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SU 4984

Names

[ CAS No. ]:
186610-89-9

[ Name ]:
SU 4984

Biological Activity

[Description]:

SU4984 is a protein tyrosine kinase inhibitor, with an IC50 of 10-20 μM for fibroblast growth factor receptor 1 (FGFR1). SU4984 is also inhibits platelet-derived growth factor receptor, and insulin receptor. SU4984 can be used for the research of cancer[1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Insulin Receptor

[Target]

FGFR1:10-20 μM (IC50)


[In Vitro]

SU4984 (5-100 μM; 5 min) inhibits the kinase activity of FGFR1K with an IC50 of 10-20 μM in the presence of 1 mM adenosine triphosphate (ATP)[1]. SU4984 (10-90 μM; 5 min) inhibits the autophosphorylation of FGFR1 induced by aFGF in NIH 3T3 cells, with an IC50 of 20-40 μM[1]. SU4984 (5 μM) substantially reduces tyrosine phosphorylation of the wild-type receptor and reduces 50% phosphorylation of constitutive C2 KIT[2]. SU4984 (1-10 μM; 6 days) kills the C2 and P815 cells[2].

[References]

[1]. Mohammadi M, et, al. Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors. Science. 1997 May 9;276(5314):955-60.

[2]. Ma Y, et, al. Indolinone derivatives inhibit constitutively activated KIT mutants and kill neoplastic mast cells. J Invest Dermatol. 2000 Feb;114(2):392-4.

Chemical & Physical Properties

[ Density]:
1.34g/cm3

[ Boiling Point ]:
649.1ºC at 760 mmHg

[ Molecular Formula ]:
C20H19N3O2

[ Molecular Weight ]:
333.38400

[ Flash Point ]:
346.4ºC

[ Exact Mass ]:
333.14800

[ PSA ]:
52.65000

[ LogP ]:
3.23450

[ Vapour Pressure ]:
9.81E-17mmHg at 25°C

[ Index of Refraction ]:
1.72

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds