產品描述: NVP-BVU972 is a selective and potent Met inhibitor with IC50 of 14 nM. |
靶點:
c-Met/HGFR |
體內研究:
NVP-BVU972有效抑制MET基因擴散的細胞系GTL-16,MKN-45和EBC-1的生長,IC50分別為66,82和32 nM。NVP-BVU972有效抑制MET激酶,而對其他激酶(包括最密切相關的激酶)RON抑制作用很低,IC50>1000 nM。NVP-BVU972抑制GTL-16細胞中組成型MET磷酸化,抑制A549細胞中HGF刺激的MET磷酸化,IC50分別為7.3和 22 nM。NVP-BVU972作用于表達野生型TPR-MET的BaF3細胞,劑量依賴性降低TPR-MET磷酸化。 |
細胞實驗:
BaF3 cells containing TPR-MET or various mutants thereof are grown in RPMI 1640 medium containing 10% fetal calf serum. For maintenance of parental BaF3 cells the medium is additionally supplemented with 10 ng/mL interleukin-3 (IL-3). For proliferation assays, BaF3 cells are seeded on 96-well-plates in triplicates at 104 cells per well and incubated with various concentrations of NVP-BVU972 for 72 hours followed by quantification of viable cells using a resazurin sodium salt dye reduction readout. IC50 values are determined with the XLFit Excel Add-In using a 4-parameter dose response model.(Only for Reference) |
參考文獻:
1. Tiedt R, et al. Cancer Res. 2011, 71(15), 5255-5264. |
溶解性:
Soluble in DMSO、Ethanol |
保存條件:
-20℃ |
配置溶液濃度參考:
|
1mg |
5mg |
10mg |
1 mM |
2.938 ml |
14.689 ml |
29.379 ml |
5 mM |
0.588 ml |
2.938 ml |
5.876 ml |
10 mM |
0.294 ml |
1.469 ml |
2.938 ml |
50 mM |
0.059 ml |
0.294 ml |
0.588 ml |
|
注意: |
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