| 产品描述： | SNX-5422 is a synthetic, novel, small molecule Hsp90 Inhibitor. As an oral formulation that demonstrates strong efficacy and tolerability, SNX-5422 is positioned as a breakthrough therapy with broad applicability across a wide range of cancers. |
| 靶点： |
HSP;HER;HSP; HER |
| 体内研究： |
PF-04929113对Her-2稳定性表现出有效的作用并导致预期的Hsp70上调。PF-04929113显示针对广泛癌症细胞类型的有效抗增殖活性,例如,MCF-7（IC50 = 16 nM）,SW620（IC50 = 19 nM）,K562（IC50 = 23 nM）,SK-MEL-5（IC50 = 25 nM）和A375（IC50 = 51 nM） |
| 细胞实验： |
Cell lines: MCF-7,SW620,K562,SK-MEL-5 and A375 cancer cell lines. Concentrations: 0-300 nM. Method: Proliferation rates are measured by seeding cells into 96-well plates,followed by compound addition 24 h later.After addition of PF-04929113,cells are allowed to grow for either an additional 72 or 144 h depending on the rate of growth.At harvest,media is removed and DNA content for individual wells is determined using CyQuant DNA dye.Levels of Hsp90 client proteins and phosphor-regulated proteins in A375 are measured by high content analysis (HCA) using an ArrayScan 4.5 instrument after 24 hours of treatment with PF-04929113,followed by methanol fixation.After fixation in 4% PBS-buffered formalin and permeablization with 0.1% TX-100,cells are probed with anti-Her2,antiphospho-S6 (pS6),antipERK,and anti-Hsp70 primary antibodies,followed by TRITC or FITC conjugated secondary antibodies.Nuclei are also stained with Hoechst DNA binding dye.For each well,250-500 individual nuclei are identified along with the avera |
| 动物实验： |
Animal Models: 5 ×106 MM.1S cells are inoculated subcutaneously in the Fox Chase SCID mice (6-7 weeks old). Formulation: PF-04929113 is dissolved in 1% carboxy methylcellulose/0.5% Tween 80 at 10 mg/mL and stored at 4 °C. Dosages: 20 or 40 mg/kg. Administration: orally 3 times per week,3 weeks in total. |
| 参考文献： |
1.Lamoureux F, et al, Clin Cancer Res, 2011, 17(8), 2301-2313. 2.Huang KH, et al, J Med Chem, 2009, 52(14), 4288-4305 3.Yutaka Okawa, et al, Blood, 2009, 113(4), 846-855. |
| 溶解性： |
H2O:<1 mg/mL Ethanol:3 mg/mL(5.8 mM) DMSO:96 mg/mL (184.1 mM) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.917 ml |
9.587 ml |
19.174 ml |
| 5 mM |
0.383 ml |
1.917 ml |
3.835 ml |
| 10 mM |
0.192 ml |
0.959 ml |
1.917 ml |
| 50 mM |
0.038 ml |
0.192 ml |
0.383 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京