TL 0259

Name: TL 0259
Brand: Tocris Bioscience
SKU: 6981

Tocris Bioscience, part of Bio-Techne | Catalog # 6981

Citations (79)

COA / SDS

Selective and highly potent Fgr and Lyn kinase inhibitor; orally bioavailable

Key Product Details

Description:	Selective and highly potent Fgr and Lyn kinase inhibitor; orally bioavailable
Chemical Name:	3-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methylbenzamide dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	682.56

View Full Technical Details for TL 0259

Technical Data
Citations

Biological Activity for TL 0259

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.

Licensing Information

Sold under license from Dana-Farber Cancer Institute

Compound Libraries for TL 0259

TL 0259 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for TL 0259

M. Wt	682.56
Formula	C₃₂H₃₄F₃N₅O₄.2HCl
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2415263-06-6
InChi Key	AMHWQBGAKJESFB-UHFFFAOYSA-N
Smiles	CCN1CCN(CC1)CC2=C(C(F)(F)F)C=C(C=C2)NC(C3=CC=C(C(OC4=NC=NC5=C4C=C(C(OC)=C5)OC)=C3)C)=O.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for TL 0259

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	34.13	50

Preparing Stock Solutions for TL 0259

The following data is based on the product molecular weight 682.56.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	2.93 mL	14.65 mL	29.30 mL
2.5 mM	0.59 mL	2.93 mL	5.86 mL
5 mM	0.29 mL	1.47 mL	2.93 mL
25 mM	0.06 mL	0.29 mL	0.59 mL

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References for TL 0259

References are publications that support the biological activity of the product.

Weir Selective inhibition of the myeloid Src-family kinase Fgr potently suppresses AML cell growth in vitro and in vivo. ACS Chem.Biol. 2018 PMID: 29763550