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：

  • 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.

  • 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.

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 M1[x[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWq0VmJxUUN3ME2wMlI4PjZizszN NVz2RoFpW0GQR1XS
SW982 Mn;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTBwM{K4NkDPxE1? NF;sUW9USU6JRWK=
KM12 MoLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV6xWJI6UUN3ME2wMlM5PTV5IN88US=> NInweIlUSU6JRWK=
COLO-205 M3i3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwNEi2OVgh|ryP NXP3R5ZVW0GQR1XS
COLO-829 M2fubmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vPSmlEPTB;MD63OVE4PiEQvF2= NHTzdJVUSU6JRWK=
MG-63 NYTiR5FpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfVTWM2OD1yLkiwOlM4KM7:TR?= MnPQV2FPT0WU
IGROV-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MormTWM2OD1yLkixNFM5KM7:TR?= NYjPUpVoW0GQR1XS
NCI-H650 NX3kbllYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTBwOEOxOVQh|ryP M4DURXNCVkeHUh?=
RT-112 M1jPPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoL0TWM2OD1yLkm4OFYh|ryP M2\GOXNCVkeHUh?=
BCPAP NIeweXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPte5prUUN3ME2xMlAyOjh6IN88US=> MnLWV2FPT0WU
ALL-PO NVjYW4F[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7DTIlKSzVyPUGuNFE2QDRizszN M3G5OHNCVkeHUh?=
KYSE-270 Mn[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnO4TWM2OD1zLkC0O|E1KM7:TR?= M175VnNCVkeHUh?=
8305C NHLafIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\sNZVKUUN3ME2xMlA6QTB2IN88US=> MYjTRW5ITVJ?
NCI-H810 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTFwMUC3O|Yh|ryP NHvLZXZUSU6JRWK=
CAL-33 NEHheZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTjPZZKSzVyPUGuNVI6OzhizszN M1LZfnNCVkeHUh?=
AN3-CA M3q5RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnj3TWM2OD1zLkKxPFY4KM7:TR?= MlTTV2FPT0WU
NKM-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTFwMke1NFYh|ryP MnfhV2FPT0WU
BPH-1 M3zuTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTFwMki3OlYh|ryP NYnwe5Q4W0GQR1XS
MES-SA NVn4XW9iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjOV3dKSzVyPUGuN|A3QDJizszN M{XpS3NCVkeHUh?=
CAL-62 NFfsR29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1L2TmlEPTB;MT6zNVkxQSEQvF2= NWD2Z202W0GQR1XS
Detroit562 M2XDcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTFwM{WyNlIh|ryP M4jKPHNCVkeHUh?=
KYSE-150 MnzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjVUXlUUUN3ME2xMlM2OjN4IN88US=> MWnTRW5ITVJ?
SK-UT-1 NGHCdllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXUTWM2OD1zLkS0OlQ4KM7:TR?= M2XSb3NCVkeHUh?=
HUTU-80 M4mzd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFG4dJpKSzVyPUGuOFQ5QDZizszN MWjTRW5ITVJ?
SIG-M5 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XMbWlEPTB;MT60PFM5PyEQvF2= M2fWTXNCVkeHUh?=
AGS M2P4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfLUnlKSzVyPUGuOVIyOjRizszN NXfVVYVsW0GQR1XS
ST486 NYDrT2x3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTFwNUOyO|gh|ryP MYrTRW5ITVJ?
HSC-2 NVnXTWJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDKTWM2OD1zLkWzPVUh|ryP M2W4TnNCVkeHUh?=
LCLC-103H M3;X[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTFwNUW4NVgh|ryP MnvRV2FPT0WU
BC-1 Mnz6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTFwNkG2OlQh|ryP NGG2TpZUSU6JRWK=
CGTH-W-1 NIXDVZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LUWWlEPTB;MT62NVY4QSEQvF2= MV7TRW5ITVJ?
