TL02-59 dihydrochloride 

TL02-59 dihydrochloride is an orally active, selective Src-family kinase Fgr inhibitor with an IC₅₀ of 0.03 nM. TL02-59 dihydrochloride inhibits Lyn and Hck with IC₅₀s of 0.1 nM and 160 nM, respectively. TL02-59 dihydrochloride potently suppresses acute myelogenous leukemia (AML) cell growth^[1].

IC50: 0.03 nM (Fgr), 0.1 nM (Lyn) and 160 nM (Hck)^[1]

TL02-59 dihydrochloride (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^[1].
TL02-59 dihydrochloride inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency^[1].
TL02-59 dihydrochloride induces growth arrest in primary AML bone marrow samples^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

TL02-59 (oral; 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^[1].
TL02-59 has a t_1/2 of 5.7 h by i.v injection and 6.5 h by p.o. administration, respectively^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

682.56

C₃₂H₃₆Cl₂F₃N₅O₄

2415263-06-6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Weir MC, et al. Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo. ACS Chem Biol. 2018 Jun 15;13(6):1551-1559.  [Content Brief]