3-(6,7-dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide
- Product Name
- 3-(6,7-dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide
- CAS No.
- 1315330-17-6
- Chemical Name
- 3-(6,7-dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide
- Synonyms
- TL02-59;TL-2-059;TL02-59, 10 mM in DMSO;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-
- CBNumber
- CB74655922
- Molecular Formula
- C32H34F3N5O4
- Formula Weight
- 609.64
- MOL File
- 1315330-17-6.mol
3-(6,7-dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide Property
- 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)
- pka
- 12.86±0.70(Predicted)
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 6981
- Product name
- TL0259
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $1049
- Updated
- 2021/12/16
- Product number
- CS-0067016
- Product name
- TL02-59
- Purity
- 99.52%
- Packaging
- 50mg
- Price
- $1650
- Updated
- 2021/12/16
- Product number
- 189861
- Product name
- 3-(6,7-Dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide
- Packaging
- 500mg
- Price
- $2700
- Updated
- 2021/12/16
- Product number
- CS-0067016
- Product name
- TL02-59
- Purity
- 99.52%
- Packaging
- 5mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0067016
- Product name
- TL02-59
- Purity
- 99.52%
- Packaging
- 10mg
- Price
- $550
- Updated
- 2021/12/16
3-(6,7-dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide Chemical Properties,Usage,Production
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 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.
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
3-(6,7-dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide Preparation Products And Raw materials
Raw materials
Preparation Products
3-(6,7-dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide Suppliers
- Tel
- 025-83697070
- Fax
- +86-25-83453306
- info@chemlin.com.cn
- Country
- China
- ProdList
- 16077
- Advantage
- 64
- Tel
- 021-65675885 18964387627
- Fax
- 021-65675885
- info@efebio.com
- Country
- China
- ProdList
- 9803
- Advantage
- 58
- Tel
- 021-61312847; 18021002903
- Fax
- QQ:3008007432
- 3008007409@qq.com
- Country
- China
- ProdList
- 71826
- Advantage
- 60
- Tel
- 021-QQ:65489617 15618227136
- Fax
- 21-5161 9052
- Sales@ATKchemical.com
- Country
- China
- ProdList
- 9125
- Advantage
- 58
- Tel
- 15911056312
- liming@bio-fount.com
- Country
- China
- ProdList
- 9729
- Advantage
- 58
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
- ProdList
- 32435
- Advantage
- 58
- Tel
- 0512-0512-13601744364 13601744364
- chemsharker@126.com
- Country
- China
- ProdList
- 1010
- Advantage
- 58
- Tel
- 18108052721
- 2850505130@qq.com
- Country
- China
- ProdList
- 5167
- Advantage
- 58
- Tel
- 18818260767
- Fax
- QQ 3610331285
- sales@chemegen.com
- Country
- China
- ProdList
- 11218
- Advantage
- 58
- Tel
- 15865264761
- 486064515@qq.com
- Country
- China
- ProdList
- 4809
- Advantage
- 58