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NVP-ADW742
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
NVP-ADW742图片
CAS NO:475488-23-4
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议
200mg电议

产品介绍
NVP-ADW742 (ADW742) 是一种具有口服活性的选择性 IGF-1R 酪氨酸激酶抑制剂，IC50 为 0.17 μM。
Cas No.475488-23-4
别名5-(3-苄氧基苯基)-7-[反式-3-[(吡咯烷-1-基)甲基]环丁基]-7H-吡咯并[2,3-D]嘧啶-4-胺,ADW742; GSK 552602A; ADW
化学名5-(3-phenylmethoxyphenyl)-7-[3-(pyrrolidin-1-ylmethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-4-amine
Canonical SMILESC1CCN(C1)CC2CC(C2)N3C=C(C4=C3N=CN=C4N)C5=CC(=CC=C5)OCC6=CC=CC=C6
分子式C28H31N5O
分子量453.58
溶解度DMF: 30 mg/mL,DMSO: 30 mg/mL,Ethanol: 30 mg/mL,Ethanol:PBS (pH 7.2) (1:10): 0.09 mg/mL
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

NVP-ADW742 is a novel inhibitor of IFG-1receptor (IGF-1R) kinase with the IC50 value of 0.17μM [1].

NVP-ADW742 has shown above 16-fold effective function against IGF-1R than insulin receptor (InsR). Furthermore, NVP-ADW742 has also been reported to inhibit other kinases , with the IC50 values of ＞10μM for HER2, PDGFR, VEGFR-2, or Bcr-Abl p210, and the IC50 values ＞5μM for c-Kit [1]. Besides, NVP-ADW742 combined with etoposide and carboplatin has been reported to inhibit cell growth and induce cytotoxicity by MTT assay using the small cell lung cancer (SCLC), including H526, H146, WBA and H209 cell lines. In addition, NVP-ADW742 has been revealed to completely inhibit the expression of VEGF mRNA which induced by IGF-I in H526 cells [2].

References:
[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.