SML3202

TL02-59

≥98% (HPLC)

• Synonym(s): 3-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methylbenzamide
• Empirical Formula (Hill Notation): C₃₂H₃₄F₃N₅O₄
• CAS Number: 1315330-17-6
• Molecular Weight: 609.64
• MDL number: MFCD29991221
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: −20°C
• SMILES string: O=C(NC1=CC(C(F)(F)F)=C(CN2CCN(CC)CC2)C=C1)C3=CC(OC4=C(C=C(C(OC)=C5)OC)C5=NC=N4)=C(C)C=C3
• InChI: 1S/C32H34F3N5O4/c1-5-39-10-12-40(13-11-39)18-22-8-9-23(15-25(22)32(33,34)35)38-30(41)21-7-6-20(2)27(14-21)44-31-24-16-28(42-3)29(43-4)17-26(24)36-19-37-31/h6-9,14-17,19H,5,10-13,18H2,1-4H3,(H,38,41)
• InChI key: AMHWQBGAKJESFB-UHFFFAOYSA-N

Description

Biochem/physiol Actions

Inhibitor of the Myeloid Src-Family Kinase Fgr

TL02-59 is a potent inhibitor of Fgr kinase, a Src-family kinase expressed in myeloid cells and associated with acute myelogenous leukemia (AML). It exhibited an IC50 value of 0.03 nM for Fgr, 0.10 nM for related Src-family kinase Lyn, with >1000-fold less potency for all other kinases tested. TL02-59 given orally in a mouse xenograft model of AML was able to eliminate spleen and peripheral blood leukemic cells and significantly reduce bone marrow engraftment.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable