LCH-7749944（Cat No.:I007632）is a selective inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) tyrosine kinase, a receptor involved in cell growth, survival, and proliferation. By targeting IGF-1R, LCH-7749944 disrupts downstream signaling pathways such as PI3K/AKT and MAPK, which are critical for cancer cell survival and proliferation. It has been studied for its potential in treating various cancers, including those with abnormal IGF-1R signaling, such as breast, lung, and prostate cancers. LCH-7749944’s ability to inhibit IGF-1R makes it a valuable tool in oncology research for developing targeted cancer therapies.
| Catalog Number | I007632 |
| CAS Number | 796888-12-5 (LCH-7749944); 1049788-58-0 (LCH-7749944 HCl) |
| Synonyms | LCH7749944; LCH 7749944; LCH-7749944; GNF-PF-2356.;N2-(3-methoxyphenyl)-N4-((tetrahydrofuran-2-yl)methyl)quinazoline-2,4-diamine |
| Molecular Formula | C20H22N4O2 |
| Purity | ≥95% |
| Target | PAK4 inhibitor |
| Solubility | Soluble in DMSO, not in water |
| Storage | 0 - 4°C for short term , or -20°C for long term. |
| IUPAC Name | 2-N-(3-methoxyphenyl)-4-N-(oxolan-2-ylmethyl)quinazoline-2,4-diamine |
| InChI | InChI=1S/C20H22N4O2/c1-25-15-7-4-6-14(12-15)22-20-23-18-10-3-2-9-17(18)19(24-20)21-13-16-8-5-11-26-16/h2-4,6-7,9-10,12,16H,5,8,11,13H2,1H3,(H2,21,22,23,24) |
| InChIKey | FBWZAFQEOKNGQL-UHFFFAOYSA-N |
| SMILES | COC1=CC=CC(=C1)NC2=NC3=CC=CC=C3C(=N2)NCC4CCCO4 |
| Reference | 1:Cancer Lett. 2012 Apr 1;317(1):24-32. doi: 10.1016/j.canlet.2011.11.007. Epub 2011 Nov 13. LCH-7749944, a novel and potent p21-activated kinase 4 inhibitor, suppresses proliferation and invasion in human gastric cancer cells.Zhang J,Wang J,Guo Q,Wang Y,Zhou Y,Peng H,Cheng M,Zhao D,Li F, PMID: 22085492 DOI: 10.1016/j.canlet.2011.11.007 </br><span>Abstract:</span> P21-activated kinase 4 (PAK4), a serine/threonine protein kinase, has involved in the regulation of cytoskeletal reorganization, cell proliferation, gene transcription, oncogenic transformation and cell invasion. Moreover, PAK4 overexpression, genetic amplification and mutations were detected in a variety of human tumors, which make it potential therapeutic target. In this paper we found that LCH-7749944, a novel and potent PAK4 inhibitor, effectively suppressed the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway. In addition, LCH-7749944 significantly inhibited the migration and invasion of human gastric cancer cells in conjunction with concomitant blockage of PAK4/LIMK1/cofilin and PAK4/MEK-1/ERK1/2/MMP2 pathways. Interestingly, LCH-7749944 also inhibited the formation of filopodia and induced cell elongation in SGC7901 cells. Importantly, LCH-7749944 caused successful inhibition of EGFR activity due to its inhibitory effect on PAK4. Taken together, these results provided novel insights into the development of PAK4 inhibitor and potential therapeutic strategies for gastric cancer.Copyright © 2011 Elsevier Ireland Ltd. All rights reserved. |
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