PF04929113
作者：齊岳
發布時間：2023-08-25
08:58:39
點擊數：
產品名稱：PF04929113
產品描述：
| 產品描述 | 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. |
| 靶點活性 | HSP90:41 nM, HER2:37 nM |
| 體外活性 | 免疫組織化學分析表明,在用PF-04929113處理后,SP70表達增加,并降低Ki67,Akt和AR表達.PF-04929113在體內抑制人類MM細胞生長,并且免疫組織化學分析顯示PF-04929113顯著抑制處理的小鼠中的p-ERK和p-Akt.同時,PF-04929113處理顯著降低CD31+細胞和MVD百分比,與體內血管生成的抑制作用一致.PF-04929113對腫瘤發展的抑制可能由增殖減少（Ki67和Akt表達降低）或凋亡率增加（增加的ApopTag染色）共同引起. |
| 體內活性 | PF-04929113對Her-2穩定性表現出有效的作用并導致預期的Hsp70上調。PF-04929113顯示針對廣泛癌癥細胞類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）。 |
| 激酶實驗 | 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. |
| 細胞實驗 | 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. |
| 動物實驗 | 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. |
| 別名 | PF-04929113, SNX-5422, PF 04929113 |
| 分子量 | 521.541 |
| 分子式 | C25H30F3N5O4 |
| CAS No. | 908115-27-5 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
Ethanol: 3 mg/mL(5.8 mM)
DMSO: 96 mg/mL (184.1 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
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