AG 1295
Based on 4 publication(s) in Google Scholar
AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor.
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- Pureza: 99.86%
- No. CAS: 71897-07-9
- Fòrmula: C16H14N2
- Peso molecular:234.30
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) AG 1295
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Actividad biológica
PDGFR[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| EOL1 | IC50 |
1.1 μM
Compound: 1a
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Inhibition of endogenous FLT3 in EOL1 cells
Inhibition of endogenous FLT3 in EOL1 cells
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[PMID: 16722630] |
| EOL1 | IC50 |
1.1 μM
Compound: AG-1295
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Inhibition of endogenous FLT3 autophosphorylation in EOL1 cells
Inhibition of endogenous FLT3 autophosphorylation in EOL1 cells
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[PMID: 17210255] |
| MV4-11 | IC50 |
2.2 μM
Compound: AG1295
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Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay
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[PMID: 32659083] |
| NIH3T3 | IC50 |
0 μM
Compound: AG-1295
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Antitumor activity measured by the inhibition of platelet-derived growth factor receptor autophosphorylation in intact Swiss 3T3 cells
Antitumor activity measured by the inhibition of platelet-derived growth factor receptor autophosphorylation in intact Swiss 3T3 cells
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[PMID: 11855980] |
| NIH3T3 | IC50 |
0.4 μM
Compound: 25
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Inhibitory activity against platelet-derived growth factor receptor tyrosine kinase in Swiss 3T3 cells
Inhibitory activity against platelet-derived growth factor receptor tyrosine kinase in Swiss 3T3 cells
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[PMID: 8667360] |
| SF-539 | IC50 |
6.2 μM
Compound: 22, AG-1295
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Inhibition of PDGFBB-induced PDGFRbeta autophosphorylation in human SF539 cells incubated for 60 mins prior to PDGFBB-induction measured after 10 mins by phosphotyrosine ELISA
Inhibition of PDGFBB-induced PDGFRbeta autophosphorylation in human SF539 cells incubated for 60 mins prior to PDGFBB-induction measured after 10 mins by phosphotyrosine ELISA
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[PMID: 22370340] |
| SF-539 | IC50 |
6.2 μM
Compound: 28
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Inhibition of PDGF-BB-induced PDGFR beta phosphorylation in human SF539 cells overexpressing PDGFR beta pretreated for 60 mins prior to PDGF-BB addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis
Inhibition of PDGF-BB-induced PDGFR beta phosphorylation in human SF539 cells overexpressing PDGFR beta pretreated for 60 mins prior to PDGF-BB addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis
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[PMID: 23375090] |
| U-251 | IC50 |
6.2 μM
Compound: 18, AG-1295
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Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA
Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA
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[PMID: 19748785] |
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].
AG1295 (10 μM, 100 μM) significantly inhibits rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB in vitro[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Rabbit conjunctival fibroblasts cells
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Concentration:1 μM, 10 μM, 100 μM
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Incubation Time:3 days
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Result:Inhibited rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB.
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 also by a reduced number of macrophages, and by the ED-A+ fibronectin deposition and the number of cells positive for alpha-smooth muscle actin[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (240-270 g)[4]
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Dosage:12 mg/kg
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Administration:Intraperitoneal injection; daily; for 14 or 21 days
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Result:Attenuated interstitial fibrosis in rat kidney after unilateral obstruction.
Chemical Information
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No. CAS 71897-07-9
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Appearance Solid
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Peso molecular 234.30
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Fòrmula C16H14N2
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Color Light yellow to yellow
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SMILES
CC1=C(C)C=C2N=CC(C3=CC=CC=C3)=NC2=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Proc Natl Acad Sci U S A
Endocytosis triggers V-ATPase-SYK-mediated priming of cGAS activation and innate immune response. [Abstract]2022 Oct 25;119(43):e2207280119. PMID: 36252040 -
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J Clin Transl Hepatol
Hydrogen Sulfide Promotes Platelet Autophagy via PDGFR-α/PI3K/Akt Signaling in Cirrhotic Thrombocytopenia. [Abstract]2024 Jul 28;12(7):625-633. PMID: 38993511 -
Commun Biol
2025 Mar 17;8(1):451. PMID: 40097701
Solvente y solubilidad
DMSO : 50 mg/mL (213.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[3]. Inhibition of aortic allograft vasculopathy by local delivery of platelet-derived growth factor receptor tyrosine-kinase blocker AG-1295. Transplantation. 2002 Nov 15;74(9):1335-41. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.2680 mL | 21.3402 mL | 42.6803 mL | 106.7008 mL |
| 5 mM | 0.8536 mL | 4.2680 mL | 8.5361 mL | 21.3402 mL | |
| 10 mM | 0.4268 mL | 2.1340 mL | 4.2680 mL | 10.6701 mL | |
| 15 mM | 0.2845 mL | 1.4227 mL | 2.8454 mL | 7.1134 mL | |
| 20 mM | 0.2134 mL | 1.0670 mL | 2.1340 mL | 5.3350 mL | |
| 25 mM | 0.1707 mL | 0.8536 mL | 1.7072 mL | 4.2680 mL | |
| 30 mM | 0.1423 mL | 0.7113 mL | 1.4227 mL | 3.5567 mL | |
| 40 mM | 0.1067 mL | 0.5335 mL | 1.0670 mL | 2.6675 mL | |
| 50 mM | 0.0854 mL | 0.4268 mL | 0.8536 mL | 2.1340 mL | |
| 60 mM | 0.0711 mL | 0.3557 mL | 0.7113 mL | 1.7783 mL | |
| 80 mM | 0.0534 mL | 0.2668 mL | 0.5335 mL | 1.3338 mL | |
| 100 mM | 0.0427 mL | 0.2134 mL | 0.4268 mL | 1.0670 mL |
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