| Identification | Back Directory | [Name]
TL02-59 dihydrochloride | [CAS]
2415263-06-6 | [Synonyms]
TL02-59 dihydrochloride
TL0259 dihydrochloride,TL-02-59 dihydrochloride,TL02 59 dihydrochloride | [Molecular Formula]
C32H35ClF3N5O4 | [MDL Number]
MFCD34470292 | [MOL File]
2415263-06-6.mol | [Molecular Weight]
646.11 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
TL 0259 is a selective and highly potent Fgr and Lyn inhibitor (IC50 values are 0.03 and 0.1 nM, respectively). Exhibits selectivity for Fgr and Lyn over other Src family kinases and other nonreceptor and receptor tyrosine kinases. Suppresses proliferation of acute myelogenous leukemia (AML) cell lines in vitro. Eliminates leukemic cells from spleen and bone of mice bearing AML xenografts. Orally bioavailable. | [in vivo]
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 t1/2 of 5.7 h by i.v injection and 6.5 h by p.o. administration, respectively[1]. | Animal Model: | NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) mice with human MV4-11 AML cells[1] | | 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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Store at -20°C | [References]
[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. DOI:10.1021/acschembio.8b00154 |
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