PF-562271

目录号：S2890

PF-562271 Chemical Structure

Molecular Weight(MW): 507.49

PF-562271是一种有效的，ATP竞争性的，可逆的FAK抑制剂，无细胞试验中IC50为1.5 nM，作用于FAK比作用于Pyk2选择性高10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。

规格 价格 库存 购买数量  
RMB 2862.96 现货
RMB 1392.84 现货
RMB 2194.82 现货
RMB 5469.68 现货
RMB 7967.47 现货
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客户使用Selleck该产品发表文献14篇：

客户使用该产品的6个实验数据：

  • VEGF and P450 enzyme production in response to FAK or Src inhibitors. MCF10A cells were cultured in LD collagen gels ?vehicle control (V), 10 uM PF-562271 FAK ATP inhibitor (PF) or Src inhibitor PP2 for 24 h. Cells were also lysed and examined for CYP1A1 or CYP4B1 by immunoblot (B and C) and densitometry (D and E). VEGF data are displayed as the mean normalized to the vehicle control, N = 6, 盨EM, *p < 0.003 vs control (A). P450 data are displayed as the mean relative to GAPDH and normalized to the control. N > 4, ±SEM, *p < 0.05 vs respective control (D and E).

    Environ Toxicol Pharmacol 2014 39(1), 114-124. PF-562271 purchased from Selleck.

  • OVISE cells were incubated for 24 hr at the indicated concentrations of the FAK inhibitors. Immunoblots were performed to assess inhibition of auto-phosphorylation by the FAK inhibitors.

    PLoS One 2014 9(2), e88587. PF-562271 purchased from Selleck.

  • Effect of matrix stiffness on the susceptibility of primary HDFs to apoptosis induced by inhibition of mechanotransduction pathways. HDFs (primary human dermal fibroblasts) were cultured on collagen-coated polyacrylamide hydrogels that recapitulated the stiffness of normal (4 kPa) or densely fibrotic (50 kPa) skin for 24 hours and treated with or without the agents indicated for an additional 48 hours. Apoptosis was assessed by annexin V staining. Data are means ± SD from three independent experiments. P value was determined by Student’s t test.

    Science, 2017, 9(420), doi: 10.1126/scitranslmed.aal3765. PF-562271 purchased from Selleck.

  • (F,G) The migration and invasion ability of 5637 and T24 cells transfected with PF-562271 and WT-METTL13 was examined. The number of cells was quantified and is shown in a column graph.

    Sci Rep, 2016, 6:19261. PF-562271 purchased from Selleck.

  • D-F. T47D cells plated as in A were treated with vehicle (−) or the FAK Y397 inhibitor, PF-562271 (+), for 1 h prior to ± PRL (4 nM) for 15 min (representative immunoblots).

    Oncotarget, 2016, 7(30):48093-48106. PF-562271 purchased from Selleck.

  • Acta Pharmacol Sin, 2018, doi:10.1038/aps.2017.189. PF-562271 purchased from Selleck.

产品安全说明书

FAK抑制剂选择性比较

生物活性

产品描述 PF-562271是一种有效的，ATP竞争性的，可逆的FAK抑制剂，无细胞试验中IC50为1.5 nM，作用于FAK比作用于Pyk2选择性高10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。
靶点
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
体外研究

