SR-3029 is a strong inhibitor of CK1δ/CK1ε, with IC50 values of 44 nM and 260 nM, respectively. It competes with ATP, having Kis of 97 nM for CK1δ/CK1ε. SR-3029 also inhibits CDK6/cyclin D3, CDK6/cyclin D1, CDK4/cyclin D3, CDK4/cyclin D1, and FLT3, with IC50s of 427, 428, 368, 576, and 3000 nM, respectively. It exhibits inhibitory activity on A375 cells, with an EC50 of 86 nM[1]. SR-3029's efficacy is lower against MCF7 and T47D breast cancer cells, as well as the MCF10A cell line, all of which have low CK1δ expression[2].
SR-3029 动物研究
Animal study
Administered at 20 mg/kg daily via intraperitoneal injection, SR-3029 shows anti-tumor properties in orthotopic MDA-MB-231, MDA-MB-468 (TNBC), SKBR3, and BT474 (HER2+) tumor xenografts without apparent toxicity in mice. The same dosage of SR-3029 also effectively suppresses tumor growth in primary patient-derived xenograft (PDX) models and significantly lowers nuclear β-catenin expression in the tumors of treated mice[2].
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