AG1024

• CAT Number: I004477
• CAS Number: 65678-07-1
• Molecular Formula: C14H13BrN2O
• Molecular Weight: 305.2
• Purity: ≥95%
• Target: IGF1R
• Solubility: DMSO 61 mg/ml; Water <1 mg/ml
• Storage: 3 years -20C powder
• IC50: 7 uM (IGF-1R autophosphorylation); 57 uM (IR)
• 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
• InChIKey: ABBADGFSRBWENF-UHFFFAOYSA-N
• SMILES: BrC1=C(O)C(C(C)(C)C)=CC(/C=C(C#N)/C#N)=C1

AG1024 (CAT: I004477), also known as Tyrphostin AG1024 or NVP-AG1024, is a small molecule inhibitor that specifically targets and inhibits the insulin-like growth factor 1 receptor (IGF-1R). It acts by binding to the ATP-binding site of IGF-1R, preventing its activation and subsequent signaling pathways. By inhibiting IGF-1R, AG1024 can impede the growth and survival of cancer cells that rely on IGF-1R signaling for their proliferation. AG1024 has been investigated for its potential in cancer therapy, particularly in cancers driven by aberrant IGF-1R signaling, and it shows promise as a targeted therapeutic agent for certain types of cancer.

Reference

1:Effects of insulin-like growth factor 1 receptor and its inhibitor AG1024 on the progress of lung cancer. Wei YH, Tang HX, Liao YD, Fu SL, Xu LQ, Chen G, Zhang C, Ju S, Liu ZG, You LK, Yu L, Zhou S.J Huazhong Univ Sci Technolog Med Sci. 2015 Dec;35(6):834-41. doi: 10.1007/s11596-015-1515-1. Epub 2015 Dec 16. PMID: 26670433
2:Studying the enhancement of programmed cell death by combined AG1024 and paclitaxel in a model of chronic myelogenous leukemia. Cheng HY, Ko FH.Life Sci. 2014 May 2;102(2):118-26. doi: 10.1016/j.lfs.2014.03.014. Epub 2014 Mar 20. PMID: 24657894
3:Enhancement of AG1024-induced H9c2 cardiomyoblast cell apoptosis via the interaction of IGF2R with Galpha proteins and its downstream PKA and PLC-beta modulators by IGF-II. Chu CH, Huang CY, Lu MC, Lin JA, Tsai FJ, Tsai CH, Chu CY, Kuo WH, Chen LM, Chen LY.Chin J Physiol. 2009 Feb 28;52(1):31-7. PMID: 19764351
4:The effect of tyrosine kinase inhibitors, tyrphostins: AG1024 and SU1498, on autocrine growth of prostate cancer cells (DU145). Kisielewska J, Ligeza J, Klein A.Folia Histochem Cytobiol. 2008;46(2):185-91. doi: 10.2478/v10042-008-0028-1. PMID: 18519236 Free Article
5:Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-Abl expressing cells and decreases AKT phosphorylation. Deutsch E, Maggiorella L, Wen B, Bonnet ML, Khanfir K, Frascogna V, Turhan AG, Bourhis J.Br J Cancer. 2004 Nov 1;91(9):1735-41. PMID: 15494718 Free PMC Article
6:The tyrphostin AG1024 accelerates the degradation of phosphorylated forms of retinoblastoma protein (pRb) and restores pRb tumor suppressive function in melanoma cells. von Willebrand M, Zacksenhaus E, Cheng E, Glazer P, Halaban R.Cancer Res. 2003 Mar 15;63(6):1420-9. PMID: 12649208 Free Article