MZ1-PC MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTFwNkKzNVIh|ryP NGP1WJdUSU6JRWK=
SW1710 NWLQdnJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HOeWlEPTB;MT62NlYzQCEQvF2= MVrTRW5ITVJ?
EW-13 NUfrNVlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HhSGlEPTB;MT62N|Q3PiEQvF2= MmPaV2FPT0WU
TE-11 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\ubWlEPTB;MT62N|UzOiEQvF2= MkTvV2FPT0WU
BHY NYmwO2ZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTFwNkW2OlMh|ryP MWTTRW5ITVJ?
ML-2 NUjFNGlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTxTWM2OD1zLk[2PFAzKM7:TR?= M2HJTHNCVkeHUh?=
MEL-JUSO M3T5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTFwN{K4PVEh|ryP NF3KPXFUSU6JRWK=
U251 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrib4txUUN3ME2xMlc1ODNzIN88US=> NF\w[4dUSU6JRWK=
MHH-ES-1 NHOzeJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPwS5ljUUN3ME2xMlc6PTZ6IN88US=> NYDYZ2U6W0GQR1XS
CAL-85-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnQUWpKSzVyPUGuPFA1QSEQvF2= MVrTRW5ITVJ?
D-336MG MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fQ[WlEPTB;MT64OVYyPCEQvF2= MnvaV2FPT0WU
VA-ES-BJ M2jMZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LHTWlEPTB;MT65NFMyPSEQvF2= M3TvPHNCVkeHUh?=
MDA-MB-468 M2frTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTFwOUGyO|Ih|ryP MVLTRW5ITVJ?
MEL-HO MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2S1NGlEPTB;MT65O|k6OyEQvF2= MoHWV2FPT0WU
SW954 NX;1OJpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTJwMECxOVEh|ryP M4rkVXNCVkeHUh?=
LB831-BLC NULO[lhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTDTWM2OD1{LkCwPVg5KM7:TR?= NHHSWnVUSU6JRWK=
EW-16 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjYfHVKSzVyPUKuNFM6QDNizszN MmLJV2FPT0WU
NCI-H460 MoH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlezTWM2OD1{LkC0PFM6KM7:TR?= M2PrV3NCVkeHUh?=
CHP-212 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M373WmlEPTB;Mj6wPVU{QSEQvF2= NFzFSIZUSU6JRWK=
MHH-NB-11 NETqbGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTTcm9KSzVyPUKuNVI5OThizszN Mmn1V2FPT0WU
DU-4475 NH6zWY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDYNlh6UUN3ME2yMlE1PzV7IN88US=> M1\OXnNCVkeHUh?=
ABC-1 NXLncZpFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXTXpJ4UUN3ME2yMlI2OTl4IN88US=> NIPwT5FUSU6JRWK=
LOUCY M2TwU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rhUmlEPTB;Mj6yOlEzQCEQvF2= MWPTRW5ITVJ?
LC-2-ad NF35UGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHi2Uo1KSzVyPUKuNlY6PjZizszN Mn75V2FPT0WU
ETK-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XJcmlEPTB;Mj6yPFQ3KM7:TR?= MoHNV2FPT0WU
KYSE-180 MnTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3OTWM2OD1{LkK4PFc1KM7:TR?= NGjqO|dUSU6JRWK=
HOP-92 NH3qZWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jFWGlEPTB;Mj6zNFY4OyEQvF2= MXrTRW5ITVJ?
RCC10RGB NUnINY9ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DkeGlEPTB;Mj6zNlUxPyEQvF2= M4j3dHNCVkeHUh?=
KASUMI-1 MkX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\PTWM2OD1{LkOyPFgh|ryP NHTsN|JUSU6JRWK=
ACN MnX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELEPHdKSzVyPUKuN|Q4PDVizszN MmP0V2FPT0WU
BxPC-3 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLSTWM2OD1{LkO1OFM3KM7:TR?= MkPhV2FPT0WU
MONO-MAC-6 NYGyToVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TzW2lEPTB;Mj60NVI1QCEQvF2= NFm0cFZUSU6JRWK=
CAL-39 NYHycYRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnlTWM2OD1{LkSxOlI5KM7:TR?= MoPGV2FPT0WU
CMK M4H4OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrJ[IpKSzVyPUKuOFE4QTVizszN NYfObIl2W0GQR1XS
MFE-296 NFO3ToNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkGxTWM2OD1{LkS3O|kzKM7:TR?= MXzTRW5ITVJ?
