PF04929113
作者：齊岳
發(fā)布時(shí)間：2023-08-25
08:58:39
點(diǎn)擊數(shù)：
產(chǎn)品名稱：PF04929113
產(chǎn)品描述：
| 產(chǎn)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(diǎn)活性 | HSP90:41 nM, HER2:37 nM |
| 體外活性 | 免疫組織化學(xué)分析表明,在用PF-04929113處理后,SP70表達(dá)增加,并降低Ki67,Akt和AR表達(dá).PF-04929113在體內(nèi)抑制人類MM細(xì)胞生長(zhǎng),并且免疫組織化學(xué)分析顯示PF-04929113顯著抑制處理的小鼠中的p-ERK和p-Akt.同時(shí),PF-04929113處理顯著降低CD31+細(xì)胞和MVD百分比,與體內(nèi)血管生成的抑制作用一致.PF-04929113對(duì)發(fā)展的抑制可能由增殖減少（Ki67和Akt表達(dá)降低）或凋亡率增加（增加的ApopTag染色）共同引起. |
| 體內(nèi)活性 | PF-04929113對(duì)Her-2穩(wěn)定性表現(xiàn)出有效的作用并導(dǎo)致預(yù)期的Hsp70上調(diào)。PF-04929113顯示針對(duì)廣泛*癥細(xì)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(shí)驗(yàn) | 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(xì)胞實(shí)驗(yàn) | 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(dòng)物實(shí)驗(yàn) | 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(chǔ)
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 )
聯(lián)系我們：
郵箱：2519696869@qq.com
QQ: 2519696869
電話：18066853083
微信：18066853083
公司介紹：
西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
主營(yíng)產(chǎn)品：COF、MOF單體系列：三蝶烯衍生物、金剛烷衍生物、四苯甲烷衍生物、peg、上轉(zhuǎn)換、石墨烯、光電材料、點(diǎn)擊化學(xué)、凝集素、載玻片、蛋白質(zhì)交聯(lián)劑、脂質(zhì)體、蛋白、多肽、氨基酸、糖化學(xué)等。
