PF-00562271

製品コードS2672 別名:PF-562271 Besylate

PF-00562271化学構造

分子量(MW):665.66

PF-00562271はPF-562271のベンゼンスルホン(benzenesulfonate)酸塩で、一種の有効で、ATP競争性的で、可逆的なFAK阻害剤で、IC50値が1.5 nMです。PF-00562271は、FAKに作用する選択性はPyk2に作用する選択性より10倍左右が高くなって、他のタンパク質キナーゼ(多少のCDKsを抜く)に作用する選択性より100倍以上が高くなります。臨床1期。

サイズ 価格(税別)  
JPY 44820.00
JPY 78020.00

カスタマーフィードバック(1)

  • Mol Ther 2012 20(5), 972-83. PF-00562271 purchased from Selleck.

製品安全説明書

FAK阻害剤の選択性比較

生物活性

製品説明 PF-00562271はPF-562271のベンゼンスルホン(benzenesulfonate)酸塩で、一種の有効で、ATP競争性的で、可逆的なFAK阻害剤で、IC50値が1.5 nMです。PF-00562271は、FAKに作用する選択性はPyk2に作用する選択性より10倍左右が高くなって、他のタンパク質キナーゼ(多少のCDKsを抜く)に作用する選択性より100倍以上が高くなります。臨床1期。
ターゲット
FAK [1]
(Cell-free assay)
PYK2 [1]
(Cell-free assay)
CDK2/CyclinE [1]
(Cell-free assay)
CDK3/CyclinE [1]
(Cell-free assay)
CDK1/CyclinB [1]
(Cell-free assay)
1.5 nM 13 nM 30 nM 47 nM 58 nM
体外試験

