AG-1296A potent inhibitor of PDGFR kinase and c-Kit

AG-1296 (CAS 146535-11-7)

AG-1296 | CAS 146535-11-7 is rated 5.0 out of 5 by 1.
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Synonym: 6,7-Dimethoxy-3-phenylquinoxaline; Tyrphostin AG 1296
Application: A potent inhibitor of PDGFR kinase and c-Kit
CAS Number: 146535-11-7
Purity: >98%
Molecular Weight: 266.29
Molecular Formula: C16H14N2O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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AG-1296 is a potent and selective inhibitor of PDGFR kinase (IC50= 0.4 μM) both in vitro and in cells (Swiss 3T3 cells). This compound also inhibits Bek (FGF receptor) tyrosine kinase and c-kit. Treatment of sis oncogene transfected NIH3T3 cells with AG-1296 reverses the transformed phenotype. It also induces apoptosis in a small-cell lung cancer cell line (H526). AG-1296 is an inhibitor of Tyrosine Kinase. AG-1296 is an inhibitor of PDGFR-α and PDGFR-β.


References

1. Levitzki, A. and Gazit, A. 1995. Science. 267: 1782-1788. PMID: 7892601
2. Kovalenko, M., et al. 1997. Biochemistry. 36: 6260-6269. PMID: 9174341
3. Krystal, G.W., et al. 1997. Cancer Res. 57: 2203-2208. PMID: 9187122
4. Strutz, F., et al. 2001. Kidney Int. 59: 579-592. PMID: 11168939

Physical State :
Solid
Solubility :
Soluble in DMSO (~3 mg/ml), methylene chloride, ACN, DMF (~3 mg/ml), and 1:2 DMF:PBS(pH7.2) (0.3 mg/ml).
Storage :
Store at -20° C
Melting Point :
163.88° C (Predicted)
Boiling Point :
~420.25° C at 760 mmHg (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.62
IC50 :
PDGF receptor tyrosine kinase: IC50 = 1 µM; β-receptors: IC50 = 800 nM; Flt3/Tel-BaF3 cell: IC50 = 300 nM; Flt3/Itd-BaF3 cell: IC50 = ~1 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
2049
MDL Number :
MFCD00270913
SMILES :
COC1=C(C=C2C(=C1)N=CC(=N2)C3=CC=CC=C3)OC

Download SDS (MSDS)

Certificate of Analysis

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AG-1296  Product Citations

See how others have used AG-1296. Click on the entry to view the PubMed entry .

Citations 1 to 5 of 5 total

PMID: # 26444902  Vietti, G. et al. 2016. Nanotoxicology. 10: 488-500.

PMID: # 25824204  Mohd Abdul Rashid, MB. et al. 2015. J Lab Autom. 20: 423-37.

PMID: # 10688905  Nebigil, CG. et al. 2000. Proc. Natl. Acad. Sci. U.S.A. 97: 2591-2596.

PMID: # 9468525  Gohla, A. et al. 1998. J. Biol. Chem. 273: 4653-4659.

PMID: # 9287333  Arteaga, CL. et al. 1997. J. Biol. Chem. 272: 23247-23254.

Citations 1 to 5 of 5 total
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Rated 5 out of 5 by from Nebigil et al Nebigil et al. (PubMed ID 10688905) used AG-1296, a platelet-derived growth factor receptor (PDGFR) kinase inhibitor, to decrease 5-HT-induced phosphorylation of PDGFR. -SCBT Publication Review
Date published: 2015-04-09
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