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TYRPHOSTIN AG 1296

Product Name
TYRPHOSTIN AG 1296
CAS No.
146535-11-7
Chemical Name
TYRPHOSTIN AG 1296
Synonyms
1296;AG 1296;A 1296;AG-1296;AG 1296;;TYRPHOSTIN AG 1296;Tyrphostin AG 1296 ,S8024;TYRPHOSTIN AG 1296 USP/EP/BP;Tyrphostin AG 1296 (AG 1296);AG-1296 (Tyrphostin AG 1296);Tyrphostin AG1296, 10 mM in DMSO
CBNumber
CB7435034
Molecular Formula
C16H14N2O2
Formula Weight
266.29
MOL File
146535-11-7.mol
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TYRPHOSTIN AG 1296 Property

Boiling point:
420.2±40.0 °C(Predicted)
Density 
1.192±0.06 g/cm3(Predicted)
storage temp. 
Keep in dark place,Sealed in dry,Store in freezer, under -20°C
solubility 
Soluble in DMSO.
form 
White solid
pka
0.48±0.30(Predicted)
color 
Yellow
Sensitive 
Light Sensitive
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

TCI Chemical
Product number
D4601
Product name
AG-1296
Purity
min. 98.0 %
Packaging
5MG
Price
$102
Updated
2025/07/31
TCI Chemical
Product number
D4601
Product name
AG-1296
Purity
min. 98.0 %
Packaging
25MG
Price
$303
Updated
2025/07/31
Cayman Chemical
Product number
10010592
Product name
AG 1296
Purity
>98%
Packaging
1mg
Price
$28
Updated
2024/03/01
Cayman Chemical
Product number
10010592
Product name
AG 1296
Purity
>98%
Packaging
5mg
Price
$117
Updated
2024/03/01
Cayman Chemical
Product number
10010592
Product name
AG 1296
Purity
>98%
Packaging
10mg
Price
$207
Updated
2024/03/01
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TYRPHOSTIN AG 1296 Chemical Properties,Usage,Production

Description

Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of atherosclerosis, restenosis, pulmonary fibrosis, and gliomas. AG-1296 is a potent and selective inhibitor of PDGF receptor kinase with an IC50 value of about 0.4 μM both in vitro and in cells (Swiss 3T3 cells). It inhibits ligand-stimulated DNA synthesis in platelet-derived growth factor receptor and stem cell factor/kit receptor transfected cells with an IC50 values of 1.5 and 1.8 μM, respectively. Treatment of sis oncogene transfected NIH3T3 cells with AG-1296 reverses the transformed phenotype.

Uses

Tyrphostin AG 1296, is the platelet-derived growth factor receptor (PDGFR) inhibitor, which can causes growth inhibition in glioblastoma cells.

Definition

ChEBI: 6,7-dimethoxy-2-phenylquinoxaline is a quinoxaline derivative.

Synthesis

582-24-1

27841-33-4

146535-11-7

GENERAL METHODS: Triphenyltin (35.5 mg, 0.1 mmol, 10 mol%) and 4,5-dimethoxy-1,2-phenylenediamine (1.2 mmol) were sequentially added to a solution of 2-hydroxyacetophenone (1 mmol) in toluene (6 mL) under air atmosphere. The reaction mixture was stirred at room temperature and the progress of the reaction was monitored by thin layer chromatography (TLC). Upon completion of the reaction, the solvent was removed by concentration under reduced pressure and the resulting residue was purified by silica gel column chromatography with dichloromethane (CH2Cl2) as eluent. The structure of the final product, 6,7-dimethoxy-2-phenylquinoxaline, was analyzed by melting point determination, nuclear magnetic resonance (NMR) spectroscopy and mass spectrometry (MS) and confirmed by comparison with literature data.

in vivo

Tyrphostin AG1296 (40 and 80 mg/kg; i.p. daily for two weeks) suppresses A375R tumor growth in vivo[4].
? Tyrphostin AG1296 (2 mg/kg; i.p. every other day for 3 weeks) inhibits the atherosclerotic plaque progression and enhances plaque stability by inhibiting inflammatory responses, reducing the expression of matrix metalloproteinases and promoting macrophages from proinflammatory phenotype to anti-inflammatory phenotype[5].

