Title : SU5416 and SU5614 inhibit kinase activity of wild-type and mutant FLT3 receptor tyrosine kinase.

Pub. Date : 2002 Oct 15

PMID : 12351406






5 Functional Relationships(s)
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1 SU5416 and SU5614 inhibit kinase activity of wild-type and mutant FLT3 receptor tyrosine kinase. SU 5614 fms related receptor tyrosine kinase 3 Homo sapiens
2 Both SU5416 and SU5614 were capable of inhibiting autophosphorylation of ITD and WT FLT3 (SU5416 concentration that inhibits 50% [IC(50)], 100 nM; and SU5614 IC(50) 10 nM). SU 5614 fms related receptor tyrosine kinase 3 Homo sapiens
3 FLT3 inhibition by SU5416 and SU5614 resulted in reduced proliferation (IC(50), 250 nM and 100 nM, respectively) and induction of apoptosis of FLT3 ITD-positive leukemic cell lines. SU 5614 fms related receptor tyrosine kinase 3 Homo sapiens
4 FLT3 inhibition by SU5416 and SU5614 resulted in reduced proliferation (IC(50), 250 nM and 100 nM, respectively) and induction of apoptosis of FLT3 ITD-positive leukemic cell lines. SU 5614 fms related receptor tyrosine kinase 3 Homo sapiens
5 We conclude that SU5416 and SU5614 are potent inhibitors of FLT3. SU 5614 fms related receptor tyrosine kinase 3 Homo sapiens