PF-562271会结合到ATP与FAK结合的部位,在激酶铰链区形成抑制剂与主链原子之间的两种氢键。PF-562271在测量FAK磷酸化可诱导的基于细胞的分析中效果很好，IC50为5 nM。PF-562271 (3.3 μM)导致PC3-M细胞周期停滞在G1期[1]。在鸡胚绒毛尿囊膜实验中PF-562271 (1nM)阻断bFGF刺激的血管生成。 PF-262271 强有效的阻断血管生长但对血管渗漏没有明显影响[2]。PF-562271 (250 nM)可以完全抑制整体A431 细胞侵入胶原蛋白中[3]。
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV-4-11 Mn7DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M333eGlEPTB;MD6yO|Y3KM7:TR?= MXnTRW5ITVJ?
SW982 NYnw[3FIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTBwM{K4NkDPxE1? Ml\1V2FPT0WU
KM12 M{TYeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW[5c41KUUN3ME2wMlM5PTV5IN88US=> MXTTRW5ITVJ?
COLO-205 NHXqXW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrlcotKSzVyPUCuOFg3PThizszN NVf1bZNRW0GQR1XS
COLO-829 NVPzNGtjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[0TWM2OD1yLke1NVc3KM7:TR?= M37XNXNCVkeHUh?=
MG-63 NUnXW21CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkn5TWM2OD1yLkiwOlM4KM7:TR?= Mne5V2FPT0WU
IGROV-1 M1zzdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvWXoVKSzVyPUCuPFExOzhizszN M4ruTnNCVkeHUh?=
NCI-H650 MlrxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHQTWM2OD1yLkizNVU1KM7:TR?= NELCPY5USU6JRWK=
RT-112 NXnoVHpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Hwe2lEPTB;MD65PFQ3KM7:TR?= M3\4enNCVkeHUh?=
BCPAP MnO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGe1PXhKSzVyPUGuNFEzQDhizszN MXnTRW5ITVJ?
ALL-PO MlrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTFwMEG1PFQh|ryP NFT2PGhUSU6JRWK=
KYSE-270 M3\IO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\FeZBXUUN3ME2xMlA1PzF2IN88US=> MVvTRW5ITVJ?
8305C NGfkZZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTFwMEm5NFQh|ryP M4TweXNCVkeHUh?=
NCI-H810 NEO4eFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLtfHRKSzVyPUGuNVA4PzZizszN MUnTRW5ITVJ?
CAL-33 Mli3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkj5TWM2OD1zLkGyPVM5KM7:TR?= Mo\kV2FPT0WU
AN3-CA MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHIbZNKSzVyPUGuNlE5PjdizszN MVzTRW5ITVJ?
NKM-1 M362eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPBTWM2OD1zLkK3OVA3KM7:TR?= M2TWNHNCVkeHUh?=
BPH-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTFwMki3OlYh|ryP M2j1bnNCVkeHUh?=
MES-SA MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn0dXlKSzVyPUGuN|A3QDJizszN NGX2XGJUSU6JRWK=
CAL-62 NVXxbnZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrFUlhKSzVyPUGuN|E6ODlizszN NXfzdVN2W0GQR1XS
Detroit562 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTFwM{WyNlIh|ryP MVnTRW5ITVJ?
KYSE-150 Ml3MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGniXmhKSzVyPUGuN|UzOzZizszN NIXabpRUSU6JRWK=
SK-UT-1 M2W0OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2K0TmlEPTB;MT60OFY1PyEQvF2= NEjpZZhUSU6JRWK=
HUTU-80 M1HlWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTFwNES4PFYh|ryP M1fySHNCVkeHUh?=
SIG-M5 NUDvflJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTFwNEizPFch|ryP NUfEW49RW0GQR1XS
AGS M4fKR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fRSmlEPTB;MT61NlEzPCEQvF2= MWDTRW5ITVJ?
ST486 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfYVJVKSzVyPUGuOVMzPzhizszN NIexOG1USU6JRWK=
HSC-2 NXTHdZF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTFwNUO5OUDPxE1? MnvuV2FPT0WU
LCLC-103H M4Hudmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjZTWM2OD1zLkW1PFE5KM7:TR?= NELXPGtUSU6JRWK=
BC-1 M{SyZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEG0dXpKSzVyPUGuOlE3PjRizszN M{T0TXNCVkeHUh?=
CGTH-W-1 MkLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTFwNkG2O|kh|ryP MUDTRW5ITVJ?
MZ1-PC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\adJRKSzVyPUGuOlI{OTJizszN MorYV2FPT0WU
SW1710 M1PvOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rmXGlEPTB;MT62NlYzQCEQvF2= NGfVRnBUSU6JRWK=
EW-13 NHzCdIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTQTWM2OD1zLk[zOFY3KM7:TR?= MoHvV2FPT0WU
TE-11 NGXROI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTCdnlSUUN3ME2xMlY{PTJ{IN88US=> M{fBU3NCVkeHUh?=
BHY NFLEfVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTsTWM2OD1zLk[1OlY{KM7:TR?= NGrTN2xUSU6JRWK=
ML-2 M1XwRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTFwNk[4NFIh|ryP NVzNR|dWW0GQR1XS
MEL-JUSO MlruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjVbZFKSzVyPUGuO|I5QTFizszN Mlz5V2FPT0WU
U251 NXLORoFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrUTWM2OD1zLke0NFMyKM7:TR?= M2DXPXNCVkeHUh?=
MHH-ES-1 MlnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnCTWM2OD1zLke5OVY5KM7:TR?= NWLCTJhGW0GQR1XS
CAL-85-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPkVVRCUUN3ME2xMlgxPDlizszN NGiyZZNUSU6JRWK=
D-336MG MnvPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33XRWlEPTB;MT64OVYyPCEQvF2= Ml6zV2FPT0WU
