BMS-2

Modify Date: 2024-02-06 20:04:08

BMS-2 Structure
BMS-2 structure
Common Name BMS-2
CAS Number 888719-03-7 Molecular Weight 458.416
Density 1.5±0.1 g/cm3 Boiling Point 701.5ºC at 760 mmHg
Molecular Formula C25H16F2N4O3 Melting Point 212-214ºC
MSDS N/A Flash Point 378.1ºC

 Use of BMS-2


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].

 Names

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

 BMS-2 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
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

~78%

BMS-2 Structure

BMS-2

CAS#:888719-03-7

Literature: Kyoung, Soon Kim; Zhang, Liping; Schmidt, Robert; Cai, Zhen-Wei; Wei, Donna; Williams, David K.; Lombardo, Louis J.; Trainor, George L.; Xie, Dianlin; Zhang, Yaquan; An, Yongmi; Sack, John S.; Tokarski, John S.; Darienzo, Celia; Kamath, Amrita; Marathe, Punit; Zhang, Yueping; Lippy, Jonathan; Jeyaseelan Sr., Robert; Wautlet, Barri; Henley, Benjamin; Gullo-Brown, Johnni; Manne, Veeraswamy; Hunt, John T.; Fargnoli, Joseph; Borzilleri, Robert M. Journal of Medicinal Chemistry, 2008 , vol. 51, # 17 p. 5330 - 5341

 Precursor & DownStream

Precursor  2

DownStream  0

 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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