BMS-2

Names

[ Name ]:
BMS-2

[Synonym ]:
1-(4-Fluorophenyl)-N-[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]-2-oxo-1,2-dihydro-3-pyridinecarboxamide
RS0065
3ce3
2-pyridone analogue,2
N-(4-(1H-Pyrrolo[2,3-b]pyridin-4-yloxy)-3-fluorophenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
3-Pyridinecarboxamide, 1-(4-fluorophenyl)-N-[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]-1,2-dihydro-2-oxo-

Biological Activity

[Description]:

MET kinase-IN-4 is an orally active Met kinase inhibitor. MET kinase-IN-4 has potent Met kinase inhibitory activity with an IC50 value of 1.9 nM. MET kinase-IN-4 can be used for the research of cancer[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR

[Target]

IC50: 1.9 nM (Met); 4 nM (Flt-3); 27 nM (VEGFR-2)[1]

[In Vitro]

MET kinase-IN-4 (Compound 2) 具有有效的 Met 激酶抑制活性，IC50 值为 1.9 nM[1]。 MET kinase-IN-4 抑制 Flt-3 和 VEGFR-2 激酶，IC50 值分别为 4 和 27 nM[1]。 MET kinase-IN-4 (3 μM) 在人和小鼠肝微粒体中表现出良好的代谢稳定性[1]。

[In Vivo]

MET kinase-IN-4 (Compound 2) 在小鼠体内具有良好的药代动力学特征[1]。 MET kinase-IN-4 在 GTL-16 人胃癌异种移植模型中表现出显著的体内抗肿瘤活性[1]。 Animal Model: Mice[1] Dosage: 5, 10 mg/kg Administration: IV, PO Result: Showed extensive extravascular distribution and a favorable half-life. Animal Model: Nude mice[1] Dosage: 6.25, 12.5, 25 and 50 mg/kg Administration: PO, once a day Result: Showed antitumor activity in dose-dependet.

[References]

[1]. Kyoung Soon Kim, et al. Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities. J Med Chem. 2008 Sep 11;51(17):5330-41.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
701.5ºC at 760 mmHg

[ Melting Point ]:
212-214ºC

[ Molecular Formula ]:
C₂₅H₁₆F₂N₄O₃

[ Molecular Weight ]:
458.416

[ Flash Point ]:
378.1ºC

[ Exact Mass ]:
458.119049

[ PSA ]:
89.01000

[ LogP ]:
4.82

[ Index of Refraction ]:
1.721

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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