VA-ES-BJ Mn3YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrCPI5jUUN3ME2xMlkxOzF3IN88US=> NUDMVFBkW0GQR1XS
MDA-MB-468 MoLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTFwOUGyO|Ih|ryP NVPxV2xxW0GQR1XS
MEL-HO MlroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTublA5UUN3ME2xMlk4QTl|IN88US=> NG\4bYZUSU6JRWK=
SW954 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTaSmRvUUN3ME2yMlAxOTVzIN88US=> M2PXWXNCVkeHUh?=
LB831-BLC NGnDW3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXWTWM2OD1{LkCwPVg5KM7:TR?= M2XEc3NCVkeHUh?=
EW-16 MkC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnj3TWM2OD1{LkCzPVg{KM7:TR?= MkLCV2FPT0WU
NCI-H460 NYXZPWZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXUWldKSzVyPUKuNFQ5OzlizszN MYjTRW5ITVJ?
CHP-212 MlrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTJwMEm1N|kh|ryP NWK5T496W0GQR1XS
MHH-NB-11 Mom0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJwMUK4NVgh|ryP NIrpd2FUSU6JRWK=
DU-4475 NFLQSVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVz0XmFFUUN3ME2yMlE1PzV7IN88US=> M3vYbXNCVkeHUh?=
ABC-1 M17BUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;ubnJKSzVyPUKuNlUyQTZizszN NIXONYJUSU6JRWK=
LOUCY NY[2dIJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYT6OGw6UUN3ME2yMlI3OTJ6IN88US=> M4nPTHNCVkeHUh?=
LC-2-ad MlT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTJwMk[5OlYh|ryP NYra[lE4W0GQR1XS
ETK-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV61dZR[UUN3ME2yMlI5PDZizszN NFPZZWJUSU6JRWK=
KYSE-180 NXzXN4dHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPqWFdsUUN3ME2yMlI5QDd2IN88US=> MYHTRW5ITVJ?
HOP-92 NEfsbG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTJwM{C2O|Mh|ryP M1mxPHNCVkeHUh?=
RCC10RGB MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPnWVc2UUN3ME2yMlMzPTB5IN88US=> MVzTRW5ITVJ?
KASUMI-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTJwM{K4PEDPxE1? MmDjV2FPT0WU
ACN M3fNOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XhUWlEPTB;Mj6zOFc1PSEQvF2= NWfX[oFXW0GQR1XS
BxPC-3 MmfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjXSnBKSzVyPUKuN|U1OzZizszN NF\lSYRUSU6JRWK=
MONO-MAC-6 NIXkTopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfx[lhRUUN3ME2yMlQyOjR6IN88US=> MnrXV2FPT0WU
CAL-39 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXSx[5hSUUN3ME2yMlQyPjJ6IN88US=> MkDDV2FPT0WU
CMK NWnrcHR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTJwNEG3PVUh|ryP MVrTRW5ITVJ?
MFE-296 NWXt[oQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTTTWM2OD1{LkS3O|kzKM7:TR?= M2XuZ3NCVkeHUh?=
DU-145 NWDhXnkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7RTWM2OD1{LkS5NVE5KM7:TR?= M4D2enNCVkeHUh?=
MDA-MB-231 NWj0[nFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTJwNEm1O|Ih|ryP MlnsV2FPT0WU
EFO-27 M1HIUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[3e5VEUUN3ME2yMlUyQDh6IN88US=> Mk[xV2FPT0WU
SNU-387 MmS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4r0WmlEPTB;Mj61NlgzKM7:TR?= NX3MVXo4W0GQR1XS
KYSE-410 NHTFW5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGG3dFdKSzVyPUKuOVY2OTdizszN MlH1V2FPT0WU
NCCIT Mlm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEP1WllKSzVyPUKuOVczPCEQvF2= NGn2eHNUSU6JRWK=
LXF-289 NXfSbod3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTJwNUiyO|Mh|ryP NGe5OFNUSU6JRWK=
HMV-II MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTJwNUi5PVch|ryP NUTHcpFTW0GQR1XS
MOLT-4 M3G4eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Lk[2lEPTB;Mj62NFcyOiEQvF2= NXzHRpB[W0GQR1XS
KOSC-2 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rzN2lEPTB;Mj62N|g4QSEQvF2= NXPiS3NjW0GQR1XS
TUR MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljFTWM2OD1{Lk[1N|Y6KM7:TR?= Ml3kV2FPT0WU
NCI-H2087 NY\1NJJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTJwN{G2OFYh|ryP MV7TRW5ITVJ?
SCC-15 NXH1d2NuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXITWM2OD1{Lke1NlUzKM7:TR?= MVnTRW5ITVJ?
HSC-4 NFTvfFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPJNVBJUUN3ME2yMlc5Ozh7IN88US=> NGHaXmdUSU6JRWK=
G-402 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfTVJBiUUN3ME2yMlgyPDR5IN88US=> NYTObJJqW0GQR1XS
GP5d NUPRZVJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfLXZpKSzVyPUKuPFM5OjdizszN NWjjOGtKW0GQR1XS
IGR-1 MnL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTJwOEO5PFch|ryP NF\uZ4hUSU6JRWK=
SK-PN-DW Mly0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTNfWJEUUN3ME2yMlg3OjB2IN88US=> NEj6RldUSU6JRWK=
OPM-2 NWrVUHk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTJwOEm5O|gh|ryP NIXQbG5USU6JRWK=
5637 NHW5PHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI[zS5ZKSzVyPUKuPVI1OzlizszN MXvTRW5ITVJ?
