ChemicalBook > CAS DataBase List > 3-(6,7-dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide

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
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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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Tocris
Product number
6981
Product name
TL0259
Purity
≥98%(HPLC)
Packaging
50
Price
$1049
Updated
2021/12/16
ChemScene
Product number
CS-0067016
Product name
TL02-59
Purity
99.52%
Packaging
50mg
Price
$1650
Updated
2021/12/16
Matrix Scientific
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
ChemScene
Product number
CS-0067016
Product name
TL02-59
Purity
99.52%
Packaging
5mg
Price
$350
Updated
2021/12/16
ChemScene
Product number
CS-0067016
Product name
TL02-59
Purity
99.52%
Packaging
10mg
Price
$550
Updated
2021/12/16
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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

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

Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
16077
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Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
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Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
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71826
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Shanghai Chaolan Chemical Technology Center
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021-QQ:65489617 15618227136
Fax
21-5161 9052
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Sales@ATKchemical.com
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China
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9125
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Fan De(Beijing) Biotechnology Co., Ltd.
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15911056312
Email
liming@bio-fount.com
Country
China
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9729
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58
TargetMol Chemicals Inc.
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+1-781-999-5354; +17819995354
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marketing@targetmol.com
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United States
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32435
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Shanghai Dongyang Biotechnology Co., Ltd.
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0512-0512-13601744364 13601744364
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chemsharker@126.com
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China
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1010
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Chengdu Peter-like Biotechnology Co., Ltd.
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18108052721
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2850505130@qq.com
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China
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5167
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ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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18818260767
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QQ 3610331285
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sales@chemegen.com
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China
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11218
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Jinan Jiuli Biotechnology Co. , Ltd.
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15865264761
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486064515@qq.com
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China
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4809
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1315330-17-6, 3-(6,7-dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamideRelated Search:


  • TL02-59
  • 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-
  • TL-02-59,Inhibitor,Lyn,Apoptosis,leukemia,inhibit,acute,Src,orally,AML,TL02-59,TL02 59,TL0259,Hck,myelogenous,Fgr
  • TL-2-059
  • TL02-59, 10 mM in DMSO
  • 1315330-17-6
  • C32H34F3N5O4