For research use only, not for therapeutic use.
GSK1904529A（Cat No.:I000378）is a potent and selective inhibitor of the insulin-like growth factor-1 receptor (IGF-1R), which plays a vital role in cancer cell proliferation, survival, and metastasis. By targeting IGF-1R, GSK1904529A disrupts signaling pathways that drive tumor growth and progression, making it a promising candidate for cancer therapy. Preclinical studies have shown its effectiveness in inhibiting the growth of various tumor types, particularly those with elevated IGF-1R activity. GSK1904529A is being explored for its potential to enhance chemotherapy and overcome drug resistance in certain cancers.
| Catalog Number | I000378 |
| CAS Number | 1089283-49-7 |
| Synonyms | N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonylpiperazin-1-yl)piperidin-1-yl]anilino]pyrimidin-4-yl]imidazo[1,2-a]pyridin-2-yl]-2-methoxybenzamide |
| Molecular Formula | C₄₄H₄₇F₂N₉O₅S |
| Purity | ≥95% |
| Target | IGF1R |
| Solubility | DMSO 125 mg/ml; Water <1 mg/ml |
| Storage | 3 years -20C powder |
| IC50 | 27/25 nM (IGF1R/IR) |
| IUPAC Name | N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonylpiperazin-1-yl)piperidin-1-yl]anilino]pyrimidin-4-yl]imidazo[1,2-a]pyridin-2-yl]-2-methoxybenzamide |
| InChI | InChI=1S/C44H47F2N9O5S/c1-5-28-26-35(38(60-3)27-36(28)53-19-15-30(16-20-53)52-21-23-54(24-22-52)61(4,57)58)49-44-47-17-14-34(48-44)42-40(50-39-11-6-7-18-55(39)42)29-12-13-37(59-2)31(25-29)43(56)51-41-32(45)9-8-10-33(41)46/h6-14,17-18,25-27,30H,5,15-16,19-24H2,1-4H3,(H,51,56)(H,47,48,49) |
| InChIKey | MOSKATHMXWSZTQ-UHFFFAOYSA-N |
| SMILES | CCC1=CC(=C(C=C1N2CCC(CC2)N3CCN(CC3)S(=O)(=O)C)OC)NC4=NC=CC(=N4)C5=C(N=C6N5C=CC=C6)C7=CC(=C(C=C7)OC)C(=O)NC8=C(C=CC=C8F)F |
| Reference | </br>1:GSK1904529A, a Potent IGF-IR Inhibitor, Reverses MRP1-Mediated Multidrug Resistance. Gupta P, Xie M, Narayanan S, Wang YJ, Wang XQ, Yuan T, Wang Z, Yang DH, Chen ZS.J Cell Biochem. 2017 Mar 7. doi: 10.1002/jcb.25975. [Epub ahead of print] PMID: 28266043 </br>2:GSK1904529A, an insulin-like growth factor-1 receptor inhibitor, inhibits glioma tumor growth, induces apoptosis and inhibits migration. Zhou Q, Zhang J, Cui Q, Li X, Gao G, Wang Y, Xu Y, Gao X.Mol Med Rep. 2015 Sep;12(3):3381-5. doi: 10.3892/mmr.2015.3869. Epub 2015 May 28. PMID: 26035416 Free PMC Article</br>3:Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase. Sabbatini P, Rowand JL, Groy A, Korenchuk S, Liu Q, Atkins C, Dumble M, Yang J, Anderson K, Wilson BJ, Emmitte KA, Rabindran SK, Kumar R.Clin Cancer Res. 2009 May 1;15(9):3058-67. doi: 10.1158/1078-0432.CCR-08-2530. Epub 2009 Apr 21. PMID: 19383820 Free Article |
