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TL02-59 dihydrochloride

Catalog No. T13186L   CAS 2415263-06-6

TL02-59 dihydrochloride is an orally active inhibitor of Src-family kinase Fgr (IC50: 0.03 nM).

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TL02-59 dihydrochloride Chemical Structure
TL02-59 dihydrochloride, CAS 2415263-06-6
Pack Size Availability Price/USD Quantity
10 mg 4-5 weeks $ 773.00
50 mg 4-5 weeks $ 3,240.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TL02-59 dihydrochloride is an orally active inhibitor of Src-family kinase Fgr (IC50: 0.03 nM).
Targets&IC50 FGR:0.03 nM , Hck:160 nM , Lyn:0.1 nM
In vitro in TF-1 cells, TL02-59 dihydrochloride (0.1-1000 nM; 6 hours) potently inhibits Fgr autophosphorylation , 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. TL02-59 dihydrochloride induces growth arrest in primary AML bone marrow samples. TL02-59 dihydrochloride inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency.
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.
Molecular Weight 682.56
Formula C32H36Cl2F3N5O4
CAS No. 2415263-06-6

Storage

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

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.

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Keywords

TL02-59 dihydrochloride 2415263-06-6 Angiogenesis Tyrosine Kinase/Adaptors Src TL0259 dihydrochloride TL02-59 TL-02-59 dihydrochloride TL02-59 Dihydrochloride TL02 59 dihydrochloride inhibitor inhibit

 

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