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AG-1024 IGF-1R inhibitor

Name: AG-1024
Brand: Selleck Chemicals
SKU: S1234
Rating: 5 (27 reviews)

Cat.No.S1234

AG-1024 (Tyrphostin, AGS 200) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, is less potent to IR with IC50 of 57 μM and specifically distinguishes between InsR and IGF-1R (as compared to other tyrphostins).

Chemical Structure

Molecular Weight: 305.17

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Quality Control

Batch: S123401 DMSO]61 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.99%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.99

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2
Other IGF-1R Inhibitors	Linsitinib (OSI-906) BMS-536924 NVP-AEW541 BMS-754807 Picropodophyllin (AXL1717) GSK1904529A NVP-ADW742 NT157 PQ 401 MSDC-0160

Chemical Information, Storage & Stability

Molecular Weight	305.17	Formula	C₁₄H₁₃BrN₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	65678-07-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Tyrphostin, AGS 200			Smiles	CC(C)(C)C1=C(C(=CC(=C1)C=C(C#N)C#N)Br)O

Solubility

In vitro
Batch:

DMSO : 61 mg/mL (199.88 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (9.83mM)	Taking the 1 mL working solution as an example, add 50 μL 60 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	IGF-1R (NIH-3T3 fibroblasts ) 7 μM Insulin Receptor (NIH-3T3 fibroblasts ) 57 μM
In vitro	AG-1024 blocks the IGF-1 receptor and IR autophosphorylation with IC50 of 7 μM and 57 μM, respectively. This compound also inhibits the receptor tyrosine kinase activity towards exogenous substrates (TKA) with IC50 values of 18 μM and 80 μM, respectively. This chemical (10 μM) inhibits cell proliferation in a time-dependent manner, and induces apoptosis in MCF-7 cells at 48 hours by 20.1% and >40% when combined with irradiation (10 Gy), more potently than that of irradiation (10 Gy) alone by 11.8%, which is associated with a down-regulation of phospho-Akt1 and bcl-2, and up-regulation of Bax, p53 and p21. It significantly inhibits melanoma cell proliferation with an IC50 of <50 nM in the absence of serum, by blocking MAPK/ERK2 signaling, subsequently rapidly inducing pRb dephosphorylation and activation, and eventually the formation of growth suppressive pRb-E2F complexes. Treatment with this compound down-regulates the expression of Bcr-Abl and P-Akt, and up-regulates DNA-PKcs expression in UT7-9 and Ba/F3-p210 cells, leading to decreased clonogenic survival and proliferation. It also significantly inhibits the proliferation of cells resistant to the BCR-ABL inhibitor STI571, which correlates with a dose-dependent decrease in Bcr-Abl protein expression.
Kinase Assay	Inhibition of IGF-1- and insulin-stimulated cellular proliferation
Kinase Assay	NIH-3T3 cells overexpressing IGF-1 or insulin receptors are plated on 96-well plates (2,000-5,000 cells/well) and maintained overnight in complete medium. Cells are then changed to DMEM containing 1% FBS in the presence of 10 nM IGF-1 or insulin and various concentrations of AG-1024 for 120 hours. Medium is replaced every 48 hours. At the indicated periods of time, the medium is aspirated from the wells and 100 μL MTT is added to each well. The cells are then incubated for 4 hours at 37 °C and lysed by addition of 100 μL isoamylic alcohol and shaking for 20 minutes. The plate is then read in the ELISA reader at 570 and 690 nm. The IC50 value is calculated at the 120-hour time point.
In vivo	Administration of AG-1024 at a dose of 30 μg for 10 days significantly inhibits the tumour growth of Ba/F3-p210 xenograft in mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/9075698/ [2] https://pubmed.ncbi.nlm.nih.gov/11747348/ [3] https://pubmed.ncbi.nlm.nih.gov/12649208/ [4] https://pubmed.ncbi.nlm.nih.gov/15494718/

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