AG-1024 (Tyrphostin; Tyrphostin AG1024)

Alias: Tyrphostin; AG-1024; AG 1024; AG1024; Tyrphostin AG1024; Tyrphostin AG-1024
Cat No.:V0626 Purity: ≥98%
AG-1024 (also called Tyrphostin or Tyrphostin AG1024) is a potent and selective inhibitor of IGF-1R (insulin-like growth factor-1) with potential antitumor activity.
AG-1024 (Tyrphostin; Tyrphostin AG1024) Chemical Structure CAS No.: 65678-07-1
Product category: IFG-1R
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
Other Sizes
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text

 

  • 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
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

AG-1024 (also called Tyrphostin or Tyrphostin AG1024) is a potent and selective inhibitor of IGF-1R (insulin-like growth factor-1) with potential antitumor activity. It has an IC50 of 7 μM, which selectively inhibits IGF-1R autophosphorylation, and an IC50 of 57 μM, which is less potent against Insulin receptor-IR. In a mouse model using a Ba/F3-p210 xenograft, AG-1024 demonstrates a notable antitumor efficacy.

Biological Activity I Assay Protocols (From Reference)
Targets
IGF1R (IC50 = 7 μM); IR (IC50 = 57 μM)
ln Vitro

AG-1024 has an IC50 of 7 μM for the IGF-1 receptor and 57 μM for IR autophosphorylation. With IC50 values of 18 μM and 80 μM, respectively, AG-1024 also inhibits the receptor tyrosine kinase activity towards exogenous substrates (TKA).[1] Inducing apoptosis in MCF-7 cells at 48 hours, AG-1024 (10 μM) inhibits cell proliferation in a time-dependent manner and increases the potency of irradiation (10 Gy) by 11.8% when combined with it. This is linked to the up-regulation of Bax, p53, and p21 and the down-regulation of phospho-Akt1 and bcl-2.[2] AG-1024 rapidly induces pRb dephosphorylation and activation, which in turn leads to the formation of growth suppressive pRb-E2F complexes, and it also significantly inhibits melanoma cell proliferation with an IC50 of less than 50 nM in the absence of serum by blocking MAPK/ERK2 signaling.[3] In UT7-9 and Ba/F3-p210 cells, AG-1024 treatment upregulates DNA-PKcs expression and downregulates Bcr-Abl and P-Akt expression, which reduces clonogenic survival and proliferation. Along with a dose-dependent reduction in Bcr-Abl protein expression, AG-1024 also dramatically inhibits the growth of cells resistant to the BCR-ABL inhibitor STI571.[4]

ln Vivo
The tumor growth of the Ba/F3-p210 xenograft in mice is significantly inhibited by administering 30 μg of AG-1024 for ten days.[4]
Enzyme Assay
On 96-well plates (2,000–5,000 cells/well), NIH-3T3 cells overexpressing insulin receptors or IGF-1 are cultured and kept overnight in full medium. The cells are subsequently switched to 1% FBS-containing DMEM for 120 hours along with different concentrations of AG-1024 and 10 nM insulin or IGF-1. Every 48 hours, the medium is changed. Each well receives 100 μL of MTT after the medium has been aspirated out at the designated intervals. After incubating the cells for four hours at 37 °C, 100 μL of isoamylic alcohol is added, and the cells are shaken for twenty minutes to lyse them. The plate is then read between 570 and 690 nm in the ELISA reader. At the 120-hour time point, the IC50 value is computed.
Cell Assay
AG-1024 is applied to cells for 24, 48, or 72 hours. Trypan blue dye exclusion is used to harvest and count cells in order to determine the proliferation. By dual staining MCF-7 with propidium iodide and fluoresceine anti-digoxigenin, apoptosis is assessed. In summary, fixed cells are stored in a dark environment after being briefly washed with PBS, suspended in TdT buffer containing TdT enzyme and Dig-dUTP for 60 minutes, and suspended in FITC blocking solution containing anti-Dig-Fluorescein for 30 minutes at room temperature. Following a 30-minute resuspension in a propidium iodide/RNase A solution and a buffer rinse, the cells are flow-cytometrically examined. To evaluate phospho-Akt1, Bax, p53, bcl-2, and p21, lysed cells are subjected to western blot analysis.
Animal Protocol
Female nude mice implanted subcutaneously with Ba/F3-p210 cells
30 μg/day
Injected i.p
References

[1]. Endocrinology . 1997 Apr;138(4):1427-33.

[2]. Br J Cancer . 2001 Dec 14;85(12):2017-21.

[3]. Cancer Res . 2003 Mar 15;63(6):1420-9.

[4]. Br J Cancer . 2004 Nov 1;91(9):1735-41.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C14H13BRN2O
Molecular Weight
305.17
Exact Mass
304.02
Elemental Analysis
C, 55.10; H, 4.29; Br, 26.18; N, 9.18; O, 5.24
CAS #
65678-07-1
Appearance
Solid powder
SMILES
CC(C)(C)C1=C(C(=CC(=C1)C=C(C#N)C#N)Br)O
InChi Key
ABBADGFSRBWENF-UHFFFAOYSA-N
InChi Code
InChI=1S/C14H13BrN2O/c1-14(2,3)11-5-9(4-10(7-16)8-17)6-12(15)13(11)18/h4-6,18H,1-3H3
Chemical Name
2-[(3-bromo-5-tert-butyl-4-hydroxyphenyl)methylidene]propanedinitrile
Synonyms
Tyrphostin; AG-1024; AG 1024; AG1024; Tyrphostin AG1024; Tyrphostin AG-1024
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: ~61 mg/mL (~199.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.2769 mL 16.3843 mL 32.7686 mL
5 mM 0.6554 mL 3.2769 mL 6.5537 mL
10 mM 0.3277 mL 1.6384 mL 3.2769 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

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
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.

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
g/mol

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.
/

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)
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.)
+
+
+

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.

(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.

Biological Data
  • AG-1024

    Dephosphorylation of pocket proteins in response to AG1024. Cancer Res. 2003 Mar 15;63(6):1420-9.
  • AG-1024

    pRb turnover in melanoma cells and normal melanocytes. Cancer Res. 2003 Mar 15;63(6):1420-9.

  • AG-1024

    pRb turnover in melanoma cells and normal melanocytes. Cancer Res. 2003 Mar 15;63(6):1420-9.

Contact Us