TL02-59 是 Src 家族激酶中 Fgr 的特异性抑制剂 (IC50 = 0.03 nM)。 TL02-59 抑制 Lyn 和 Hck，IC50 分别为 0.1 nM 和 160 nM。 TL02-59 有效抑制急性髓性白血病细胞的生长。

TL02-59 is a selective inhibitor of Fgr in Src-family kinase (IC50 = 0.03 nM). TL02-59 inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia cell growth.

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. In TF-1 myeloid cells, TL02-59 (0.1, 1, 10, 100, 1000 nM; 6 h) 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].

In mice, TL02-59 (1, 10 mg/kg; oral) completely eliminates AML cells from the spleen and peripheral blood while dramatically suppressing bone marrow involvement. TL02-59 has a t1/2 of 5.7 h by i.v and 6.5 h by p.o., respectively[1].

1315330-17-6

C32H34F3N5O4

609.64

DMSO:125 mg/mL (205.04 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years