1. Protein Tyrosine Kinase/RTK
  2. PDGFR
  3. AG 1295

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.

For research use only. We do not sell to patients.

AG 1295 Chemical Structure

AG 1295 Chemical Structure

CAS No. : 71897-07-9

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

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Description

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[1][2][3][4].

IC50 & Target

PDGFR[1]

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.
Molecular Weight

234.30

Formula

C16H14N2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 6.67 mg/mL (28.47 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2680 mL 21.3402 mL 42.6803 mL
5 mM 0.8536 mL 4.2680 mL 8.5361 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.90%

References

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
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AG 1295 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
AG 1295
Cat. No.:
HY-101957
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