Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF04929113 (SNX-5422) 是一种合成的新型小分子 Hsp90 抑制剂。作为一种具有强大疗效和耐受性的口服制剂,它被定位为一种突破性疗法,在广泛的癌症中具有广泛的适用性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 315 | 现货 | ||
2 mg | ¥ 453 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 997 | 现货 | ||
25 mg | ¥ 2,160 | 现货 | ||
50 mg | ¥ 3,230 | 现货 | ||
100 mg | ¥ 4,990 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 855 | 现货 |
产品描述 | PF04929113 (SNX-5422) is a synthetic, novel, small molecule Hsp90 Inhibitor. As an oral formulation that demonstrates strong efficacy and tolerability, PF04929113 is positioned as a breakthrough therapy with broad applicability across a wide range of cancers. |
靶点活性 | HSP90:41 nM, HER2:37 nM |
体外活性 | 免疫组织化学分析表明,在用PF-04929113处理后,SP70表达增加,并降低Ki67,Akt和AR表达.PF-04929113在体内抑制人类MM细胞生长,并且免疫组织化学分析显示PF-04929113显著抑制处理的小鼠中的p-ERK和p-Akt.同时,PF-04929113处理显著降低CD31+细胞和MVD百分比,与体内血管生成的抑制作用一致.PF-04929113对肿瘤发展的抑制可能由增殖减少(Ki67和Akt表达降低)或凋亡率增加(增加的ApopTag染色)共同引起. |
体内活性 | 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)。 |
激酶实验 | The Hsp90 loaded media is challenged with PF-04929113 at a given concentration, ranging from 0.8 to 500 μM, and the amount of Hsp90 liberated at each concentration is determined by Bradford protein assay. The resulting IC50 values are corrected for the ATP ligand concentration and presented as apparent Kd values. |
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 average staining intensity for the client and phospho-proteins for each cell.Average client staining intensities are then calculated for each well. |
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. |
别名 | PF-04929113, SNX-5422, PF 04929113 |
分子量 | 521.53 |
分子式 | C25H30F3N5O4 |
CAS No. | 908115-27-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 3 mg/mL(5.8 mM)
DMSO: 96 mg/mL (184.1 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.9174 mL | 9.5872 mL | 19.1744 mL | 47.9359 mL |
5 mM | 0.3835 mL | 1.9174 mL | 3.8349 mL | 9.5872 mL | |
DMSO | 10 mM | 0.1917 mL | 0.9587 mL | 1.9174 mL | 4.7936 mL |
20 mM | 0.0959 mL | 0.4794 mL | 0.9587 mL | 2.3968 mL | |
50 mM | 0.0383 mL | 0.1917 mL | 0.3835 mL | 0.9587 mL | |
100 mM | 0.0192 mL | 0.0959 mL | 0.1917 mL | 0.4794 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PF04929113 908115-27-5 Angiogenesis Cytoskeletal Signaling JAK/STAT signaling Metabolism Tyrosine Kinase/Adaptors HSP HER PF-04929113 SNX5422 SNX-5422 SNX 5422 PF 04929113 Inhibitor inhibitor inhibit