MGCD-265
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) .
Product Specifications
CAS Number
875337-44-3
Product Name Alternative
Glesatinib
Purity
>98% (HPLC)
Solubility
DMSO:104 mg/mL (200.92 mM) ; Ethanol:<1 mg/mL (<1 mM) ; Water:<1 mg/mL (<1 mM)
Smiles
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
Molecular Formula
C26H20FN5O2S2
Molecular Weight
517.6
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
N- ((3-fluoro-4- ((2- (1-methyl-1H-imidazol-4-yl) thieno[3,2-b]pyridin-7-yl) oxy) phenyl) carbamothioyl) -2-phenylacetamide
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