WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406233

CAS#: 65678-07-1

Description: AG-1024 is also called Tyrphostin, is a selective inhibitor of IGF-1R. AG-1024 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. Tyrphostin AG 1024 could be used as a potential therapeutic agent in combination with irradiation.

Chemical Structure

CAS# 65678-07-1

Theoretical Analysis

MedKoo Cat#: 406233
Name: AG-1024
CAS#: 65678-07-1
Chemical Formula: C14H13BrN2O
Exact Mass: 304.02
Molecular Weight: 305.170
Elemental Analysis: C, 55.10; H, 4.29; Br, 26.18; N, 9.18; O, 5.24

Price and Availability

Size Price Availability Quantity
5mg USD 240 2 Weeks
10mg USD 400 2 Weeks
50mg USD 800 2 Weeks
100mg USD 1250 2 Weeks
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Synonym: AG1024; AG-1024; AG 1024. Tyrphostin.

IUPAC/Chemical Name: 2-(3-bromo-5-tert-butyl-4-hydroxybenzylidene)malononitrile


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

SMILES Code: N#C/C(C#N)=C/C1=CC(C(C)(C)C)=C(O)C(Br)=C1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Product Data:
Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 305.169820000000000000000000000000 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Zhou W, Lou W, Chen J, Ding B, Chen B, Xie H, Zhou L, Zheng S, Jiang D. AG-1024 Sensitizes Sorafenib-Resistant Hepatocellular Carcinoma Cells to Sorafenib via Enhancing G1/S Arrest. Onco Targets Ther. 2021 Feb 15;14:1049-1059. doi: 10.2147/OTT.S289324. PMID: 33623392; PMCID: PMC7894871. 2: Wen B, Deutsch E, Marangoni E, Frascona V, Maggiorella L, Abdulkarim B, Chavaudra N, Bourhis J. Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells. Br J Cancer. 2001 Dec 14;85(12):2017-21. doi: 10.1054/bjoc.2001.2171. PMID: 11747348; PMCID: PMC2364012. 3: Zhou X, Chen N, Xu H, Zhou X, Wang J, Fang X, Zhang Y, Li Y, Yang J, Wang X. Regulation of Hippo-YAP signaling by insulin-like growth factor-1 receptor in the tumorigenesis of diffuse large B-cell lymphoma. J Hematol Oncol. 2020 Jun 16;13(1):77. doi: 10.1186/s13045-020-00906-1. PMID: 32546241; PMCID: PMC7298789. 4: Giuffrida ML, Caraci F, Pignataro B, Cataldo S, De Bona P, Bruno V, Molinaro G, Pappalardo G, Messina A, Palmigiano A, Garozzo D, Nicoletti F, Rizzarelli E, Copani A. Beta-amyloid monomers are neuroprotective. J Neurosci. 2009 Aug 26;29(34):10582-7. doi: 10.1523/JNEUROSCI.1736-09.2009. PMID: 19710311; PMCID: PMC6665714. 5: Liu J, Zhang Y, Liu M, Shi F, Cheng B. AG1024, an IGF-1 receptor inhibitor, ameliorates renal injury in rats with diabetic nephropathy via the SOCS/JAK2/STAT pathway. Open Med (Wars). 2023 Apr 6;18(1):20230683. doi: 10.1515/med-2023-0683. PMID: 37034500; PMCID: PMC10080708. 6: Tomita S, Inaba K, Sekimoto M. Tyrphostin AG1024 downregulates aryl hydrocarbon receptor (AhR) expression in an IGF1R and IR-independent manner. Toxicol Lett. 2022 May 1;360:62-70. doi: 10.1016/j.toxlet.2022.02.003. Epub 2022 Feb 8. PMID: 35149128. 7: Zhao W, Wu X, Xie H, Ke Y, Yung WH. Permissive role of insulin in the expression of long-term potentiation in the hippocampus of immature rats. Neurosignals. 2010;18(4):236-45. doi: 10.1159/000324040. Epub 2011 Feb 22. PMID: 21346324. 8: Arous C, Mizgier ML, Rickenbach K, Pinget M, Bouzakri K, Wehrle-Haller B. Integrin and autocrine IGF2 pathways control fasting insulin secretion in β-cells. J Biol Chem. 2020 Dec 4;295(49):16510-16528. doi: 10.1074/jbc.RA120.012957. Epub 2020 Sep 15. PMID: 32934005; PMCID: PMC7864053. 