| CAS: | 1449685-96-4 | |
| 分子式: | C30H31F3N4O3 | |
| 分子量: | 552.59 | |
| 英文名称: |
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| 用途: | DDR1-IN-1是一种有效的选择性discoidin domain receptor 1 (DDR1)受体酪氨酸激酶抑制剂，IC50 为 105 nM，选择性大约是作用于DDR2的3倍。在U2OS细胞中，DDR1-IN-1抑制基底DDR1自身磷酸化，EC50为86 nM，并且缺乏胶原蛋白刺激时具有更强的DDR1自身磷酸化抑制作用。在一组具有DDR1功能获得性突变和/或过表达的不同癌细胞系中，DDR1-IN-1在低于10 μM的浓度下，不抑制细胞增殖，而GSK2126458会增强DDR1-IN-1的抗增殖活性。[1] |
| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | |||||||||||||||||||||||||||||
| D872990 | MACKLIN | DDR1-IN-1 | 97% | 455元/5mg; 733元/10mg; 1466元/25mg; | 咨询 | ||||||||||||||||||||||||||||
储存：-20℃ 状态：白色到米黄色粉末 | |||||||||||||||||||||||||||||||||
| D792373 | MACKLIN | DDR1-IN-1 | 10mM in DMSO | 960元/1ml; | 咨询 | ||||||||||||||||||||||||||||
储存：-20°C | |||||||||||||||||||||||||||||||||
| SML2274 | Sigma-Aldrich | DDR1-IN-1 | ≥98% (HPLC) | 1319.43元/5 MG; 3336.73元/25 MG; | 咨询 | ||||||||||||||||||||||||||||
产品说明 生化/生理作用 DDR1-IN-1 is a type II, subtype-selective discoidin domain receptor (DDR) tyrosine kinase inhibitor (DDR1/2 IC50 = 105 nM/413 nM) that effectively blocks collagen-induced DDR1 pY513 autophosphorylation in U2OS cells (EC50 = 86.76 nM) with excellent selectivity over a panel of >380 kinases. DDR1-IN-1 inhibits DDR2-mediated MT1-MMP activation in human rheumatoid synovial fibroblasts (RASF) upon collagen stimulation (IC50 < 2.5 μM) and enhances PI3K/mTOR inhibitor GSK2126458 antiproliferation efficacy in SNU-1040 colorectal cancer culture (123%, 70%, 50% of control, respectively, post 48-hr 250 nM DDR1-IN-1, 82.5 nM GSK2126458, or combined treatment). ent). ned treatment). 基本信息
产品性质
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