| Identification | Back Directory | [Name]
AZM 475271 | [CAS]
476159-98-5 | [Synonyms]
M 475271
AZM 475271
AZM-475271;M475271;M-475271
N-(2-Chloro-5-methoxyphenyl)-6-methoxy
4-Quinazolinamine, N-(2-chloro-5-methoxyphenyl)-6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]- | [Molecular Formula]
C23H27ClN4O3 | [MDL Number]
MFCD19690925 | [MOL File]
476159-98-5.mol | [Molecular Weight]
442.94 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 |
|
| Company Name: |
InvivoChem
|
| Telephone: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|