SU 11274

• CAT Number: I004481
• CAS Number: 658084-23-2
• Molecular Formula: C₂₈H₃₀ClN₅O₄S
• Molecular Weight: 568.09
• Purity: ≥95%
• Target: c-MET
• Solubility: DMSO ≥90mg/mL Water <1.2mg/mL Ethanol ≥1.8mg/mL
• Storage: 3 years -20C powder
• IC50: 10 nM [1]
• InChI: InChI=1S/C28H30ClN5O4S/c1-17-25(30-18(2)26(17)28(36)34-12-10-32(3)11-13-34)16-23-22-15-21(8-9-24(22)31-27(23)35)39(37,38)33(4)20-7-5-6-19(29)14-20/h5-9,14-16,30H,10-13H2,1-4H3,(H,31,35)/b23-16-
• InChIKey: FPYJSJDOHRDAMT-KQWNVCNZSA-N
• SMILES: CC1=C(NC(=C1C(=O)N2CCN(CC2)C)C)C=C3C4=C(C=CC(=C4)S(=O)(=O)N(C)C5=CC(=CC=C5)Cl)NC3=O

SU 11274(CAT:I004481)is a selective inhibitor of the MET receptor tyrosine kinase. It acts by binding to the ATP-binding site of MET and inhibiting its kinase activity. MET is involved in various cellular processes, including cell proliferation, survival, migration, and invasion. Aberrant activation of the MET pathway has been implicated in the development and progression of several cancers, including lung, gastric, and liver cancers. SU 11274 has shown promising antitumor activity by blocking MET signaling and inhibiting tumor growth in preclinical studies. It is being investigated as a potential therapeutic agent for the treatment of MET-driven cancers.

Reference

1:Tyrosine kinase inhibitor SU11274 increased tumorigenicity and enriched for melanoma-initiating cells by bioenergetic modulation. Kucerova L, Demkova L, Skolekova S, Bohovic R, Matuskova M.BMC Cancer. 2016 May 12;16:308. doi: 10.1186/s12885-016-2341-y. PMID: 27175734 Free PMC Article2:SU11274 suppresses proliferation and motility of pancreatic cancer cells. Tomizawa M, Shinozaki F, Motoyoshi Y, Sugiyama T, Yamamoto S, Ishige N.Oncol Lett. 2015 Sep;10(3):1468-1472. Epub 2015 Jul 2. PMID: 26622692 Free PMC Article3:Co-culture of hepatocellular carcinoma cells and human umbilical endothelial cells damaged by SU11274. Tomizawa M, Shinozaki F, Motoyoshi Y, Sugiyama T, Yamamoto S, Ishige N.Biomed Rep. 2014 Nov;2(6):799-803. Epub 2014 Sep 10. PMID: 25279148 Free PMC Article4:Effect of c-Met inhibitor SU11274 on human colon cancer cell growth. Gao SH, Liu C, Wei J, Feng Y.Chin Med J (Engl). 2013 Jul;126(14):2705-9. PMID: 23876900 5:Study of critical role of c-Met and its inhibitor SU11274 in colorectal carcinoma. Gao W, Bing X, Li M, Yang Z, Li Y, Chen H.Med Oncol. 2013 Jun;30(2):546. doi: 10.1007/s12032-013-0546-3. Epub 2013 Mar 28. PMID: 23536000 6:Synergistic effect of afatinib with su11274 in non-small cell lung cancer cells resistant to gefitinib or erlotinib. Chen G, Noor A, Kronenberger P, Teugels E, Umelo IA, De Grève J.PLoS One. 2013;8(3):e59708. doi: 10.1371/journal.pone.0059708. Epub 2013 Mar 18. PMID: 23527257 Free PMC Article7:c-Met inhibitor SU11274 enhances the response of the prostate cancer cell line DU145 to ionizing radiation. Yu H, Li X, Sun S, Gao X, Zhou D.Biochem Biophys Res Commun. 2012 Oct 26;427(3):659-65. doi: 10.1016/j.bbrc.2012.09.117. Epub 2012 Sep 28. PMID: 23026049 8:Activated O2(•−) and H2O2 mediated cell survival in SU11274-treated non-small-cell lung cancer A549 cells via c-Met-PI3K-Akt and c-Met-Grb2/SOS-Ras-p38 pathways. Liu Y, Shi QF, Ye YC, Tashiro S, Onodera S, Ikejima T.J Pharmacol Sci. 2012;119(2):150-9. Epub 2012 May 26. PMID: 22673163 Free Article9:Activation of ERK-p53 and ERK-mediated phosphorylation of Bcl-2 are involved in autophagic cell death induced by the c-Met inhibitor SU11274 in human lung cancer A549 cells. Liu Y, Yang Y, Ye YC, Shi QF, Chai K, Tashiro S, Onodera S, Ikejima T.J Pharmacol Sci. 2012;118(4):423-32. Epub 2012 Mar 29. PMID: 22466960 Free Article10:Inhibition of phosphorylated c-Met in rhabdomyosarcoma cell lines by a small molecule inhibitor SU11274. Hou J, Dong J, Sun L, Geng L, Wang J, Zheng J, Li Y, Bridge J, Hinrichs SH, Ding SJ.J Transl Med. 2011 May 16;9:64. doi: 10.1186/1479-5876-9-64. PMID: 21575221 Free PMC Article