1315330-17-6
1315330-17-6 structure
- Name: TL02-59
- Chemical Name: 3-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N-{4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl}-4-methylbenzamide
- CAS Number: 1315330-17-6
- Molecular Formula: C32H34F3N5O4
- Molecular Weight: 609.639
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2019-01-20 06:37:12
- Modify Date: 2024-01-10 17:40:08
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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].
| Name | 3-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N-{4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl}-4-methylbenzamide |
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| 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 |
| 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]. |
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| 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 |
| 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 |