TL02-59

TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC 50 of 0.03 nM. TL02-59 inhibits Lyn and Hck with IC 50 s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth In Vitro TL02-59 (0.1-1000 nM; 6 hours) potently inhibits Fgr autophosphorylation in TF-1 cells, with paritial inhibition at 0.1-1 nM and complete inhibition above 10 nM. Hck, Lyn and Flt3 are inhibited in the 100 to 1000 nM range. TL02-59 inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency. TL02-59 induces growth arrest in primary AML bone marrow samples. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: TF-1 myeloid cells Concentration: 0.1, 1, 10, 100, 1000 nM Incubation Time: 6 hours Result: Inhibited Fgr autophosphorylation in TF-1 cells. In Vivo TL02-59 (oral administration; 1 and 10 mg/kg; for three weeks) completely eliminates AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement . TL02-59 has a t 1/2 of 5.7 h by i.v injection and 6.5 h by p.o. administration, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NOD.Cg-Prkdc scid Il2rg tm1Wjl /SzJ (NSG) mice with human MV4-11 AML cells Dosage: 1 and 10 mg/kg Administration: Oral; for three weeks Result: Eliminated AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement. Form:Solid IC50& Target:IC50: 0.03 nM (Fgr), 0.1 nM (Lyn) and 160 nM (Hck)

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