化学性质
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 453.58 |
| Cas No. | 475488-23-4 |
| Formula | C28H31N5O |
| Solubility | Soluble in DMSO |
| Chemical Name | 5-(3-phenylmethoxyphenyl)-7-[3-(pyrrolidin-1-ylmethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-4-amine |
| Canonical SMILES | C1CCN(C1)CC2CC(C2)N3C=C(C4=C3N=CN=C4N)C5=CC(=CC=C5)OCC6=CC=CC=C6 |
| 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。 |
资料参考
NVP-ADW742是一种新的IFG-1受体(IGF-1R)激酶抑制剂,IC50值为0.17 μM[1].
NVP-ADW742对IGF-1R比对胰岛素受体(InsR)更有效(超过16倍).此外,NVP-ADW742也可抑制其他激酶,对HER2\PDGFR\VEGFR-2或Bcr-Abl p210的IC50值大于10 μM,对c-Kit的IC50值大于5 μM[1].另外,在针对包括H526\H146\WBA和H209细胞系的小细胞肺癌(SCLC)的MTT试验中,NVP-ADW742与依托泊苷和卡铂联合使用可抑制细胞生长,诱发细胞毒性.除此之外,NVP-ADW742可完全抑制H526细胞中IGF-I诱导的VEGF mRNA表达[2].
参考文献：
[1] Mitsiades CS1, Mitsiades NS, McMullan CJ, Poulaki V, Shringarpure R, Akiyama M, Hideshima T, Chauhan D, Joseph M, Libermann TA, García-Echeverría C, Pearson MA, Hofmann F, Anderson KC, Kung AL. Inhibition of the insulin-like growth factor receptor-1 tyrosine kinase activity as a therapeutic strategy for multiple myeloma, other hematologic malignancies, and solid tumors . Cancer Cell. 2004 Mar; 5(3):221-30.
[2]Warshamana-Greene GS1, Litz J, Buchdunger E, García-Echeverría C, Hofmann F, Krystal GW. The insulin-like growth factor-I receptor kinase inhibitor, NVP-ADW742, sensitizes small cell lung cancer cell lines to the effects of chemotherapy. Clin Cancer Res. 2005 Feb 15;11(4):1563-71.
生物活性
| Description | NVP-ADW742是一种IGF-1R的选择性抑制剂,IC50值为0.17 μM. |
| 靶点 | IGF-1R | | | | | |
| IC50 | 0.17 μM | | | | | |
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