ChemicalBook CAS DataBase List 476159-98-5

476159-98-5

Name	AZM 475271
CAS	476159-98-5
Molecular Formula	C23H27ClN4O3
MDL Number	MFCD19690925
Molecular Weight	442.94
MOL File	476159-98-5.mol

Chemical Properties

Boiling point	556.1±50.0 °C(Predicted)
density	1.252±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO:43.15(Max Conc. mg/mL);97.42(Max Conc. mM)
form	A solid
pka	8.92±0.10(Predicted)
color	White to off-white

Safety Data

Symbol(GHS)	GHS06
Signal word	Danger
Hazard statements	H301
Precautionary statements	P264-P270-P301+P310-P321-P330-P405-P501

Hazard Information

Uses

AZM 475271 is an src tyrosine kinase inhibitor.

Biological Activity

AZM475271 (M475271) is an orally activepotent and selective inhibitor against src family kinases src and yes (IC50 = 25 nM & 10 nMrespectively; lck/VEGFR2/EGFR/csk/FGFR1 IC50 = 0.2/0.5/0.6/7.6/∼20 μM) th at 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.).

in vivo

AZM475271(50 mg/kg; p.o.; once daily for 32 days) reduces tumor volume and the effect can be enhanced by combination with Gemcitabine (100 mg/kg; i.p.; twice weekly for 32 days) in athymic nude mice injected with L3.6pl cells^[2].
AZM475271 (50 mg/kg; p.o.; once) has biological effective plasma concentration with 24 hours in healthy nude mice ^[2].

Animal Model:	Healthy nude mice^[2]
Dosage:	50 mg/kg
Administration:	Oral gavage (p.o.); once
Result:	The plasma concentration was 32.1 μM (14.206 ng/mL), 20 μM (8879 ng/mL), and 11.7 μM (5187 ng/mL) at 2, 6, and 24 hours after p.o..

Animal Model:	Athymic nude mice (injected with 1 X 10⁶ viable L3.6pl cells)^[2]
Dosage:	50 mg/kg
Administration:	Oral gavage (p.o.); once daily for 32 days
Result:	The median tumor volume was significantly less than that in control mice. After combination therapy, primary pancreatic tumor volume was significantly less than that seen with Gemcitabine alone. The incidence of liver metastasis was markedly reduced. Did not significantly change animal weight when used alone, but reduced animal weight combined with Gemcitabine. Has antiproliferative effect alone and in combination with Gemcitabine. Induce apoptosis in pancreatic carcinoma cells in vivo, maximum apoptotic effect was observed in the combination with Gemcitabine. Reduced microvessel density (MVD) alone and no significant difference in combination with Gemcitabine.

IC 50

Lck: 0.03 μM (IC₅₀)

storage

Store at -20°C

Spectrum Detail

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