MGCD-265

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MGCD-265 是一种有效的、多靶点和 ATP 竞争性的 c-Met 和 VEGFR1/2/3 抑制剂，IC50 分别为 1 nM、3 nM/3 nM/4 nM。

MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.(In Vitro):MGCD-265 analog inhibits A549 cells migration and DU145 cells scattering, with IC50s of 0.4 μM and 0.08 μM, respectively, in HGF-driven cell migration and scattering assays.MGCD-265 analog inhibits HUVEC ERK phosphorylation (IC50=0.03 μM) and HUVEC proliferation (IC50=0.006 μM) in VEGF-dependent cell-based assays.(In Vivo):MGCD-265 analog (20 mg/kg; p.o.) inhibits tumor growth inhibition on various human tumor models in mice.MGCD-265 analog exhibits moderate oral bioavailability (rat 12%, dog 42%) and Cmax (rat 0.14, dog 0.21 uM/(mg/kg)) following oral administration (rat 5-25, dog 5 mg/kg).MGCD-265 analog exhibits reasonable terminal elimination half-lives (rat 1.2, dog 5.8 h) due to plasma clearance (rat 0.33, dog 1.1 L/(kg h)) following intravenous administration (rat 2.5, dog 0.8 mg/kg) .

MGCD-265 analog inhibits A549 cells migration and DU145 cells scattering, with IC50s of 0.4 μM and 0.08 μM, respectively, in HGF-driven cell migration and scattering assays.MGCD-265 analog inhibits HUVEC ERK phosphorylation (IC50=0.03 μM) and HUVEC proliferation (IC50=0.006 μM) in VEGF-dependent cell-based assays.

MGCD-265 analog (20 mg/kg; p.o.) inhibits tumor growth inhibition on various human tumor models in mice.MGCD-265 analog exhibits moderate oral bioavailability (rat 12%, dog 42%) and Cmax (rat 0.14, dog 0.21 uM/(mg/kg)) following oral administration (rat 5-25, dog 5 mg/kg).MGCD-265 analog exhibits reasonable terminal elimination half-lives (rat 1.2, dog 5.8 h) due to plasma clearance (rat 0.33, dog 1.1 L/(kg h)) following intravenous administration (rat 2.5, dog 0.8 mg/kg) . Animal Model:Female Sprague-Dawley rats Dosage:2.5 mg/kg for i.v.; 5-25 mg/kg for oral (Pharmacokinetic Analysis)Administration:Intravenous injection and oral administration Result:Oral bioavailability (12%), Cmax (0.14 μM/(mg/kg)), T1/2 (1.2 h), Animal Model:Male beagle dogs Dosage:0.8 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis) Administration:Intravenous administration and oral administration Result:Oral bioavailability (42%), Cmax (0.21 uM/(mg/kg)), T1/2 (5.8 h).

Glesatinib

Angiogenesis

c-Met/HGFR

Met| RON| VEGFR1| VEGFR2| VEGFR3

Cancer

——

875337-44-3

517.6

C26H20FN5O2S2

>98% (HPLC)

DMSO:104 mg/mL (200.92 mM); Ethanol:<1 mg/mL (<1 mM); Water:<1 mg/mL (<1 mM)

O=C(NC(NC1=CC=C(OC2=C3C(C=C(C4=CN(C)C=N4)S3)=NC=C2)C(F)=C1)=S)CC5=CC=CC=C5

N-((3-fluoro-4-((2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)carbamothioyl)-2-phenylacetamide

(-20℃)

With Ice Pack

≥ 2 years