PF-562271 shows the selective inhibitory effects on FAK and Pyk2 tyrosine kinase activity with IC50 of 1.5 nM and 14 nM, respectively. And in cell-based assays, the IC50 of PF-562271 is shown to be 5 nM for FAK, which is more selective compared to other kinase targets. [1] In 2 dimensional (2D) cultures, PF-562271 results in a dose-dependent cell proliferation inhibition in FAK WT, FAK−/− and FAK kinase-deficient (KD) cells with IC50 of 3.3 μM, 2.08 μM and 2.01 μM, respectively. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV-4-11 cell NH\UTppIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mor2TY5pcWKrdHnvckBw\iCqdX3hckBOXi12LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPzZ4IN88US=> M{jyTHNCVkeHUh?=
human SW982 cell MmLuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1rtd2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d7OEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzQDJizszN MVzTRW5ITVJ?
human KM12 cell M36zbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXPJcohq[mm2aX;uJI9nKGi3bXHuJGtOOTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO4OVU4KM7:TR?= MkT0V2FPT0WU
human COLO-205 cell MmLHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFe1e4ZKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tNlA2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52OE[1PEDPxE1? NHi1PYhUSU6JRWK=
human COLO-829 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH\rTnZKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tPFI6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC55NkG3OkDPxE1? MXPTRW5ITVJ?
human MG-63 cell M4\PW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGnJVIpKdmirYnn0bY9vKG:oIHj1cYFvKE2JLU[zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE45ODZ|NzFOwG0> MX\TRW5ITVJ?
human IGROV-1 cell M2X0c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGlIWk:YLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlgyODN6IN88US=> NYfDUJpFW0GQR1XS
human NCI-H650 cell M1[0dmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHm2UHFKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IOlUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC56M{G1OEDPxE1? MoH2V2FPT0WU
human RT-112 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{L0dGlvcGmkaYTpc44hd2ZiaIXtZY4hWlRvMUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE46QDR4IN88US=> MVrTRW5ITVJ?
human BCPAP cell NEDLdldIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoPOTY5pcWKrdHnvckBw\iCqdX3hckBDS1CDUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFEzQDhizszN M2PscXNCVkeHUh?=
ALL-PO cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFn5NFlKdmirYnn0bY9vKG:oIHj1cYFvKEGOTD3QU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvODF3OESg{txO MYjTRW5ITVJ?
human KYSE-270 cell NEDF[4pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWrJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvMkewJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4xPDdzNDFOwG0> MV;TRW5ITVJ?
human 8305C cell NIX4OHBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXXxPYR7UW6qaXLpeIlwdiCxZjDoeY1idiB6M{C1R{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvODl7MESg{txO M2TufHNCVkeHUh?=
NCI-H810 cell M4HlXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXzJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KOEGwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4yODd5NjFOwG0> NU\5dW1{W0GQR1XS
human CAL-33 cell MlexS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4PBbWlvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLUOzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4yOjl|ODFOwG0> MmfMV2FPT0WU
human AN3-CA cell NH7id5FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUTJcohq[mm2aX;uJI9nKGi3bXHuJGFPOy2FQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNlE5PjdizszN MlTvV2FPT0WU
human NKM-1 cell NUHXeZo5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1;aOmlvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlI4PTB4IN88US=> NGTwd|lUSU6JRWK=
human BPH-1 cell NYrsTmZyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2PPPGlvcGmkaYTpc44hd2ZiaIXtZY4hSlCKLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlI5PzZ4IN88US=> NFOwU41USU6JRWK=
human MES-SA cell M4LteGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHzy[WxKdmirYnn0bY9vKG:oIHj1cYFvKE2HUz3TRUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzB4OEKg{txO NFi5NmRUSU6JRWK=
human CAL-62 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWjJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC14MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|E6ODlizszN MV\TRW5ITVJ?
human KYSE-150 cell NYP4Z25UT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUnJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvMUWwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{PTJ|NjFOwG0> MmSyV2FPT0WU
human SK-UT-1 cell Mon2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYHJcohq[mm2aX;uJI9nKGi3bXHuJHNMNVWWLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlQ1PjR5IN88US=> MX;TRW5ITVJ?
human HUTU-80 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF7vbI5KdmirYnn0bY9vKG:oIHj1cYFvKEiXVGWtPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjR2OEi2JO69VQ>? MnT3V2FPT0WU
human SIG-M5 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVz0PItzUW6qaXLpeIlwdiCxZjDoeY1idiCVSVetUVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjR6NEi3JO69VQ>? M2\mXHNCVkeHUh?=
human AGS cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV72eYFDUW6qaXLpeIlwdiCxZjDoeY1idiCDR2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlUzOTJ2IN88US=> MVPTRW5ITVJ?
human ST486 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnjGTY5pcWKrdHnvckBw\iCqdX3hckBUXDR6NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVMzPzhizszN NF;uSYtUSU6JRWK=
human HSC-2 cell NFy0dIhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIToU4NKdmirYnn0bY9vKG:oIHj1cYFvKEiVQz2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42Ozl3IN88US=> Ml;PV2FPT0WU
human BC-1 cell NFHRXGtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUTJcohq[mm2aX;uJI9nKGi3bXHuJGJENTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLk[xOlY1KM7:TR?= MofGV2FPT0WU
human CGTH-W-1 cell NWHoSmh{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn;6TY5pcWKrdHnvckBw\iCqdX3hckBET1SKLWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjF4N{mg{txO MXHTRW5ITVJ?
human MZ1-PC cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmLsTY5pcWKrdHnvckBw\iCqdX3hckBOYjFvUFOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlYzOzF{IN88US=> MVzTRW5ITVJ?
human SW1710 cell M4rrN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX\Jcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlI3OjhizszN NHHNSI1USU6JRWK=
human EW-13 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWDhPZplUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjN2Nk[g{txO MXXTRW5ITVJ?
human U251 cell NHLKfXhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX\UZ5B[UW6qaXLpeIlwdiCxZjDoeY1idiCXMkWxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44PDB|MTFOwG0> MYXTRW5ITVJ?
human NCI-H460 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYfJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KNE[wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4xPDh|OTFOwG0> NEGwOVNUSU6JRWK=
human DU-4475 cell NYOxZXhZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnG2TY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4yPDd3OTFOwG0> NFvIVIhUSU6JRWK=
human MFE-296 cell NVrZcnpPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MljJTY5pcWKrdHnvckBw\iCqdX3hckBOTkVvMkm2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk41Pzd7MjFOwG0> NYO5S4RZW0GQR1XS
human DU-145 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEDk[5FKdmirYnn0bY9vKG:oIHj1cYFvKESXLUG0OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPDlzMUig{txO NX3nU5F6W0GQR1XS
human MDA-MB-231 cell NWX4enlxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVvwd|ZrUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOjNzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj60PVU4OiEQvF2= M1jafHNCVkeHUh?=
human SNU-387 cell MmqxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV3oN|d5UW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtN|g4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi53MkiyJO69VQ>? Mnq1V2FPT0WU

