WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205566
CAS#: NONE
Description: OPB-31121 is an orally bioavailable inhibitor of signal transducer and activator of transcription 3 (STAT3), with potential antineoplastic activity. OPB-31121 inhibits the phosphorylation of STAT3, which prevents binding of STAT3 to DNA sequences on a variety of STAT3-responsive promoters and may result in the inhibition of STAT3-mediated transcription and, potentially, the inhibition of tumor cell proliferation. STAT3 is constitutively activated in a variety of cancers, contributing to the loss of cell growth control and neoplastic transformation.
MedKoo Cat#: 205566
Name: OPB-31121
CAS#: NONE
Chemical Formula:
Exact Mass:
Molecular Weight:
Elemental Analysis:
OPB-31121 is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.
Synonym: OPB31121; OPB-31121; OPB 31121;
IUPAC/Chemical Name: NONE
The following data is based on the product molecular weight 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.
| 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 |
1: Brambilla L, Genini D, Laurini E, Merulla J, Perez L, Fermeglia M, Carbone GM, Pricl S, Catapano CV. Hitting the right spot: Mechanism of action of OPB-31121, a novel and potent inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3). Mol Oncol. 2015 Jun;9(6):1194-206. doi: 10.1016/j.molonc.2015.02.012. Epub 2015 Mar 5. PubMed PMID: 25777967.
2: Oh DY, Lee SH, Han SW, Kim MJ, Kim TM, Kim TY, Heo DS, Yuasa M, Yanagihara Y, Bang YJ. Phase I study of OPB-31121, an Oral STAT3 Inhibitor, in Patients with Advanced Solid Tumors. Cancer Res Treat. 2015 Feb 26. doi: 10.4143/crt.2014.249. [Epub ahead of print] PubMed PMID: 25715763.
3: Okusaka T, Ueno H, Ikeda M, Mitsunaga S, Ozaka M, Ishii H, Yokosuka O, Ooka Y, Yoshimoto R, Yanagihara Y, Okita K. Phase 1 and pharmacological trial of OPB-31121, a signal transducer and activator of transcription-3 inhibitor, in patients with advanced hepatocellular carcinoma. Hepatol Res. 2015 Feb 11. doi: 10.1111/hepr.12504. [Epub ahead of print] PubMed PMID: 25676869.
4: Bendell JC, Hong DS, Burris HA 3rd, Naing A, Jones SF, Falchook G, Bricmont P, Elekes A, Rock EP, Kurzrock R. Phase 1, open-label, dose-escalation, and pharmacokinetic study of STAT3 inhibitor OPB-31121 in subjects with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Jul;74(1):125-30. doi: 10.1007/s00280-014-2480-2. Epub 2014 May 13. PubMed PMID: 24819685.
5: Hayakawa F, Sugimoto K, Harada Y, Hashimoto N, Ohi N, Kurahashi S, Naoe T. A novel STAT inhibitor, OPB-31121, has a significant antitumor effect on leukemia with STAT-addictive oncokinases. Blood Cancer J. 2013 Nov 29;3:e166. doi: 10.1038/bcj.2013.63. PubMed PMID: 24292418; PubMed Central PMCID: PMC3880446.
6: Kim MJ, Nam HJ, Kim HP, Han SW, Im SA, Kim TY, Oh DY, Bang YJ. OPB-31121, a novel small molecular inhibitor, disrupts the JAK2/STAT3 pathway and exhibits an antitumor activity in gastric cancer cells. Cancer Lett. 2013 Jul 10;335(1):145-52. doi: 10.1016/j.canlet.2013.02.010. Epub 2013 Feb 10. PubMed PMID: 23402820.
