CAN508 (60 mg/kg; i.p.; daily for 10 days) has antitumor effects in esophageal adenocarcinoma xenografts[1]. Animal Model: 4 weeks-old female nude mice (esophageal adenocarcinoma xenografts)[1] Dosage: 60 mg/kg Administration: I.p.; daily for 10 days Result: Caused reduction of tumor growth starting from post-treatment day three with 50.83% reduction.
In Vitro
CAN508 reduces the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays[1]. CAN508 (20-40 μM; 72 hours) significantly reduces cell proliferation in a dose dependent manner in all three esophageal adenocarcinoma cell lines (SKGT4, OE33 and FLO-1 cells) with IC50s ranging from 34.99 to 91.09 μM[2]. CAN508 (40 μM; 72 hours) increases apoptosis in all three esophageal adenocarcinoma cells[2]. Apoptosis Analysis[1] Cell Line: SKGT4, OE33 and FLO-1 cells Concentration: 40 μM Incubation Time: 72 hours Result: Increased apoptosis by 2 fold in all three esophageal adenocarcinoma cells compared to untreated controls.
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Krystof V, et al. 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006;49(22):6500-6509.
[2]. Tong Z, et al. Antitumor effects of cyclin dependent kinase 9 inhibition in esophageal adenocarcinoma. Oncotarget. 2017;8(17):28696-28710.
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