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Submit ReviewTL 0259
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 |
| 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 for TL 0259
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 | 29.3 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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Product Datasheets for TL 0259
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
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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
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