| 產(chǎn)品描述： | AP26113 is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2. |
| 靶點： |
IGF-1R;EGFR;ALK;EGFR;IGF-1R;ALK |
| 體內(nèi)研究： |
在SU-DHL-1（GI50=9 nM）, H3122 （GI50=4 nM）和 Ba/F3-EML4-ALK v1（1 gI50=3 nM）細胞系中,抑制生長細胞生長。在表達EGFR-DEL(HCC827)的NSCLC細胞系中（IC50=62 nM）,AP26113作用于抑制EGFR 磷酸化,抑制細胞生長 |
| 細胞實驗： |
Three-day cell viability assays are carried out by plating 2,000, 1,500 and 2,000 cells per well of Ba/F3, PC9 or MGH121, respectively, into black transparent-bottom 96-well plates. On the same day for Ba/F3 cells and the following day for PC9 and MGH121 cells, the cells are treated with each TKI across a 10-dose range from 0.3?nM to 10?μM. After 72?h of drug treatment, cell viability is measured using the CellTiter-Glo assay. (Only for Reference) |
| 參考文獻： |
1.Uchibori K, et al. Nat Commun. 2017, 8:14768. 2.Wei-Sheng Huang, et al. J Med Chem, 2016, 59(10):4948-4964. |
| 溶解性： |
H2O:<1 mg/mL Ethanol:98 mg/mL (185.3 mM) DMSO:42 mg/mL (79.4 mM) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.89 ml |
9.452 ml |
18.903 ml |
| 5 mM |
0.378 ml |
1.89 ml |
3.781 ml |
| 10 mM |
0.189 ml |
0.945 ml |
1.89 ml |
| 50 mM |
0.038 ml |
0.189 ml |
0.378 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京