Description:
PMD-026 is a first-in-class, orally bioavailable, selective p90 ribosomal S6 kinase (RSK) inhibitor with potent anticancer activity, particularly against triple-negative breast cancer (TNBC). In biochemical assays, PMD-026 inhibits RSK1–4 with IC50 values of 0.7–2 nM and shows good selectivity in kinome-wide profiling. In TNBC cell lines, PMD-026 suppresses anchorage-independent growth with IC50 values of 0.2–6.2 µM and anchorage-dependent proliferation with IC50 values of 1.8–8.4 µM, while inducing apoptosis and reducing phosphorylation of the downstream biomarker YB-1. In vivo, PMD-026 produced 72% tumor growth inhibition in MDA-MB-231 xenografts and 73% tumor regression in MDA-MB-468 xenografts. PMD-026 also demonstrated synergistic antitumor activity with paclitaxel, doxorubicin, fulvestrant, and enzalutamide in preclinical models, supporting its potential applications in RSK-targeted cancer research, TNBC, hormone-resistant breast cancer, prostate cancer, melanoma, and hematologic malignancies.
Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance,
we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one
month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at
least 1 hour.