DU-145 NFTqeVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDKdVNQUUN3ME2yMlQ6OTF6IN88US=> M1HWTnNCVkeHUh?=
MDA-MB-231 NUKzOppbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TBRWlEPTB;Mj60PVU4OiEQvF2= NWn0dnJKW0GQR1XS
EFO-27 NYXvcnVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTab4lKSzVyPUKuOVE5QDhizszN NH\KVHpUSU6JRWK=
SNU-387 NXn0PZoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnwO3BKSzVyPUKuOVI5OiEQvF2= NEPmblJUSU6JRWK=
KYSE-410 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTJwNU[1NVch|ryP NXzU[|YzW0GQR1XS
NCCIT MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\oemFKSzVyPUKuOVczPCEQvF2= MlnaV2FPT0WU
LXF-289 MnLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnMTHlHUUN3ME2yMlU5Ojd|IN88US=> MWDTRW5ITVJ?
HMV-II Ml7OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\WU|RYUUN3ME2yMlU5QTl5IN88US=> M4DKTXNCVkeHUh?=
MOLT-4 MoLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLhPVAzUUN3ME2yMlYxPzF{IN88US=> NWnudW5oW0GQR1XS
KOSC-2 NVzoZ4h7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HKVmlEPTB;Mj62N|g4QSEQvF2= MnHxV2FPT0WU
TUR M{\VfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfnTWM2OD1{Lk[1N|Y6KM7:TR?= MXnTRW5ITVJ?
NCI-H2087 MmXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXmdpcxUUN3ME2yMlcyPjR4IN88US=> MXHTRW5ITVJ?
SCC-15 M3iwPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33YTGlEPTB;Mj63OVI2OiEQvF2= MV;TRW5ITVJ?
HSC-4 MlrDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4P1[2lEPTB;Mj63PFM5QSEQvF2= NHz5U4lUSU6JRWK=
G-402 M4nzXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHFTWM2OD1{LkixOFQ4KM7:TR?= NGHFNppUSU6JRWK=
GP5d Mo\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJwOEO4Nlch|ryP M37RTHNCVkeHUh?=
IGR-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPITWM2OD1{LkizPVg4KM7:TR?= NYPUS2kxW0GQR1XS
SK-PN-DW NHr5emNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLkTWM2OD1{Lki2NlA1KM7:TR?= M3:0d3NCVkeHUh?=
OPM-2 MkXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4ryZWlEPTB;Mj64PVk4QCEQvF2= NF:5UHBUSU6JRWK=
5637 NEPBTGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1uyVWlEPTB;Mj65NlQ{QSEQvF2= NXnPfJZwW0GQR1XS
NCI-H2030 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDVUm5WUUN3ME2yMlk5ODJ7IN88US=> M{PQN3NCVkeHUh?=
SK-LU-1 M4rrRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYX3TlBDUUN3ME2yMlk5OzN2IN88US=> MofJV2FPT0WU
EW-18 MoHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTNwMEWzNkDPxE1? NE\TZWdUSU6JRWK=
786-0 M16xPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rEe2lEPTB;Mz6wOVc5PCEQvF2= MVzTRW5ITVJ?
NCI-H1963 M3\2dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjpfnVKSzVyPUOuNFg5OjVizszN NFLmRVNUSU6JRWK=
A2780 M3TPU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLZTWM2OD1|LkGwN|QyKM7:TR?= NI\3W|RUSU6JRWK=
NCI-H526 MlWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjlVJpCUUN3ME2zMlE{QTZzIN88US=> MYTTRW5ITVJ?
