Tyrphostin AG 1296

Alias: AG 1296; AG1296; AG-1296; tyrphostin AG1296

Cat No.:V0574 Purity: ≥98%

COA Product Data Instructions for use SDS

Tyrphostin AG 1296 (AG-1296) is a novel, potent, selective and ATP-competitive inhibitor of PDGFR with potential antitumor activity.

Tyrphostin AG 1296 Chemical Structure CAS No.: 146535-11-7
Product category: PDGFR

This product is for research use only, not for human use. We do not sell to patients.

Size	Price	Stock	Qty
1mg
5mg
10mg
25mg
50mg
100mg
250mg
Other Sizes

ADD TO CART CHECKOUT BULK INQUIRY

1-708-310-1919 sales@invivochem.com

Official Supplier of:

Business Relationship with 5000+ Clients Globally
Major Universities, Research Institutions, Biotech & Pharma
Citations by Top Journals: Nature, Cell, Science, etc.

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators

Product Description

Tyrphostin AG 1296 (AG-1296) is a novel, potent, selective and ATP-competitive inhibitor of PDGFR with potential antitumor activity. It exhibits no activity against EGFR and inhibits PDGFR with an IC50 of 0.3-0.5 μM. Tyrphostin AG 1296 functions by binding to PDGFR and causing the ATP-binding site to undergo a conformational change. It effectively prevents the ligand-induced autophosphorylation of the PDGF receptor in Swiss 3T3 cell membranes in an in vitro experiment. Up to 100μM of tyrphostin AG 1296 does not interfere with the EGF receptor. Tyrphostin AG 1296 likewise prevents PDGF-induced mitogenesis, but not insulin or EGF-induced mitogenesis. With an IC50 mean of 1.5μM, it reversibly inhibits PDGF-induced DNA synthesis.

Biological Activity I Assay Protocols (From Reference)

Targets

PDGFR (IC50 = 0.3 μM-0.5 μM); c-Kit (IC50 = 1.8 μM); FGFR (IC50 = 12.3 μM)

ln Vitro

AG 1296 selectively inhibits the PDGF receptor kinase and PDGF-dependent DNA synthesis in porcine aorta endothellal cells and Swiss 3T3 cells, respectively, at 50% inhibitory concentrations below 5 and 1μM. In Swiss 3T3 cells, AG1296 inhibits FGFR and c-Kit with IC50 values of 12.3 μM and 1.8 μM, respectively. While autophosphorylation of the VEGFR KDR and VEGF-induced DNA synthesis in porcine aortic endothelial cells are unaffected by AG1296, it has a strong inhibitory effect on human PDGF-α and -β receptor signaling. NIH 3T3 cells transfected with sis have their transformed phenotype reversed by treatment with AG1296; src-transformed NIH 3T3 cells remain unaffected.[1] AG1296 is an inhibitor of ATP competition. AG1296 prevents PDGF receptor autophosphorylation while interfering neither with PDGF binding nor PDGF receptor dimerization. Consequently, AG1296 is a specific inhibitor of the receptor tyrosine kinase's catalytic activity.[2]

ln Vivo

Enzyme Assay

Confluent cultures of Swiss 3T3 cells are used to prepare membranes, as explained. A 45μl volume containing 10μg of membrane protein per assay, 50 mM Hepes (pH 7.5), 2μg/mL PDGF, or both, and 3 mM MnCl₂ is added. The mixture is then incubated for 20 minutes on ice. This allows for the measurement of receptor autophosphorylation. Tyrphostins are added 15 minutes before the growth factors are added, in a volume of 0.5 μl (in DMSO; final concentration, 0.5%), to test their effects. The addition of [γ-³²P]ATP starts the phosphorylation process, which is stopped after two minutes by adding 10μL of a solution that contains 0.6 SDS, 30%β-mercatoethanol, 40% glycerol, and 0.5 mg/mL bromophenol blue. The gels undergo autoradiographic analysis after being dried, stained, and processed.

Cell Assay

In 24-well plates, 5000 cells per well are seeded with DMEM/10% FCS. The medium is switched to DMEM/2% FcS the following day, either with or without growth factors, and tyrphostins are added as needed. The cells are counted in a hemocytometer three days later.

Animal Protocol

Nud/nud mice are injected with A375R cells
40, 80 mg/kg
I.p. daily for two weeks

References

[1]. Cancer Res . 1994 Dec 1;54(23):6106-14.

[4]. Biochemistry . 1997 May 27;36(21):6260-9.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C16H14N2O2

Molecular Weight

266.29

Exact Mass

266.11

Elemental Analysis

C, 72.16; H, 5.30; N, 10.52; O, 12.02

CAS #

146535-11-7

Related CAS #

146535-11-7

Appearance

Solid powder

SMILES

COC1=C(C=C2C(=C1)N=CC(=N2)C3=CC=CC=C3)OC

InChi Key

QNOXYUNHIGOWNY-UHFFFAOYSA-N

InChi Code

InChI=1S/C16H14N2O2/c1-19-15-8-12-13(9-16(15)20-2)18-14(10-17-12)11-6-4-3-5-7-11/h3-10H,1-2H3

Chemical Name

6,7-dimethoxy-2-phenylquinoxaline

Synonyms

AG 1296; AG1296; AG-1296; tyrphostin AG1296

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: ~6 mg/mL (~22.5 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Solubility (In Vivo)

Chemical Name:2-Phenyl-6,7-dimethoxyquinoxaline ; 6,7-Dimethoxy-2-phenylquinoxaline

InChi Key:QNOXYUNHIGOWNY-UHFFFAOYSA-N

InChi Code:InChI=1S/C16H14N2O2/c1-19-15-8-12-13(9-16(15)20-2)18-14(10-17-12)11-6-4-3-5-7-11/h3-10H,1-2H3

SMILES Code:COC1=C(OC)C=C2N=CC(C3=CC=CC=C3)=NC2=C1

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.7553 mL	18.7765 mL	37.5530 mL
	5 mM	0.7511 mL	3.7553 mL	7.5106 mL
	10 mM	0.3755 mL	1.8777 mL	3.7553 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculate Reset

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate Reset

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

Calculate Reset

Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.