2=3.5 h), and well clearance (1.18 L.h_-1.kg_-1), has a moderate oral bioavailability (74%) in mouse^[1].
c-Met-IN-14 (i.p.; below 200 mg/kg) doesn’t cause abnormalities, anaphylactic responses, allergic reactions on mice^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

701.20

C₃₄H₃₈ClFN₄O₇S

2443380-34-3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Nan X, et al. Design, synthesis and biological evaluation of novel N-sulfonylamidine-based derivatives as c-Met inhibitors via Cu-catalyzed three-component reaction. Eur J Med Chem. 2020 Aug 15. 200:112470.  [Content Brief]