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TL02-59

Catalog No. T13186   CAS 1315330-17-6

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.

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TL02-59 Chemical Structure
TL02-59, CAS 1315330-17-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 108.00
5 mg In stock $ 228.00
10 mg In stock $ 372.00
25 mg In stock $ 629.00
50 mg In stock $ 896.00
100 mg In stock $ 1,220.00
1 mL * 10 mM (in DMSO) In stock $ 297.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
Targets&IC50 FGR:0.03 nM , Hck:160 nM , Lyn:0.1 nM
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[1].
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[1].
Molecular Weight 609.64
Formula C32H34F3N5O4
CAS No. 1315330-17-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 120 mg/mL (196.84 mM), Sonication is recommended.

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Metabolism Compound Library Orally Active Compound Library Anti-Pancreatic Cancer Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

TL02-59 1315330-17-6 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors Src Hck TL-02-59 Inhibitor Lyn leukemia inhibit acute orally AML TL02 59 TL0259 myelogenous Fgr inhibitor

 

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