PF-04929113 (SNX-5422)

製品コードS2656

PF-04929113 (SNX-5422)化学構造

分子量(MW):521.53

PF-04929113 (SNX-5422)は一種の有効で、選択性的なHSP90阻害剤で、Kd値が41nMですが、Her-2分解を誘導して、このIC50値が37nMになります。臨床 1/2期。

サイズ 価格 在庫  
JPY 80633.28 あり
JPY 38876.76 あり
JPY 67674.36 あり

カスタマーフィードバック(3)

  • J Biol Chem 2013 288(23), 16308-20. PF-04929113 (SNX-5422) purchased from Selleck.

    Effect of SNX-2112 on E. histolytica morphology. Trophozoites were treated with 3 uM SNX-2112 for 48 h. (A) E. histolytica trophozoites treated with 0.5% DMSO. Arrow indicates live trophozoite. Magnification, x 10. (B) E. histolytica trophozoites treated with 3 uM SNX-2112. Treatment caused complete lysis of trophozoites (arrow). Magnification, x 10. Trophozoites were imaged under phase-contrast microscope.

    Antimicrob Agents Chemother 2014 58(7), 4138-44. PF-04929113 (SNX-5422) purchased from Selleck.

  • 8505C and CAL62 cells were treated with SNX5422 at 5 μM for 72 h, and the protein levels of hsp90, hsp70, Raf-1, GSK3b, and total and phospho-Akt were measured. All experiments were performed in triplicate. The blots are representative of independent experiments.

    Endocrine, 2016, 51(2):274-82.. PF-04929113 (SNX-5422) purchased from Selleck.

製品安全説明書

HSP (e.g. HSP90)阻害剤の選択性比較

生物活性

製品説明 PF-04929113 (SNX-5422)は一種の有効で、選択性的なHSP90阻害剤で、Kd値が41nMですが、Her-2分解を誘導して、このIC50値が37nMになります。臨床 1/2期。
ターゲット
HER2 [1] HSP90 [1]
37 nM 41 nM(Kd)
体外試験

PF-04929113 is a small-molecule Hsp90 inhibitor based on the 6,7-dihydro-indazol-4-one scaffold. PF-04929113 developed by Serenex, converts to SNX-2122, which is the active Hsp90 inhibitor form. PF-04929113 exhibits potent effects on Her-2 stability and causes expected up-regulation of Hsp70. PF-04929113 shows potent antiproliferative activity against a broad range of cancer cell types, e.g. MCF-7 (IC50=16 nM), SW620 (IC50=19 nM), K562 (IC50=23 nM), SK-MEL-5 (IC50=25 nM), and A375 (IC50=51 nM). [1]

体内試験 PF-04929113 inhibits human MM cell growth in vivo, and immuno-histochemical analysis shows PF-04929113 significantly inhibits p-ERK and p-Akt in treated mice. Meanwhile, PF-04929113 treatment significantly decreases the percentage of CD31+ cells and MVD, consistent with an inhibitory effect on angiogenesis in vivo. A 50 mg/kg administration of PF-04929113 delivered 3 times per week significantly delays castrate-resistant LNCaP tumor growth and prolongs cancer specific survival. [2] Immuno-histochemical analysis indicates increased SP70 expression, and decreases Ki67, Akt, and AR expression, after treatment with PF-04929113. Inhibition of tumor progression by PF-04929113 may result from a combination of decreased proliferative (reduced Ki67 and Akt expression) or increased apoptosis (increased ApopTag staining) rates. [3]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
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Affinity for Hsp90:

Hsp90 from porcine spleen extract is isolated by affinity capture on a purine-affinity media. The Hsp90 loaded media is then 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.
細胞試験: [1]
+ 展開
  • 細胞株: MCF-7, SW620, K562, SK-MEL-5 and A375 cancer cell lines
  • 濃度: 0-300 nM
  • 反応時間: 72 or 144 hours
  • 実験の流れ: All assays are done in 96-well plates. All cell lines are purchased from ATCC. 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 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.
    (参考用のみ)
動物試験:[2]
+ 展開
  • 動物モデル: 5 × 106 MM.1S cells are inoculated subcutaneously in the Fox Chase SCID mice (6-7 weeks old).
  • 製剤: PF-04929113 is dissolved in 1% carboxy methylcellulose/0.5% Tween 80 at 10 mg/mL and stored at 4 °C for in vivo stud
  • 投薬量: 20 or 40 mg/kg
  • 投与方法: PF-04929113 is administered orally 3 times per week, total 3 weeks.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 104 mg/mL (199.41 mM)
Ethanol 5 mg/mL (9.58 mM)
Water Insoluble
体内 順序で溶剤を入れること:
0.5% CMC+0.25% Tween 80
25 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 521.53
化学式

C25H30F3N5O4

CAS No. 908115-27-5
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02973399 Recruiting Cancer Esanex Inc. February 7, 2017 Phase 1
NCT00644072 Completed Lymphoma|Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) March 7, 2008 Phase 1
NCT02612285 Terminated Cancer Esanex Inc. March 2016 Phase 2
NCT02063958 Active, not recruiting Cancer Esanex Inc. February 2014 Phase 1
NCT01635712 Active, not recruiting Cancer Esanex Inc. February 2014 Phase 1
NCT01892046 Active, not recruiting Cancer Esanex Inc. November 2013 Phase 1

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

HSP (e.g. HSP90)信号経路図

HSP (e.g. HSP90) Inhibitors with Unique Features

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