NCI-H2030 NX64NW5WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;uV3FJUUN3ME2yMlk5ODJ7IN88US=> NWrhWJV6W0GQR1XS
SK-LU-1 NYq0S2k3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHmTWM2OD1{Lkm4N|M1KM7:TR?= NX7LPYFFW0GQR1XS
EW-18 MoiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTNwMEWzNkDPxE1? M4WzNHNCVkeHUh?=
786-0 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELDRWxKSzVyPUOuNFU4QDRizszN NXXG[llwW0GQR1XS
NCI-H1963 MmWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPhTWM2OD1|LkC4PFI2KM7:TR?= M3fiRnNCVkeHUh?=
A2780 MkOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjE[Y1KSzVyPUOuNVA{PDFizszN MXTTRW5ITVJ?
NCI-H526 MlyxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLoXnhHUUN3ME2zMlE{QTZzIN88US=> M2S5SnNCVkeHUh?=
BHT-101 NX3tV4dpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;UU4pKSzVyPUOuNVU4QThizszN NVL1Xmh4W0GQR1XS
RPMI-7951 NF3aNoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fTcmlEPTB;Mz6yNFE{PyEQvF2= NUHnVYttW0GQR1XS
HL-60 MlH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHReW5KSzVyPUOuNlEyPCEQvF2= MoXIV2FPT0WU
CTV-1 M{HSSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrhWXVKSzVyPUOuNlU{PzdizszN NYHmcHM1W0GQR1XS
IST-SL1 NGroW3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLNb4FHUUN3ME2zMlI6PDZ3IN88US=> NH6xfGlUSU6JRWK=
G-401 M1vlTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTNwMkm4NFgh|ryP MXHTRW5ITVJ?
OVCAR-5 NELNe2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYWyU4J[UUN3ME2zMlM3OzV{IN88US=> NYe5dVhQW0GQR1XS
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A375 Ml;wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjLZ|J6UUN3ME2zO{44PjR5IN88US=> Mn\DV2FPT0WU
TGBC24TKB NWD3fG5yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTN6LkCyN|kh|ryP NXjWfI5OW0GQR1XS
MDA-MB-453 NGm3UnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XlOWlEPTB;M{muNFIyQCEQvF2= NVu1SGpkW0GQR1XS
Capan-2 NXzNOY1IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33kUmlEPTB;M{muNFUxQSEQvF2= M4DpbXNCVkeHUh?=
SW756 Mlz4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYe0OVZLUUN3ME2zPU42ODlzIN88US=> MU\TRW5ITVJ?
KU-19-19 M3LNSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU[1UJVrUUN3ME2zPU43Ojh{IN88US=> NYjq[Fg{W0GQR1XS
NCI-H2170 NIHQc4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHD[|RKSzVyPUO5Mlk6PzdizszN M3vuXnNCVkeHUh?=
COLO-678 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;CTWM2OD12MD61PVUh|ryP MV\TRW5ITVJ?
PF-382 MlLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTRyLke0PFch|ryP M2rZbHNCVkeHUh?=
OAW-42 MljLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4[yeWlEPTB;NEKuNlk1OiEQvF2= M325bHNCVkeHUh?=
LB996-RCC MljlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrsO4ZFUUN3ME20Nk45ODB6IN88US=> NXTTVGVtW0GQR1XS
SAS MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjVT3JKSzVyPUSzMlQzQDhizszN MnG4V2FPT0WU
MRK-nu-1 Mm\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvXSYZSUUN3ME20OE44PDF2IN88US=> MorPV2FPT0WU
EoL-1-cell MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTR2LkmxN|Yh|ryP NXzvOowxW0GQR1XS
NCI-H2342 NE\WdpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHwTWM2OD12NT6xNVE4KM7:TR?= NVHmW4ZWW0GQR1XS
NCI-H1703 NXHY[WttT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfYdYdOUUN3ME20Ok4xPTl{IN88US=> MX3TRW5ITVJ?
NCI-H187 NHHIV5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\NZ3dzUUN3ME20Ok4yQDZ7IN88US=> Mn7YV2FPT0WU
CP66-MEL NEDseVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjET2JVUUN3ME20Ok4zPzh7IN88US=> MmHlV2FPT0WU
HCC1569 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHvfIh[UUN3ME20Ok42QTF5IN88US=> M3\vbXNCVkeHUh?=
BL-70 MoPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4j4XGlEPTB;NE[uO|c{PyEQvF2= NUTlSYhCW0GQR1XS
Saos-2 M{DQUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTOTWM2OD12Nz6zNVI{KM7:TR?= NF\QR3NUSU6JRWK=
LC-1F NV3LRodLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvNV4VKSzVyPUS3MlYyODVizszN MXjTRW5ITVJ?
KY821 M4HYNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYP6XW86UUN3ME20O{43PDN2IN88US=> MmHtV2FPT0WU
PSN1 NXfWfmE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfZNJpIUUN3ME20PE4yPDBzIN88US=> NV;Zb5JNW0GQR1XS
RT4 Mk\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfXTWM2OD12OD64N|c4KM7:TR?= NXKzNYZxW0GQR1XS
LS-1034 NV3RT21GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Hve2lEPTB;NEiuPFk2PCEQvF2= M{TWO3NCVkeHUh?=
NCI-H1395 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTPTWVKUUN3ME20PU4xPDl{IN88US=> NUizN5ZzW0GQR1XS
EKVX MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTR7Lk[3N|Eh|ryP MmXsV2FPT0WU
IST-MES1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfic2QzUUN3ME20PU45QTR2IN88US=> NHq2eoVUSU6JRWK=