9: Song RX, Chen Y, Zhang Z, Bao Y, Yue W, Wang JP, Fan P, Santen RJ. Estrogen utilization of IGF-1-R and EGF-R to signal in breast cancer cells. J Steroid Biochem Mol Biol. 2010 Feb 28;118(4-5):219-30. doi: 10.1016/j.jsbmb.2009.09.018. Epub 2009 Oct 6. PMID: 19815064; PMCID: PMC2826506. 10: Olianas MC, Dedoni S, Onali P. Regulation of PI3K/Akt signaling by N-desmethylclozapine through activation of δ-opioid receptor. Eur J Pharmacol. 2011 Jun 25;660(2-3):341-50. doi: 10.1016/j.ejphar.2011.04.012. Epub 2011 Apr 19. PMID: 21515255. 11: Lee JH, Choi SI, Kim RK, Cho EW, Kim IG. Tescalcin/c-Src/IGF1Rβ-mediated STAT3 activation enhances cancer stemness and radioresistant properties through ALDH1. Sci Rep. 2018 Jul 16;8(1):10711. doi: 10.1038/s41598-018-29142-x. PMID: 30013043; PMCID: PMC6048049. 12: Swetha M, Ramaiah KVA. Insulin treatment promotes tyrosine phosphorylation of PKR and inhibits polyIC induced PKR threonine phosphorylation. Arch Biochem Biophys. 2015 Nov 1;585:98-108. doi: 10.1016/ Epub 2015 Aug 28. PMID: 26321373. 13: Kim DH, Lee HE, Kwon KJ, Park SJ, Heo H, Lee Y, Choi JW, Shin CY, Ryu JH. Early immature neuronal death initiates cerebral ischemia-induced neurogenesis in the dentate gyrus. Neuroscience. 2015 Jan 22;284:42-54. doi: 10.1016/j.neuroscience.2014.09.074. Epub 2014 Oct 6. PMID: 25301746. 14: Tang Q, Ma J, Sun J, Yang L, Yang F, Zhang W, Li R, Wang L, Wang Y, Wang H. Genistein and AG1024 synergistically increase the radiosensitivity of prostate cancer cells. Oncol Rep. 2018 Aug;40(2):579-588. doi: 10.3892/or.2018.6468. Epub 2018 May 30. PMID: 29901146; PMCID: PMC6072286. 15: Pan YH, Jiao L, Lin CY, Lu CH, Li L, Chen HY, Wang YB, He Y. Combined treatment with metformin and gefitinib overcomes primary resistance to EGFR-TKIs with EGFR mutation via targeting IGF-1R signaling pathway. Biologics. 2018 Aug 20;12:75-86. doi: 10.2147/BTT.S166867. PMID: 30154647; PMCID: PMC6108345. 16: He Y, Yuan X, Zhou G, Feng A. Activation of IGF-1/IGFBP-3 signaling by berberine improves intestinal mucosal barrier of rats with acute endotoxemia. Fitoterapia. 2018 Jan;124:200-205. doi: 10.1016/j.fitote.2017.11.012. Epub 2017 Nov 14. PMID: 29154866. 17: Ilatovskaya DV, Levchenko V, Brands MW, Pavlov TS, Staruschenko A. Cross- talk between insulin and IGF-1 receptors in the cortical collecting duct principal cells: implication for ENaC-mediated Na+ reabsorption. Am J Physiol Renal Physiol. 2015 Apr 1;308(7):F713-9. doi: 10.1152/ajprenal.00081.2014. Epub 2015 Jan 28. PMID: 25651558; PMCID: PMC4385890. 18: Yao WF, Liu JW, Sheng GL, Huang DS. Blockade of IGF-IR exerts anticancer effects in hepatocellular carcinoma. Mol Med Rep. 2011 Jul-Aug;4(4):719-22. doi: 10.3892/mmr.2011.486. Epub 2011 May 9. PMID: 21567089. 19: Ito S, Yanai M, Yamaguchi S, Couraud PO, Ohtsuki S. Regulation of Tight- Junction Integrity by Insulin in an In Vitro Model of Human Blood-Brain Barrier. J Pharm Sci. 2017 Sep;106(9):2599-2605. doi: 10.1016/j.xphs.2017.04.036. Epub 2017 Apr 26. PMID: 28456720. 20: He Y, Yuan X, Zuo H, Li X, Sun Y, Feng A. Berberine induces ZIP14 expression and modulates zinc redistribution to protect intestinal mucosal barrier during polymicrobial sepsis. Life Sci. 2019 Sep 15;233:116697. doi: 10.1016/j.lfs.2019.116697. Epub 2019 Jul 25. PMID: 31351968.