Animal Model:Nud/nud mice are injected with A375R cells[4]
Dosage:40, 80 mg/kg
Administration:I.p. daily for two weeks
Result:Led to an intermediate level of tumor growth suppression at dose of 40 mg/kg, and significant inhibition of A375R tumor growth at dose of 80 mg/kg.
Well tolerated by healthy mice without significant signs of overt toxicity or weight loss.

target

PDGFR

IC 50

PDGFRα; PDGFRβ

References

[1] MARINA KOVALENKO. Phosphorylation Site-Specific Inhibition of Platelet-Derived Growth Factor β-Receptor Autophosphorylation by the Receptor Blocking Tyrphostin AG1296[J]. Biochemistry Biochemistry, 1997, 36 21: 6260-6269. DOI:10.1021/bi962553l
[2] G W KRYSTAL  J L  P Carlson. Induction of apoptosis and inhibition of small cell lung cancer growth by the quinoxaline tyrphostins.[J]. Cancer research, 1997, 57 11: 2203-2208.
[3] F. STRUTZ. TGF-beta 1 induces proliferation in human renal fibroblasts via induction of basic fibroblast growth factor (FGF-2).[J]. Kidney international, 2001, 69 1: 579-592. DOI:10.1046/j.1523-1755.2001.059002579.x

TYRPHOSTIN AG 1296 Preparation Products And Raw materials

Raw materials

Preparation Products

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TYRPHOSTIN AG 1296 Suppliers

Shanghai Boyle Chemical Co., Ltd.
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Fax
86-21-57758967
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sales@boylechem.com
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China
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J & K SCIENTIFIC LTD.
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18210857532; 18210857532
Fax
86-10-82849933
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jkinfo@jkchemical.com
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China
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Adamas Reagent, Ltd.
Tel
400-6009262 16621234537
Fax
021-64823266
Email
chenyj@titansci.com
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China
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Jinan Trio PharmaTech Co., Ltd.
Tel
0531-88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com
Country
China
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Spectrum Chemical Manufacturing Corp.
Tel
021-021-021-67601398-809-809-809 15221380277
Fax
021-57711696
Email
marketing_china@spectrumchemical.com
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China
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Jinan Bond Chemical Technology Co., Ltd.
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86-531-88280989
Fax
86-531-88280989
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mymail1996@126.com
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China
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256
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Jiangsu Aikon Biopharmaceutical R&D co.,Ltd.
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025-66113011 17798518460
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(1)02557626880
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cfzhang@aikonchem.com
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China
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TOKYO CHEMICAL INDUSTRY CO., LTD.
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03-36680489
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03-3668-0520
Email
Sales-JP@TCIchemicals.com
Country
Japan
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28387
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TCI Europe
Tel
320-37350700
Fax
+32 (0)37350701
Email
sales@tcieurope.eu
Country
Europe
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23671
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TCI AMERICA
Tel
800-4238616
Fax
+1-888-520-1075 / +1-503-283-1987
Email
sales@tciamerica.com
Country
Americas
ProdList
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View Lastest Price from TYRPHOSTIN AG 1296 manufacturers

Career Henan Chemical Co
Product
TYRPHOSTIN AG 1296 146535-11-7
Price
US $1.00/g
Min. Order
1g
Purity
99%
Supply Ability
200kg
Release date
2019-12-25

146535-11-7, TYRPHOSTIN AG 1296Related Search:


  • TYRPHOSTIN AG 1296
  • AG 1296
  • 6,7-DIMETHOXY-2-PHENYLQUINOXALINE
  • 6,7-DIMETHOXY-3-PHENYLQUINOXALINE
  • Quinoxaline,6,7-dimethoxy-2-phenyl-
  • AG-1296;AG 1296;
  • AG 1296 - CAS 146535-11-7 - Calbiochem
  • AG-1296 (Tyrphostin AG 1296)
  • Tyrphostin AG 1296 (AG 1296)
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  • A 1296
  • AG 1296, protein tyrosine kinase inhibitor
  • Tyrphostin AG1296, 10 mM in DMSO
  • Tyrphostin AG 1296 ,S8024
  • 146535-11-7
  • BioChemical
  • Cell Biology
  • Cell Signaling and Neuroscience
  • Receptor Tyrosine Kinase Inhibitors
  • Platelet Derived Growth Factor Receptor (PDGFR)
  • Kinase/Phosphatase Biology
  • Inhibitors