... Click to View More Cell Line Experimental Data
体内研究 在携带U87MG的小鼠中PF-562271 (< 33 mg/kg 口服)抑制肿瘤中FAK磷酸化并具有时间和剂量依赖特性。PF-562271 (50 mg/kg, 口服，一天两次)对BxPc3异种移植小鼠中肿瘤生长抑制率为86% ，对PC3-M异种移植小鼠中肿瘤生长抑制率为45%。PF-562271 (25mg/kg, 一天两次)处理的携带H125肺部异种移植肿瘤凋亡率提高2倍[1]。 PF-562271 (33 mg/kg,口服)24小时后抑制小鼠中肿瘤细胞的广泛运动。PF-562271 (33 mg/kg, 口服)导致小鼠中E-cadherin动力学的改变，这与减弱的E-cadherin依赖的整体细胞运动有关 [3]。在皮下局部异种移植PC3M-luc-C6的小鼠模型中 PF-562271 (25 mg/kg, 口服，一天两次)导致肿瘤生长率62%的抑制[4]。在胫骨植入MDA-MB-231细胞的大鼠中PF-562271 (5mg/kg, 口服)导致骨钙素和松质骨参数显著而相似的增加同时导致肿瘤生长速度和骨愈合信号的下降[5]。

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验：[1]
+ 展开
  • Animal Models: 携带BxPc3或 PC3-M异种移植的无胸腺雌性小鼠
  • Formulation: 5% Gelucire
  • Dosages: 50 mg/kg
  • Administration: 填喂给药
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL warmed (197.04 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)：
30% PEG400+0.5% Tween80+5% propylene glycol 		30 mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 507.49
化学式

