Art. -Nr.: HY-101957

AG 1295

4 Cited Publications

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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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Reinheit: 99.86%
CAS. Nr.: 71897-07-9
Formel: C₁₆H₁₄N₂
Molecular Weight:234.30

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AG 1295 Chemical Structure

CAS. Nr.: 71897-07-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

PDGFR^[1]

Alle PDGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
EOL1	IC₅₀	1.1 μM Compound: 1a	Inhibition of endogenous FLT3 in EOL1 cells Inhibition of endogenous FLT3 in EOL1 cells	[PMID: 16722630]
EOL1	IC₅₀	1.1 μM Compound: AG-1295	Inhibition of endogenous FLT3 autophosphorylation in EOL1 cells Inhibition of endogenous FLT3 autophosphorylation in EOL1 cells	[PMID: 17210255]
MV4-11	IC₅₀	2.2 μM Compound: AG1295	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	[PMID: 32659083]
NIH3T3	IC₅₀	0 μM Compound: AG-1295	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	[PMID: 11855980]
NIH3T3	IC₅₀	0.4 μM Compound: 25	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	[PMID: 8667360]
SF-539	IC₅₀	6.2 μM Compound: 22, AG-1295	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	[PMID: 22370340]
SF-539	IC₅₀	6.2 μM Compound: 28	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	[PMID: 23375090]
U-251	IC₅₀	6.2 μM Compound: 18, AG-1295	Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA	[PMID: 19748785]

In Vitro

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.

Cell Viability Assay^[2]

Cell Line:

Rabbit conjunctival fibroblasts cells
Concentration:

1 μM, 10 μM, 100 μM
Incubation Time:

3 days
Result:

Inhibited rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB.

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 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.

Animal Model:

Sprague-Dawley rats (240-270 g)^[4]
Dosage:

12 mg/kg
Administration:

Intraperitoneal injection; daily; for 14 or 21 days
Result:

Attenuated interstitial fibrosis in rat kidney after unilateral obstruction.

Chemical Information

CAS. Nr. 71897-07-9
Appearance Solid
Molecular Weight 234.30
Formel C₁₆H₁₄N₂
Color Light yellow to yellow
SMILES

CC1=C(C)C=C2N=CC(C3=CC=CC=C3)=NC2=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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
MedComm-Oncology

2023 Oct 17.
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

Cd248a regulates pericyte development and viability in zebrafish. [Abstract]

2025 Mar 17;8(1):451. PMID: 40097701

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.2680 mL

21.3402 mL

42.6803 mL

5 mM

0.8536 mL

4.2680 mL

8.5361 mL

10 mM

0.4268 mL

2.1340 mL

4.2680 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

AG 1295

4 Cited Publications

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AG 1295

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Reprogramming Compound Library

Anti-Cardiovascular Disease Compound Library

Angiogenesis-Related Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Human Metabolite Library

Anti-Pulmonary Fibrosis Compound Library

Coagulation and Anti-coagulation Compound Library

Publications Citing Use of MedChemExpress (MCE) AG 1295

Alle PDGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AG 1295

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Reprogramming Compound Library

Anti-Cardiovascular Disease Compound Library

Angiogenesis-Related Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Human Metabolite Library

Anti-Pulmonary Fibrosis Compound Library

Coagulation and Anti-coagulation Compound Library

Publications Citing Use of MedChemExpress (MCE) AG 1295

Alle PDGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AG 1295 Related Classifications

HY-101957 Related Classifications