TL 0259

Pricing Availability   Qty
Cat.No. 6981 - TL 0259 | C32H34F3N5O4.2HCl
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)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity

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

Technical Data

M. Wt 682.56
Formula C32H34F3N5O4.2HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
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 Data

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

Preparing Stock Solutions

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

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


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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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Literature in this Area

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