CAS 888719-03-7|BMS-2

Introduction:Basic information about CAS 888719-03-7|BMS-2, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameBMS-2
CAS Number888719-03-7Molecular Weight458.416
Density1.5±0.1 g/cm3Boiling Point701.5ºC at 760 mmHg
Molecular FormulaC25H16F2N4O3Melting Point212-214ºC
MSDS/Flash Point378.1ºC

Names

Name1-(4-fluorophenyl)-N-[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]-2-oxopyridine-3-carboxamide
SynonymMore Synonyms

BMS-2 BiologicalActivity

DescriptionMET 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 CatalogResearch Areas >>CancerSignaling Pathways >>Protein Tyrosine Kinase/RTK >>VEGFRSignaling Pathways >>Protein Tyrosine Kinase/RTK >>c-Met/HGFR
Target

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

In VitroMET 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 VivoMET 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

Density1.5±0.1 g/cm3
Boiling Point701.5ºC at 760 mmHg
Melting Point212-214ºC
Molecular FormulaC25H16F2N4O3
Molecular Weight458.416
Flash Point378.1ºC
Exact Mass458.119049
PSA89.01000
LogP4.82
Index of Refraction1.721
InChIKeyOBSFXHDOLBYWRJ-UHFFFAOYSA-N
SMILESO=C(Nc1ccc(Oc2ccnc3[nH]ccc23)c(F)c1)c1cccn(-c2ccc(F)cc2)c1=O

Synonyms

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-
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