| CAS NO: | 1097917-15-1 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 200mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 580.74 |
| Cas No. | 1097917-15-1 |
| Formula | C29H40N8O3S |
| Synonyms | ASP 3026;ASP-3026 |
| Solubility | insoluble in H2O; ≥14.53 mg/mL in DMSO; ≥4.9 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)-1,3,5-triazine-2,4-diamine |
| Canonical SMILES | CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC=NC(=N2)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
ASP3026是ALK的选择性抑制剂，IC50值为3.5 nM[1]。
ASP3026是ALK有效的抑制剂，选择性与已报导的ALK抑制剂Crizotinib不同。当对一组86个酪氨酸激酶进行测试时发现，ASP3026对ALK、ROS和ACK激酶的选择性最高。NCI-H2228 NSCLC细胞表达EML4-ALK，用ASP3026处理5天，导致细胞生长受到抑制，IC50值为64.8 nM。ASP3026也可抑制NPM-ALK+ALCL细胞的存活能力，在SU-DHL-1、SUP-M2、SR-786和Karpas 299细胞中的IC50值分别为0.4、0.75、1和2.5 M[2，3]。
NCI-H2228皮下移植的小鼠口服ASP3026，ALK的磷酸化和肿瘤的生长显著降低。ASP3026以30 mg/kg/d处理2周导致肿瘤退化了78%。在老鼠Karpas 299细胞中，ASP3026处理引起明显的淋巴瘤退化[2，3]。
参考文献：
[1] Kuromitsu S, Mori M, Shimada I, et al. Anti-tumor activity of ASP3026, a novel and selective ALK inhibitor of anaplastic lymphoma kinase (ALK).Annual Meeting of the American Association for Cancer Research (AACR), Orlando, FL. 2011.
[2] Mori M, Ueno Y, Konagai S, et al. The Selective Anaplastic Lymphoma Receptor Tyrosine Kinase Inhibitor ASP3026 Induces Tumor Regression and Prolongs Survival in Non–Small Cell Lung Cancer Model Mice. Molecular cancer therapeutics, 2014, 13(2): 329-340.
[3] George S K, Vishwamitra D, Manshouri R, et al. The ALK inhibitor ASP3026 eradicates NPM-ALK+ T-cell anaplastic large-cell lymphoma in vitro and in a systemic xenograft lymphoma model. Oncotarget, 2014, 5(14): 5750-5763.
| Description | ASP3026是ALK的选择性抑制剂，IC50值为3.5 nM。 | |||||
| 靶点 | ALK | |||||
| IC50 | 3.5 nM | |||||
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