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| 品牌 | absin | CAS | 475489-16-8 |
|---|---|---|---|
| 分子式 | C27H29N5O | 纯度 | 98% |
| 分子量 | 439.55 | 货号 | abs47028256 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a potent inhibitor of IGF-1R/InsR | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
NVP-AEW541 475489-16-8
| 产品描述 | |
| 描述 | NVP-AEW541 is a potent inhibitor of IGF-1R/InsR with IC50 of 150 nM/140 nM, greater potency and selectivity for IGF-1R in a cell-based assay. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 可溶性/溶解性 | DMSO:88 mg/mL (200.2 mM) |
| 生物活性 | |
| 靶点 | IGF-1R |
| In vitro(体外研究) | NVP-AEW541 inhibits the in vitro kinase activity of the recombinant IGF-IR kinase domain with an IC50 value of 0.15 μM and to be equipotent against the recombinant InsR kinase domain. NVP-AEW541 is confirmed active toward the IGF-IR kinase (IC50=86 nM) and shown to be selective at the cellular level. Indeed, NVP-AEW541 is found to be 27-fold more potent toward the native IGF-IR, as compared to the structurally related native InsR (IC50=2.3 μM). NVP-AEW541 suppresses the IGF-I-mediated survival, soft agar and proliferation of MCF-7 cells with IC50 of 0.162 μM, 0.105 μM and 1.64 μM, respectively. |
| In vivo(体内研究) | Oral administration of NVP-AEW541 (20, 30, or 50 mg/kg) results in abrogation of basal and IGF-I-induced receptor, and PKB and MAPK phosphorylation in the NWT-21 tumor xenograft. NVP-AEW541 is administered by oral gavage twice a day for 14 consecutive days. The control group is similarly treated with 0.2 mL carrier twice a day. Tumor volume and animal weight are measured thrice a week till the end of the treatment. At that time, animals are sacrificed and tumors are collected and formalin fixed for histologic and immunohistochemical analyses. In both cases, NVP-AEW541 treatment causes tumor shrinkage that reached the statistical significance (P=0.0156 and P=0.0111 for HTLA-230 and SK-N-BE2c, respectively). |
| 研究领域 | |
| 研究领域 | CancerCancer Metabolism CancerTumor biomarkers NeuroscienceEndocrine system Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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