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Drug repositioning of regorafenib for renal cell carcinoma identifies <i>DDR2</i>‑associated sensitivity in ACHN models.


ABSTRACT: Renal cell carcinoma (RCC) is heterogeneous and frequently refractory to cytotoxic therapy. We investigated whether contexts with elevated DDR2-a collagenactivated receptor tyrosine kinase-are preferentially sensitive to regorafenib, a multikinase inhibitor with activity against DDR2. DDR2 mRNA was quantified by quantitative PCR in Caki1 (clear cell), ACHN (papillary), and Caki2 (papillary) relative to HK2. Shortterm viability was assessed by a tetrazolium (MTT) assay with fourparameter logistic fits to estimate the lowest observed effect concentration (LOEC) and halfmaximal inhibitory concentration (IC₅₀). In an ACHN xenograft model, mice were randomized to vehicle or regorafenib (10 mg/kg, intraperitoneally) every 3 days for 21 days. ACHN and Caki1 expressed higher DDR2 tha

SUBMITTER: Moon J 

PROVIDER: S-EPMC12723414 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature