SOR-C13 is a transient receptor potential vanilloid subtype 6 (TRPV6) polypeptide antagonist (IC50=14nM). SOR-C13 inhibits TRPV6 calcium channel-mediated Ca2+ influx to reduce calcium signaling and proliferation in tumor cells. SOR-C13 suppresses epithelial tumor growth in the ovary, breast, prostate and pancreas through TRPV6-targeted binding. SOR-C13 can be used in studies on TRPV6-overexpressing solid tumors and tumor-targeted delivery[1-4].
In vitro, 25-83.5μM SOR-C13 was applied to TRPV6-transfected HEK-293 cells for 600ms. SOR-C13 reduced TRPV6 current amplitude[5]. Caco-2 cells were pretreated with 10μM SOR-C13 for 30 minutes, then treated with 200μM lithocholic acid for 24 hours. SOR-C13 blocked lithocholic acid-induced inhibition of DSG2 protein expression and inhibited lithocholic acid-induced decrease in transepithelial electrical resistance TEER[6].
In vivo, NOD/SCID mice bearing SKOV-3 cell xenografts received intraperitoneal injections of 400-800mg/kg SOR-C13 daily for 12 days. SOR-C13 inhibited tumor growth[7].
References:[1] Fu S, Hirte H, Welch S, et al. First-in-human phase I study of SOR-C13, a TRPV6 calcium channel inhibitor, in patients with advanced solid tumors. Invest New Drugs. 2017 Jun;35(3):324-333.
[2] Pennington MW, Czerwinski A, Norton RS. Peptide therapeutics from venom: Current status and potential. Bioorg Med Chem. 2018;26(10):2738-2758.
[3] Bordon KCF, Cologna CT, Fornari-Baldo EC, et al. From Animal Poisons and Venoms to Medicines: Achievements, Challenges and Perspectives in Drug Discovery. Front Pharmacol. 2020 Jul 24;11:1132.
[4] Neuberger A, Sobolevsky AI. Molecular pharmacology of the onco-TRP channel TRPV6. Channels. 2023;17(1):2266669.
[5] Bowen CV, DeBay D, Ewart HS, et al. In Vivo Detection of Human TRPV6-Rich Tumors with Anti-Cancer Peptides Derived from Soricidin. PLoS ONE. 2013 Mar 15;8(3):e58866.
[6] Yan J, Wang Y, Tong B, et al. Disruption of the gut microbiota induces the LCA/TRPV6 signalling axis, impairing desmosome junctions in vitamin A-deficient rats. Food Res Int. 2025;222:117656.
[7] Xue H, Wang Y, MacCormack TJ, et al. Inhibition of Transient Receptor Potential Vanilloid 6 channel, elevated in human ovarian cancers, reduces tumour growth in a xenograft model. J Cancer. 2018;9(17):3196-3207.
















