OPB-51602

• CAT Number: I008474
• Purity: ≥95%
• Synonyms: OPB51602; OPB 51602; OPB51602.;NONE
• Target: STAT3 inhibitor
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4 °C for short term, or -20 °C for long term

OPB-51602 is a n orally bioavailable inhibitor of signal transducer and activator of transcription 3 (STAT3), with potential antineoplastic activity. STAT3 inhibitor OPB-51602 inhibits the phosphorylation and thus the activation of STAT3 protein, impeding STAT3 protein from translocating from the cytoplasm to the nucleus and thereby blocking STAT3/’s regulation of gene expression through direct binding to the promoters of responsive genes. STAT3 regulates the cellular functions that lead to the cancer phenotype, and constitutive activation of STAT3 is observed in a wide range of human cancers, inducing uncontrolled proliferation and neoplastic transformation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Reference

1:Phase I study of OPB-51602, an oral inhibitor of signal transducer and activator of transcription 3, in patients with relapsed/refractory hematological malignancies. Ogura M, Uchida T, Terui Y, Hayakawa F, Kobayashi Y, Taniwaki M, Takamatsu Y, Naoe T, Tobinai K, Munakata W, Yamauchi T, Kageyama A, Yuasa M, Motoyama M, Tsunoda T, Hatake K.Cancer Sci. 2015 Jul;106(7):896-901. doi: 10.1111/cas.12683. Epub 2015 May 25. PMID: 25912076 Free PMC Article2:Phase I and biomarker study of OPB-51602, a novel signal transducer and activator of transcription (STAT) 3 inhibitor, in patients with refractory solid malignancies. Wong AL, Soo RA, Tan DS, Lee SC, Lim JS, Marban PC, Kong LR, Lee YJ, Wang LZ, Thuya WL, Soong R, Yee MQ, Chin TM, Cordero MT, Asuncion BR, Pang B, Pervaiz S, Hirpara JL, Sinha A, Xu WW, Yuasa M, Tsunoda T, Motoyama M, Yamauchi T, Goh BC.Ann Oncol. 2015 May;26(5):998-1005. doi: 10.1093/annonc/mdv026. Epub 2015 Jan 21. PMID: 25609248