SR-3029

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SR-3029 是一种有效、高选择性、ATP 竞争性和脑穿透性酪蛋白激酶 1δ/ε (CK1δ/ε) 抑制剂，IC50 分别为 44/260 nM。

SR-3029 is a potent, highly selective, ATP-competitive and brain penetrating Casein Kinase 1δ/ε (CK1δ/ε) inhibitor with IC50 of 44/260 nM, respectively; inhibits melanoma A375 cell growth with IC50 of 86 nM; triggers apoptosis of CK1δ-expressing breast tumor cells ex vivo, tumor regression in orthotopic models of triple-negative breast cancer in mice model.(In Vitro):The in vitro activities of Moxifloxacin and Amoxicillin are compared by time-kill curve and inhibition of intracellular growth experiments by using a model of bone marrow-derived mouse macrophages infected by?L. monocytogenes?EGDe. Moxifloxacin acts much more rapidly, beginning to exert its effects in the first 3 h and achieving complete broth sterilization within 24 h of incubation. Moxifloxacin appears to have a protective effect against macrophage lysis, as many cells are still viable after 24 h of incubation.(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.

SR-3029 is a potent CK1δ/CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively. SR-3029 is ATP competitive, with Kis 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.

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.

SR3029

Metabolic Enzyme/Protease

Casein Kinase

CK1δ

Cancer

——

1454585-06-8

480.4452

C23H19F3N8O

>98% (HPLC)

DMSO: ≥ 30 mg/mL

FC1=CC(N2C=NC3=C(NCC4=NC5=CC=C(F)C(F)=C5N4)N=C(N6CCOCC6)N=C23)=CC=C1

9H-Purin-6-amine, N-[(6,7-difluoro-1H-benzimidazol-2-yl)methyl]-9-(3-fluorophenyl)-2-(4-morpholinyl)-

(-20℃)

With Ice Pack

≥ 2 years