TL 0259

Pricing Availability   Qty
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)

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
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 Data for TL 0259

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 2.93 mL 14.65 mL 29.3 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 et al (2018) Selective inhibition of the myeloid Src-family kinase Fgr potently suppresses AML cell growth in vitro and in vivo. ACS Chem.Biol. 13 1551 PMID: 29763550

If you know of a relevant reference for TL 0259, please let us know.

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Keywords: TL 0259, TL 0259 supplier, TL0259, Fgr, Lyn, Src, family, nonreceptor, tyrosine, kinases, inhibitors, inhibits, potent, selective, orally, bioavailable, Kinases, 6981, Tocris Bioscience

Citations for TL 0259

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