1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. Src
    Apoptosis
  3. TL02-59

TL02-59 

Cat. No.: HY-112852
Handling Instructions

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

For research use only. We do not sell to patients.

TL02-59 Chemical Structure

TL02-59 Chemical Structure

CAS No. : 1315330-17-6

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Description

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

IC50 & Target

IC50: 0.03 nM (Fgr)[1]

In Vitro

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

Western Blot Analysis[1]

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.
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[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
Dosage: 1 and 10 mg/kg
Administration: Oral administration; 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.
Molecular Weight

609.64

Formula

C₃₂H₃₄F₃N₅O₄

CAS No.

1315330-17-6

SMILES

O=C(NC1=CC=C(CN2CCN(CC)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(OC4=C5C=C(OC)C(OC)=CC5=NC=N4)=C3

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TL02-59
Cat. No.:
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