C21H20F3N7O3S
CAS号 717907-75-0
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项
Selleck产品目录册

FAK Signaling Pathway Map

相关FAK产品

  • PND-1186 (VS-4718) New

    PND-1186 (VS-4718)是一种可逆的选择性FAK抑制剂，IC50为1.5 nM。Phase 1。

  • PF-431396 New

    PF-431396是双PYK2/FAK抑制剂，IC50分别为11nM和2 nM。

  • Defactinib (VS-6063, PF-04554878) New

    Defactinib (VS-6063, PF-04554878)是一种选择性，且口服有效的FAK抑制剂。Phase 2。

  • PF-00562271 Besylate

    PF-00562271 Besylate是PF-562271的苯磺酸盐，是一种有效的，ATP竞争性，可逆的FAK抑制剂，IC50为1.5 nM，作用于Pyk2比作用于FAK效果低10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。Phase 1。

  • TAE226 (NVP-TAE226)

    TAE226 (NVP-TAE226)是一种有效的FAK抑制剂，IC50为5.5 nM，最有效作用于Pyk2，对InsR， IGF-1R， ALK和c-Met作用效果比其弱10到100倍左右。

  • PF-573228

    PF-573228是一种ATP竞争性的FAK抑制剂，无细胞试验中IC50为4 nM，作用于FAK比作用于Pyk2，CDK1/7 和 GSK-3β选择性高~50到250倍。

  • PF-562271 HCl

    PF-562271 HCl是PF-562271的盐酸盐形式，是一种强效的ATP竞争性的可逆的抑制剂，作用于FAK其IC50为1.5 nM。相比较FAK，对Pyk2的效果少了大约十倍，除了CDKs类的蛋白酶，PF-562271 HCl的选择性相比其他蛋白酶大大约100倍。

  • Ibrutinib (PCI-32765)

    Ibrutinib (PCI-32765)是一种有效的，高选择性的Brutons tyrosine kinase (Btk)抑制剂，无细胞试验中IC50为0.5 nM，对Bmx， CSK， FGR， BRK及HCK适度有效，对EGFR， Yes， ErbB2， JAK3等作用效果较弱。

  • Dasatinib

    Dasatinib是一种新型有效的多靶点抑制剂，作用于Abl，Src和 c-Kit，在无细胞试验中IC50分别为 <1 nM，0.8 nM 和 79 nM。

  • Saracatinib (AZD0530)

    Saracatinib (AZD0530)是一种有效的Src抑制剂，无细胞试验中IC50为2.7 nM，对c-Yes， Fyn， Lyn， Blk， Fgr和Lck也具有活性；但对Abl和EGFR (L858R和L861Q)活性较低。Phase 2/3。

    Features:Saracatinib是第一个作用于人类肿瘤组织Src通路的抑制剂。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID