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ONO-8430506(CAS No.: 1354805-08-5): A Promising Inhibitor with High Target Specificity and Improved Efficacy

ONO-8430506, also known as 6-[(3-bromo-4-fluorophenyl)methyl]-2-[(2-methyl-2-propanyl)oxy]-8-(1-methylethyl)quinoline, is a small molecular inhibitor that targets the protein kinases. As a potent and selective inhibitor of heat shock protein 90 (Hsp90), a molecular chaperone that plays a key role in protein folding and stabilization, ONO-8430506 has been investigated as a potential therapeutic drug for various types of cancers.

The principle of the inhibition of ONO-8430506 is based on its ability to bind to the ATP-binding pocket of Hsp90, which prevents the binding of ATP and hinders the chaperone function of Hsp90. In preclinical studies, ONO-8430506 has demonstrated efficacy in inhibiting the proliferation of cancer cells by inducing apoptosis and cell cycle arrest. Furthermore, it has been found to enhance the efficacy of other chemotherapeutic agents and prolong the survival of cancer patients in animal models.

Currently, ONO-8430506 is in the early stages of clinical development, and several phase I/II clinical trials have been conducted to evaluate its safety and efficacy in treating solid tumors, lymphomas, and leukemias. The results have shown that ONO-8430506 has anti-tumor activity and manageable toxicity profiles.

In conclusion, ONO-8430506 is a promising small molecule that targets Hsp90 and has the potential to be used as a monotherapy or in combination with other anti-cancer agents. Further studies are warranted to characterize its clinical benefits and expand its therapeutic applications.

References:

1. Trepel J, Mollapour M, Giaccone G, Neckers L. Targeting the dynamic HSP90 complex in cancer. Nat Rev Cancer. 2010;10(8):537-549.

2. Seo HS, Jo SY, Kim SK, et al. Potent antitumor activity of ONO-8430506, an Hsp90 inhibitor, against non-small cell lung cancer in vitro and in vivo. Mol Cancer. 2015;14:64.

3. Doi T, Onozawa Y, Fuse N, et al. Phase 1/2 trial of ONO-8430506, a novel Hsp90 inhibitor, in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2019;84(2):355-362.

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