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

AG 1295 

Cat. No.: HY-101957 Purity: 99.88%
Handling Instructions

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

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 86 In-stock
Estimated Time of Arrival: December 31
5 mg USD 78 In-stock
Estimated Time of Arrival: December 31
10 mg USD 133 In-stock
Estimated Time of Arrival: December 31
50 mg USD 400 In-stock
Estimated Time of Arrival: December 31
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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].

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].

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.

71897-07-9

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (266.75 mM; Need ultrasonic)

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
10 mM 0.4268 mL 2.1340 mL 4.2680 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.88 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.88 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.88 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AG 1295AG1295AG-1295PDGFRPlatelet-derived growth factor receptorRTKPDGF-receptorautophosphorylationInhibitorinhibitorinhibit

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