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SR-3029

CAS No. : 1454585-06-8

MCE 國(guó)際站：SR-3029

產(chǎn)品活性：SR-3029 是一種有效的，ATP 競(jìng)爭(zhēng)性的 CK1δ 和 CK1ε 的抑制劑，IC₅₀ 值分別為 44 nM 和 260 nM，K_i 均為 97 nM。

研究領(lǐng)域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt

作用靶點(diǎn)：Casein Kinase

In Vitro: SR-3029 is a potent CK1δ/CK1ε inhibitor, with IC₅₀s of 44 nM and 260 nM, respectively. SR-3029 is ATP competitive, with K_is of 97 nM for CK1δ/CK1ε. SR-3029 also blocks 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. SR-3029 shows inhibitory effects on A375 cells, with an EC₅₀ of 86 nM. CK1δ is a necessary and sufficient driver of Wnt/β-catenin signaling in human breast cancer. SR-3029 shows less potent activities against MCF7 and T47D breast cancer cells and the MCF10A cell line, which express low amounts of CK1δ.

In Vivo: SR-3029 (20 mg/kg daily i.p.) exibits anti-tumor effects in rthotopic MDA-MB-231, MDA-MB-468 (TNBC), SKBR3 and BT474 (HER2+) tumor xenografts with no overt toxicity in mice. SR-3029 (20 mg/kg daily i.p.) also effectively inhibits the growth of tumor in primary patient-derived xenograft (PDX) models. In addition, SR-3029 (20 mg/kg, i.p.) strongly reduces the expression of nuclear β-catenin in tumors of mice.

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