多くの細胞株試験データを見る場合、クリックしてください

体内試験 In several human s.c. xenograft models, PF-562271 exhibits dose-dependent tumor growth inhibition, and produces maximum tumor inhibition for PC-3M, BT474, BxPc3, and LoVo ranging from 78% to 94% inhibition at doses of 25 to 50 mg/kg twice daily, without weight loss, morbidity, or death. [1] PF-562271 (25 mg/kg by p.o.) leads to a significant decrease in tumor progression in both subcutaneous and bone metastasis PC3M-luc-C6 xenograft models. [3] In a Huh7.5 hepatocellular carcinoma xenograft model, combination therapy of sunitinib and PF-562271 targets angiogenesis and tumor aggressiveness, and produces more significant anti-tumor effect than single agent by blocking tumor growth and impacting the ability of the tumor to recover upon withdrawal of the therapy. [4]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

Recombinant kinase assay and enzyme kinetics :

Briefly, purified-activated FAK kinase domain (amino acid 410–689) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, and 48 mM MgCl2] for 15 minutes. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted PF-562271 at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2 M H2SO4). IC50 values are determined using the Hill-Slope Model. Broad kinase selectivity profiling is performed in house and by using the KinaseProfiler Selectivity Screening Service available through UpState Biotechnology.
細胞試験: [2]
+ 展開
  • 細胞株: Squamous cell carcinoma (SCC)
  • 濃度: 0 to 1 μM
  • 反応時間: 72 hours
  • 実験の流れ: Cells are plated for 48 hours before addition of PF-562271. After 3 days cells are fixed by addition of ice cold 25% trichloroacetic acid (TCA) solution prior to staining with Sulforhodamine B (SRB) dye solution. Plates are washed with 1% glacial acetic acid, air-dried and resuspended in 10 mM Tris buffer, pH 10.5 before reading absorbance at 540 nm. Curve fitting and generation of IC50 values is carried out using GraphPad Prism 4 software from six replicates.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: PC-3M, BT474, BxPc3, LoVo, U87MG, H125 and H460 cells are injected s.c. into the right flank of athymic female mice .
  • 製剤: PF-562271 is dissolved in 5% Gelucire.
  • 投薬量: ≤100 mg/kg
  • 投与方法: Administered via p.o.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 14 mg/mL (21.03 mM) warming
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
4% DMSO+30% PEG 300+ddH2O
3mg/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 665.66
化学式

C21H20F3N7O3S.C6H6O3S

CAS No. 939791-38-5
保管
別名 PF-562271 Besylate

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
NCT00666926 Completed Head and Neck Neoplasm|Prostatic Neoplasm|Pancreatic Neoplasm Verastem, Inc. December 2005 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

よくある質問(FAQ)

  • 問題1:

    What’s the difference between S2890 and S2672?

  • 回答:

    S2890 is free base and S2672 is the besylate salt, S2672 has better solubility than S2890.

  • 問題2:

    We are planning both in vitro and in vivo experiments and want to know how to reconstitute the drug for these purposes?

  • 回答:

    PF-00562271 has poor solubility in DMSO and water. Its solubility in DMSO is only 0.4mg/ml. In a previous literature report (http://www.ncbi.nlm.nih.gov/pubmed/18339875), the author used 5% Gelucire to formulate the compound. You can also consider other co-solvents such as PEG400, CMC, Tween80, and Captisol.

  • 問題3:

    Can you provide with a few common vehicles for PF-00562271, S2672 for use as oral gavage?

  • 回答:

    S2672 PF-00562271 can be dissolved in 0.5% CMC Na at 30 mg/ml as a suspension. If 4% DMSO can be used in your experiment, it will help dissolving the suspension more homogeneously.

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