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PF04929113

PF04929113

产品编号 T6341   CAS 908115-27-5
别名: PF-04929113, SNX-5422, PF 04929113

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。

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PF04929113 Chemical Structure
PF04929113, CAS 908115-27-5
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
其他形式的 PF04929113:
产品目录号及名称: PF04929113 (T6341)
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选择批次  
纯度: 99.06%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 3 mg/mL(5.8 mM)

DMSO: 96 mg/mL (184.1 mM)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Huang KH, et al, J Med Chem, 2009, 52(14), 4288-4305 2. Yutaka Okawa, et al, Blood, 2009, 113(4), 846-855. 3. Lamoureux F, et al, Clin Cancer Res, 2011, 17(8), 2301-2313.
(S)-Afatinib Epertinib hydrochloride Tuxobertinib BMS-599626 CUDC-101 Sigma-1 receptor antagonist 3 Dihydroberberine BMS-599626 2HCL(714971-09-2 Free base)

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 抗癌临床化合物库 抗癌活性化合物库 抗癌药物库 抗肝癌化合物库 临床期小分子药物库 抗乳腺癌化合物库 细胞重编程化合物库 口服活性化合物库 代谢化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

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

 

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