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AG 1295

Catalog No. T14137   CAS 71897-07-9

AG 1295, a selective inhibitor of platelet-derived growth factor receptor (PDGFR) tyrosine-kinase, effectively halts PDGFR autophosphorylation without impacting the autophosphorylation of the EGF receptor[1][2][3][4].

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AG 1295 Chemical Structure
AG 1295, CAS 71897-07-9
Pack Size Availability Price/USD Quantity
5 mg In stock $ 47.00
10 mg In stock $ 80.00
25 mg In stock $ 146.00
50 mg In stock $ 247.00
100 mg In stock $ 372.00
1 mL * 10 mM (in DMSO) In stock $ 52.00
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Purity: 99.64%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AG 1295, a selective inhibitor of platelet-derived growth factor receptor (PDGFR) tyrosine-kinase, effectively halts PDGFR autophosphorylation without impacting the autophosphorylation of the EGF receptor[1][2][3][4].
In vitro AG1295 (10 μM, 100 μM) significantly inhibits rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB in vitro[2]. AG 1295 inhibits PDGFR autophosphorylation with IC50s of 0.3-0.5 μM and 0.5-1 μM for membrane autophosphorylation assays and Swiss 3T3 cells, respectively[1].
In vivo AG-1295 reduces neointimal formation in aortic allograft vasculopathy by inhibition of PDGFR-beta-triggered tyrosine phosphorylation[3]. AG1295 (12 mg/kg; i.p.; daily; for 14 or 21 days) significantly reduces interstitial fibrosis as verified by a smaller Sirius-Red stained area, and by a reduced number of macrophages, and by the ED-A+ fibronectin deposition. It is also verified by the number of cells positive for alpha-smooth muscle actin[4].
Molecular Weight 234.3
Formula C16H14N2
CAS No. 71897-07-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL (256.08 mM), Sonification is recommended.

TargetMolReferences and Literature

1. Kovalenko M, et al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Res. 1994 Dec 1;54(23):6106-14. 2. Zheng Y, et al. Platelet-derived growth factor receptor kinase inhibitor AG1295 and inhibition of experimental proliferative vitreoretinopathy. Jpn J Ophthalmol. 2003 Mar-Apr;47(2):158-65. 3. Inhibition of aortic allograft vasculopathy by local delivery of platelet-derived growth factor receptor tyrosine-kinase blocker AG-129Transplantation. 2002 Nov 15;74(9):1335-41. 4. Ludewig D, et al. PDGF receptor kinase blocker AG1295 attenuates interstitial fibrosis in rat kidney after unilateral obstruction. Cell Tissue Res. 2000 Jan;299(1):97-103.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Anti-Lung Cancer Compound Library Reprogramming Compound Library NO PAINS Compound Library Angiogenesis related Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Cytokine Inhibitor Library

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Nintedanib esylate Vatalanib dihydrochloride Olaratumab TAK-632 Ilorasertib Lenvatinib mesylate Ponatinib Hydrochloride PDGFRα kinase inhibitor 1

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Keywords

AG 1295 71897-07-9 Angiogenesis Tyrosine Kinase/Adaptors PDGFR Platelet-derived growth factor receptor RTK AG-1295 inhibit PDGF-receptor autophosphorylation Inhibitor AG1295 inhibitor

 

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