AZM475271

C₂₃H₂₇ClN₄O₃

442.94

MFCD19690925

AZM475271 (M475271) is an orally active, potent and selective inhibitor against src family kinases src and yes (IC50 = 25 nM & 10 nM, respectively; lck/VEGFR2/EGFR/csk/FGFR1 IC50 = 0.2/0.5/0.6/7.6/∼20 μM) that effectively suppresses src-dependent cellular signaling events (26%/48% inhibition of 50 ng/mL VEGF-induced HUVEC proliferation/migration at 100 nM; 31%/72% inhibition of 10 ng/mL VEGF-induced Flk-1/Src phosphorylation in HUVECs at 300 nM) and exbihits anticancer efficacy both in cultures (70% PC-9/30% A549 proliferation inhibition at 1 μM) and in vivo (78%/100% PC-9 tumor growth suppression in mice via 10/50 mg/kg/day p.o.).

≥98% (HPLC)

powder

white to beige

DMSO: 2 mg/mL, clear

−20℃

ClC1=CC=C(C=C1NC2=NC=NC3=CC(OCC4CCN(CC4)C)=C(C=C32)OC)OC

11 - Combustible Solids

WGK 3