| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S83404-2mg买3赠1 |
98.70% | ￥180.00 |
4 | - | - | - | - |
|
S83404-5mg促销 |
98.70% | ￥235.00 ￥188.00 |
6 | - | - | - | - |
|
S83404-10mg促销 |
98.70% | ￥350.00 ￥280.00 |
5 | - | - | - | - |
|
S83404-25mg |
98.70% | ￥450.00 |
5 | - | - | - | - |
|
S83404-50mg |
≥98% | ￥840.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively, and Kis of 97 nM for both kinases. | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | CKIδ:44 nM (IC50);CDK6/cyclin D3:427 nM (IC50);CDK6/cyclin D1:428 nM (IC50);CDK4/cyclin D3:368 nM (IC50);CDK4/cyclin D1:576 nM (IC50);FLT3:3000 nM (IC50);CaseinKinase | ||||||||||||||||||||
| 体外研究： | 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 | ||||||||||||||||||||
| 体内研究： | 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 | ||||||||||||||||||||
| 参考文献： | 1. Bibian M, et al. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4374-80. 2. Rosenberg LH, et al. Therapeutic targeting of casein kinase 1δ in breast cancer. Sci Transl Med. 2015 Dec 16;7(318):318ra202. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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