PF-04217903

製品コードS1094

PF-04217903化学構造

分子量(MW):372.38

PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM in A549 cell line, susceptible to oncogenic mutations (no activity to Y1230C mutant). Phase 1.

サイズ 価格(税別) 在庫  
In DMSO JPY 28500 あり
JPY 20200 あり
JPY 28500 あり
JPY 80000 あり
JPY 146400 あり
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バルク問合せ

カスタマーフィードバック(4)

  • Clonogenicity of LXFA 526L and LXFA 1647L with titration of the MET inhibitor PF-04217903 and combination of PF-04217903 at 0.1 uM with 0.66 uM cetuximab.

    Eur J Cancer 2011 47(8), 1231-43. PF-04217903 purchased from Selleck.

  • Western blot analysis of c-Met, MAPK and Akt. 0-100nM PF04217903 was added.

     

     

    Dr. Zhang of Tianjin Medical University. PF-04217903 purchased from Selleck.

  • (A) p-MET, p-eIF4E, and p-ERK1/2 levels in S462 cells 24 hours after treatment with 1 μM PF04217903 and 750 nM PD901. (B) Change in cell number after treatment with 1 μM PF04217903 (PF903) and/or 750 nM PD901. Graph represents the average log2 of fold change in cell number 72 hours after treatment relative to time 0 (mean ± SD, n = 3).

    J Clin Invest, 2016, 126(6):2181-90. PF-04217903 purchased from Selleck.

  • MET signaling inhibition attenuated the invasion and metastasis-promoting effects induced by VEGF inhibition in hepa1-6 orthotopic models. Inhibitory effects of VEGF antibody, PF-04217903 alone, and their combination on HCC growth and intrahepatic metastasis in the hepa1-6 orthotopic models. Tumor volumes and numbers of tumor foci in the orthotopic implantation models were measured and quantified.

    J Exp Clin Cancer Res, 2018, 37(1):93. PF-04217903 purchased from Selleck.

製品安全説明書

c-Met阻害剤の選択性比較

生物活性

製品説明 PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM in A549 cell line, susceptible to oncogenic mutations (no activity to Y1230C mutant). Phase 1.
ターゲット
c-Met [1]
(A549 cells)
4.8 nM
体外試験

Being more selective than staurosporine or PF-02341066, PF-04217903 displays >1000-fold selectivity for c-Met over a panel of 208 kinases, although more susceptible to oncogenic mutations of c-Met that attenuate potency than PF-02341066. In addition to WT c-Met, PF-04217903 displays similar potency to inhibit the activity of c-Met-H1094R, c-Met-R988C, and c-Met-T1010I with IC50 of 3.1 nM, 6.4 nM, and 6.7 nM, respectively, but has no inhibitory activity against c-Met-Y1230C with IC50 of >10 μM. [1] PF-04217903 in combination with sunitinib significantly inhibits endothelial cells, but not the tumor cells B16F1, Tib6, EL4, and LLC [2] PF-04217903 significantly inhibits the clonogenic growth of LXFA 526L and LXFA 1647L with IC50 values of 16 nM, and 13 nM, respectively, yielding an additive effect when in combination with cetuximab. [3] PF-04217903 potently inhibits c-Met-driven processes such as cell growth, motility, invasion, and morphology of a variety of tumor cells. PF-04217903 treatment (2 μM) increased cell death of GTL-16 cells, which involves the downregulation of phosphorylated 4E-BP1, ERK/MAPK associated proteins and PI3K/AKT pathway. [4]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A549 cells NHLMNVZHfW6ldHnvckBie3OjeR?= NYr3SHc1OSCq MV3BcpRi\2:waYP0JIFkfGm4aYT5JIF1KGNvTVXUJJJm[2WydH;yJIlvKGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBifXSxcHjvd5Bpd3K7bHH0bY9vKGGodHXyJFEhcHJiYomgSWxKW0FuIFnDOVA:PCCwTR?= NXj2eFRNOjJ7MkS3N|Q>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 Although unable to inhibit tumor growth in the sunitinib-sensitive B16F1 and Tib6 tumor models, the combination of PF-04217903 and sunitinib significantly inhibits tumor growth in sunitinib-resistant EL4, and LLC tumor models compared with sunitinib or PF-04217903 alone by significantly blocking vascular expansion, indicating a functional role for HGF/c-Met axis in the sunitinib-resistant tumors. [2]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
- 合併

Cellular c-Met phosphorylation ELISA:

A549 cells with endogenous human WT c-Met are seeded in 96-well plates in growth medium and cultured overnight. On the second day of the assay, the growth medium is replaced with serum-free medium (with 0.04% BSA). Serial dilutions of PF-04217903 are added to each well, and cells are incubated at 37 °C for 1 hour. Then 40 ng/mL HGF is added to the cells for 20 minutes. The cells are washed once with HBSS supplemented with 1 mM Na3VO4, and protein lysates are generated from cells using lysis buffer. Phosphorylation of c-Met is assessed by an ELISA method utilizing capture antibodies specific for c-Met and a detection antibody specific for phosphorylated tyrosine residues. Antibody-coated plates are incubated in the presence of protein lysates at 4 °C overnight and washed with 1% Tween 20 in PBS seven times. HRP-PY20 (horseradish peroxidase-conjugated anti-phosphotyrosine) is diluted 1:500 in blocking buffer and added to each plate for 30 minutes. Plates are then washed again, and TMB peroxidase substrate is added to initiate the HRP-dependent colorimetric reaction and the reaction stopped by addition of 0.09 N H2SO4. ELISA end points are the absorbance measured at 450 nm using a spectrophotometer. IC50 value is calculated by concentration-response curve fitting utilizing a Microsoft Excel-based four-parameter analytical met
細胞試験: [2]
- 合併
  • 細胞株: B16F1, Tib6, EL4, and LLC, HUVECs and C166 cells
  • 濃度: Dissolved in DMSO, final concentrations ~2 μM
  • 反応時間: 4 days
  • 実験の流れ: Cells are treated with different concentrations PF-04217903 for 4 days. Cell proliferation is assessed by counting content of each well using a Coulter counter machine.
    (参考用のみ)
動物試験:[2]
- 合併
  • 動物モデル: Immunodeficient nude mice (nu/nu) subcutaneously implanted with tumor cell lines B16F1, EL4, LLC, or Tib6
  • 製剤: Dissolved in DMSO, and diluted in saline
  • 投薬量: 45 mg/kg
  • 投与方法: Orally
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 5 mg/mL (13.42 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
2mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程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 372.38
化学式

C19H16N8O

CAS No. 956905-27-4
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

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    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

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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 ( 入力 出力 )

  • 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

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

c-Metシグナル伝達経路

c-Met Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID