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ChemicalBook--->CAS DataBase List--->1315330-17-6

1315330-17-6

1315330-17-6 Structure

1315330-17-6 Structure
IdentificationBack Directory
[Name]

3-(6,7-dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide
[CAS]

1315330-17-6
[Synonyms]

TL02-59
TL-02-59,Inhibitor,Lyn,Apoptosis,leukemia,inhibit,acute,Src,orally,AML,TL02-59,TL02 59,TL0259,Hck,myelogenous,Fgr
3-(6,7-dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide
Benzamide, 3-[(6,7-dimethoxy-4-quinazolinyl)oxy]-N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-
[Molecular Formula]

C32H34F3N5O4
[MDL Number]

MFCD29991221
[MOL File]

1315330-17-6.mol
[Molecular Weight]

609.64
Chemical PropertiesBack Directory
[Boiling point ]

630.5±55.0 °C(Predicted)
[density ]

1.290±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO: 125 mg/mL (205.04 mM)
[form ]

Solid
[pka]

12.86±0.70(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth[1].
[Biological Activity]

TL02-59 is a potent inhibitor of Fgr kinasea Src-family kinase expressed in myeloid cells and associated with acute myelogenous leukemia (AML). It exhibited an IC50 value of 0.03 nM for Fgr0.10 nM for related Src-family kinase Lynwith >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.
[in vivo]

TL02-59 (oral administration; 1 and 10 mg/kg; for three weeks) completely eliminates AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement[1].
? TL02-59 has a t1/2 of 5.7 h by i.v injection and 6.5 h by p.o. administration, respectively[1].

Animal Model:NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) mice with human MV4-11 AML cells[1]
Dosage:1 and 10 mg/kg
Administration:Oral; for three weeks
Result:Eliminated AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement.
[References]

[1] Weir MC, et al. Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo. ACS Chem Biol. 2018 Jun 15;13(6):1551-1559. DOI:10.1021/acschembio.8b00154
Spectrum DetailBack Directory
[Spectrum Detail]

3-(6,7-dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide(1315330-17-6)1HNMR
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