TL02-59

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TL02-59 是 Src 家族激酶中 Fgr 的选择性抑制剂 (IC50 = 0.03 nM)。 TL02-59 抑制 Lyn 和 Hck，IC50 分别为 0.1 nM 和 160 nM。

TL02-59 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.(In Vitro):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.(In Vivo):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.

Western Blot Analysis Cell 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.

Animal Model:NOD.Cg-PrkdcscidIl2rgtm1Wjl/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.

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Apoptosis

Apoptosis

ELOVL1

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1315330-17-6

609.65

C32H34F3N5O4

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (205.04 mM)

CCN1CCN(Cc2ccc(NC(=O)c3ccc(C)c(Oc4ncnc5cc(OC)c(OC)cc45)c3)cc2C(F)(F)F)CC1

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(-20℃)

With Ice Pack

≥ 2 years