AG-1024

Selective IGF-1R inhibitor CAS# 65678-07-1

AG-1024

Catalog No. BCC1242----Order now to get a substantial discount!

Product Name & Size Price Stock
AG-1024: 5mg $69 In Stock
AG-1024: 10mg Please Inquire In Stock
AG-1024: 20mg Please Inquire Please Inquire
AG-1024: 50mg Please Inquire Please Inquire
AG-1024: 100mg Please Inquire Please Inquire
AG-1024: 200mg Please Inquire Please Inquire
AG-1024: 500mg Please Inquire Please Inquire
AG-1024: 1000mg Please Inquire Please Inquire
Related Products
  • BMS-536924

    Catalog No.:BCC1177
    CAS No.:468740-43-4
  • NVP-ADW742

    Catalog No.:BCC4553
    CAS No.:475488-23-4
  • NVP-AEW541

    Catalog No.:BCC1180
    CAS No.:475489-16-8
  • Linsitinib

    Catalog No.:BCC3697
    CAS No.:867160-71-2

Quality Control of AG-1024

Number of papers citing our products

Chemical structure

AG-1024

3D structure

Chemical Properties of AG-1024

Cas No. 65678-07-1 SDF Download SDF
PubChem ID 2044 Appearance Powder
Formula C14H13BrN2O M.Wt 305.17
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Tyrphostin AG 1024
Solubility DMSO : ≥ 50 mg/mL (163.84 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-[(3-bromo-5-tert-butyl-4-hydroxyphenyl)methylidene]propanedinitrile
SMILES CC(C)(C)C1=C(C(=CC(=C1)C=C(C#N)C#N)Br)O
Standard InChIKey ABBADGFSRBWENF-UHFFFAOYSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of AG-1024

DescriptionAG-1024 is a selective inhibitor of IGF-1R with IC50 value of 7 μM.
TargetsIGF-1R    
IC507 μM     

Protocol

Cell experiment: [1]

Cell lines

MCF-7

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reacting condition

10 nM, 5 days for cell proliferation inhibition 10 nM, 48 hours for apoptosis induction

Applications

The Tyrphostin AG-1024 induced a marked decrease of cell proliferation in a time-dependent manner. It also potently induced cell apoptosis with a 20.1 % of apoptotic cells.

Animal experiment : [2]

Animal models

Female nude mice implanted with Ba/F3-p210 cells

Dosage form

Intraperitoneal injection, 30 μg in100 μl, once per day for 10 days

Application

After injection with Ba/F3-p210 cells (Bcr-Abl expressing cells), nude mice were injected after 6 days with PBS 0.1 ml (control) or Tyrphostin AG1024 30 μg/100 μl (1 μl of 980 μM). The growth of the Ba/F3-p210 xenografts was significantly delayed when mice were treated with Tyrphostin AG1024.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Wen B, Deutsch E, Marangoni E, et al. Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells. British journal of cancer, 2001, 85(12): 2017.

[2] Deutsch E, Maggiorella L, Wen B, et al. Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-Abl expressing cells and decreases AKT phosphorylation. British journal of cancer, 2004, 91(9): 1735-1741.

AG-1024 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

AG-1024 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of AG-1024

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.2769 mL 16.3843 mL 32.7686 mL 65.5372 mL 81.9216 mL
5 mM 0.6554 mL 3.2769 mL 6.5537 mL 13.1074 mL 16.3843 mL
10 mM 0.3277 mL 1.6384 mL 3.2769 mL 6.5537 mL 8.1922 mL
50 mM 0.0655 mL 0.3277 mL 0.6554 mL 1.3107 mL 1.6384 mL
100 mM 0.0328 mL 0.1638 mL 0.3277 mL 0.6554 mL 0.8192 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on AG-1024

AG1024 is an inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) that specifically inhibits autophosphorylation of IGF-1R and IR with IC50 values of 7μM and 57 μm, respectively [1].

AG1024 has shown to inhibit IGF-1- and insulin-stimulated cellular proliferation in NIH-3T3 mouse fibroblast cells with IC50 values of 0.4μM and 0.1μM, respectively. Additionally, AG1024 shows to block tyrosine kinase activity towards exogenous substrates (TKA) with IC50 values of 18μM and 80μM [1].

AG1024 has been reported to block receptor tyrosine kinase activity, resulting in abolishment of MAPK and Akt pathways and inhibition of cell growth. Moreover, studies showed that AG1024 concentration-dependently inhibited E2 stimulation in MCF-7:PF cells [2].

References:
[1] Párrizas M1, Gazit A, Levitzki A, Wertheimer E, LeRoith D. Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins. Endocrinology. 1997 Apr;138(4):1427-33.
[2] Fan P1, Agboke FA1, McDaniel RE1, Sweeney EE1, Zou X1, Creswell K1, Jordan VC2.Inhibition of c-Src blocks oestrogen-induced apoptosis and restores oestrogen-stimulated growth in long-term oestrogen-deprived breast cancer cells. Eur J Cancer. 2014 Jan; 50(2):457-68.

Featured Products
New Products
 

References on AG-1024

Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells.[Pubmed:11747348]

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

Insulin-like growth factor-1 (IGF-1) plays an important growth-promoting effect by activating the PI3K/Akt signalling pathway, inhibiting apoptotic pathways and mediating mitogenic actions. Tyrphostin AG 1024, one selective inhibitor of IGF-1R, was used to evaluate effects on proliferation, radiosensitivity, and radiation-induced cell apoptosis in a human breast cancer cell line MCF-7. Exposure to Tyrphostin AG 1024 inhibited proliferation and induced apoptosis in a time-dependent manner, and the degree of growth inhibition for IC20 plus irradiation (4 Gy) was up to 50% compared to the control. Examination of Tyrphostin AG 1024 effects on radiation response demonstrated a marked enhancement in radiosensitivity and amplification of radiation-induced apoptosis. Western blot analysis indicated that Tyrphostin AG 1024-induced apoptosis was associated with a downregulation of expression of phospho-Akt1, increased expression of Bax, p53 and p21, and a decreased expression of bcl-2 expression, especially when combined with irradiation. To our knowledge, this is the first report showing that an IGF-1 inhibitor was able to markedly increase the response of tumour cells to ionizing radiation. These results suggest that Tyrphostin AG 1024 could be used as a potential therapeutic agent in combination with irradiation.

Description

AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of insulin receptor (IR; IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity.

Keywords:

AG-1024,65678-07-1,Tyrphostin AG 1024,Natural Products,IGF1R, buy AG-1024 , AG-1024 supplier , purchase AG-1024 , AG-1024 cost , AG-1024 manufacturer , order AG-1024 , high purity AG-1024

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: