RK-287107 (100 and 300 mg/kg; i.p. administration; once per day; 5-days on/ 2-days off schedule for 2 weeks) inhibits tumor growth in a mouse xenograft model[1]. Animal Model: 6-week-old female NOD.CB17-Prkdcscid/J mice with colorectal cancer COLO-320DM[1] Dosage: 100 and 300 mg/kg Administration: Administration i.p.; once per day; 5-days on/ 2-days off schedule for 2 weeks Result: 100 and 300 mg/kg resulted in 32.9% and 44.2% TGI, respectively.
In Vitro
RK-87107 (0.01-10 μM; 12 hours) shows an antiproliferative effect on colorectal cancer cells harboring short adenomatous polyposis coli (APC) mutations. The 50% growth inhibition (GI50) value of RK-287107 on COLO-320DM cells is 0.449 μM[1]. RK-287107 (0.03-10 μM; 16 hours) causes accumulation of tankyrase and Axin1/2[1]. RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells[1]. Cell Proliferation Assay[1] Cell Line: Colorectal cancer COLO-320DM, SW403, RKO, HCC2998, HCT-116, and DLD-1 cells Concentration: 0.01, 0.1, 1, 10 μM Incubation Time: 12 hours Result: Inhibited the growth of APC-mutated (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells. The GI50 value of RK-287107 on COLO-320DM is 0.449 μM. Did not inhibit the growth of APC-wild (β-catenin-independent) colorectal cancer cell lines, including RKO, HCT-116, HCC2998 and DLD-1. Western Blot Analysis[1] Cell Line: COLO-320DM cells Concentration: 0.03, 0.1, 0.33, 1, 3, and 10 μM Incubation Time: 16 hours Result: Downregulation of active β-catenin was observed
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Mizutani A, et al. RK-287107, a potent and specific tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model. Cancer Sci. 2018 Dec;109(12):4003-4014.
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