TL02-59

Modify Date: 2024-01-10 17:40:08

TL02-59 Structure
TL02-59 structure
Common Name TL02-59
CAS Number 1315330-17-6 Molecular Weight 609.639
Density 1.3±0.1 g/cm3 Boiling Point 630.5±55.0 °C at 760 mmHg
Molecular Formula C32H34F3N5O4 Melting Point N/A
MSDS N/A Flash Point 335.1±31.5 °C

 Use of TL02-59


TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 also 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].

 Names

Name 3-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N-{4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl}-4-methylbenzamide
Synonym More Synonyms

 TL02-59 Biological Activity

Description TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 also 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].
Related Catalog
Target

IC50: 0.03 nM (Fgr)[1]

In Vitro TL02-59 inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency[1]. TL02-59 induces growth arrest in primary AML bone marrow samples[1]. TL02-59 (0.1-1000 nM; 6 hours) potently inhibits Fgr autophosphorylation in TF-1 cells, with paritial inhibition at 0.1-1 nM and complete inhibition above 10 nM. Hck, Lyn and Flt3 are inhibited in the 100 to 1000 nM range[1]. Western Blot Analysis[1] Cell Line: TF-1 myeloid cells Concentration: 0.1, 1, 10, 100, 1000 nM Incubation Time: 6 hours Result: Inhibited Fgr autophosphorylation in TF-1 cells.
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 Dosage: 1 and 10 mg/kg Administration: Oral administration; 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.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 630.5±55.0 °C at 760 mmHg
Molecular Formula C32H34F3N5O4
Molecular Weight 609.639
Flash Point 335.1±31.5 °C
Exact Mass 609.256287
LogP 5.22
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.603

 Synonyms

Benzamide, 3-[(6,7-dimethoxy-4-quinazolinyl)oxy]-N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-
3-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N-{4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl}-4-methylbenzamide
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