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About This Item
Empirical Formula (Hill Notation):
C23H27ClN4O3
CAS Number:
Molecular Weight:
442.94
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
ClC1=CC=C(C=C1NC2=NC=NC3=CC(OCC4CCN(CC4)C)=C(C=C32)OC)OC
InChI
1S/C23H27ClN4O3/c1-28-8-6-15(7-9-28)13-31-22-12-19-17(11-21(22)30-3)23(26-14-25-19)27-20-10-16(29-2)4-5-18(20)24/h4-5,10-12,14-15H,6-9,13H2,1-3H3,(H,25,26,27)
InChI key
WPOXAFXHRJYEIC-UHFFFAOYSA-N
Biochem/physiol Actions
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.).
Orally active, potent and selective src and yes inhibitor with anticancer efficacy both in cultures and in mice in vivo.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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