产品
编 号：F752781
分子式：C34H38ClFN4O7S
分子量：701.2
分子式：C34H38ClFN4O7S
分子量：701.2
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CAS No: 2443380-34-3
产品详情
生物活性：
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.
体内研究：
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 (Tmax=2.5 h), high maximum concentration (Cmax=1228.4 ng/mL), high plasma exposure (AUC0-∞=6.8 μg.h.mL-1), accepted elimination half-life (T1/2=3.5 h), and well clearance (1.18 L.h-1.kg-1), has a moderate oral bioavailability (74%) in mouse.c-Met-IN-14 (i.p.; below 200 mg/kg) doesn’t cause abnormalities, anaphylactic responses, allergic reactions on mice.Animal Model:8-week-old male BALB/c mice
Dosage:0 (vehicle), 100, 200, 300, or 400 mg/kg
Administration:Intraperitoneal injection; treatment on day 0 and assessment every 3 days for 15 days
Result:Showed no obvious toxicity in acute toxicity tests.
Animal Model:Pharmacokinetic profiles of compound 26af in BALB/c mouse
Dosage:
Administration:
Result:RouteDose (mg/kg)T1/2 (h)Cmax (ng.mL-1)Tmax (h)AUC0-∞ (μg.h.mL-1)CL (L.h-1.kg-1)CL (%)
i.v.21.8675.6-2.3-
p.o.83.51228.42.56.81.1874
体外研究：
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).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.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.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.
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.
体内研究：
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 (Tmax=2.5 h), high maximum concentration (Cmax=1228.4 ng/mL), high plasma exposure (AUC0-∞=6.8 μg.h.mL-1), accepted elimination half-life (T1/2=3.5 h), and well clearance (1.18 L.h-1.kg-1), has a moderate oral bioavailability (74%) in mouse.c-Met-IN-14 (i.p.; below 200 mg/kg) doesn’t cause abnormalities, anaphylactic responses, allergic reactions on mice.Animal Model:8-week-old male BALB/c mice
Dosage:0 (vehicle), 100, 200, 300, or 400 mg/kg
Administration:Intraperitoneal injection; treatment on day 0 and assessment every 3 days for 15 days
Result:Showed no obvious toxicity in acute toxicity tests.
Animal Model:Pharmacokinetic profiles of compound 26af in BALB/c mouse
Dosage:
Administration:
Result:RouteDose (mg/kg)T1/2 (h)Cmax (ng.mL-1)Tmax (h)AUC0-∞ (μg.h.mL-1)CL (L.h-1.kg-1)CL (%)
i.v.21.8675.6-2.3-
p.o.83.51228.42.56.81.1874
体外研究：
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).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.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.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.
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