BHT-101 Ml\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorTTWM2OD1|LkG1O|k5KM7:TR?= MWDTRW5ITVJ?
RPMI-7951 NIDsWYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkCyTWM2OD1|LkKwNVM4KM7:TR?= MnTSV2FPT0WU
HL-60 NV3BfXpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGG4PWRKSzVyPUOuNlEyPCEQvF2= MY\TRW5ITVJ?
CTV-1 NHezbmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2L4WWlEPTB;Mz6yOVM4PyEQvF2= Ml;2V2FPT0WU
IST-SL1 M2nzZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[zTWM2OD1|LkK5OFY2KM7:TR?= M3;NfHNCVkeHUh?=
G-401 NIiwd4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;rb3YzUUN3ME2zMlI6QDB6IN88US=> M1vDNHNCVkeHUh?=
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LB2241-RCC M1q5fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPnU|dwUUN3ME2xN{4yPDZ7IN88US=> NHTQOVhUSU6JRWK=
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RPMI-8402 MojnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M376cmlEPTB;MUOuOVA{OSEQvF2= Mn;EV2FPT0WU
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NCI-H2405 NFHwWINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjIclJsUUN3ME2xOk4zOjF6IN88US=> NILYOGZUSU6JRWK=
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MN-60 NE\qOJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYO2VmlKUUN3ME2xO{44QTN4IN88US=> Mn\CV2FPT0WU
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TE-8 NEPPOXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHxXmJQUUN3ME2xPE4xPjZ7IN88US=> MVzTRW5ITVJ?
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HCC1187 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;QNJBqUUN3ME2xPU4yPzl4IN88US=> NEj4WmhUSU6JRWK=
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NCI-H524 MnjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHiRpBUUUN3ME2xPU42PzJ3IN88US=> MXrTRW5ITVJ?
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SW1573 M1rxTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHocYFPUUN3ME2yN{4xPjR4IN88US=> NX;TXWdWW0GQR1XS
RO82-W-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjRU|FPUUN3ME2yN{4zPTFzIN88US=> NYnofIE5W0GQR1XS
SKG-IIIa NHH2NHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHaSm5XUUN3ME2yN{4{PTR4IN88US=> NXLOfldpW0GQR1XS
MC-CAR MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWGxSnd[UUN3ME2yN{42OTh|IN88US=> MlvKV2FPT0WU
NCI-H446 MmPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHMTWM2OD1{Mz62NFk{KM7:TR?= MoP0V2FPT0WU
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TGBC1TKB MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUD0PYllUUN3ME2yN{44PDZzIN88US=> MVPTRW5ITVJ?
EFM-19 NVrJSFRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPxSo1FUUN3ME2yOE4yQDR2IN88US=> NYO5[JhDW0GQR1XS
SK-N-DZ M1:zXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;sPWVKSzVyPUK0MlQ6PzdizszN NY[5RlNNW0GQR1XS
NCI-H661 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DVVGlEPTB;MkSuOVIyPyEQvF2= MnfxV2FPT0WU
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Ca-Ski Ml7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPrTpdFUUN3ME2yOE46OjN5IN88US=> MWTTRW5ITVJ?
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FADU M{DPRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrjOYFlUUN3ME2yOk42OTV{IN88US=> Moi2V2FPT0WU
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U-87-MG M2fZXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjWTWM2OD1{Nj61N|A2KM7:TR?= NYHrfY97W0GQR1XS
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MZ7-mel M2fJ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTJ5LkW1OFgh|ryP Mn;jV2FPT0WU
SNU-C1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTBOXV{UUN3ME2yO{43PDlzIN88US=> NVTISXVuW0GQR1XS
MDA-MB-175-VII NEHs[2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DVbWlEPTB;MkeuOlk4PSEQvF2= Mm\GV2FPT0WU
HuP-T3 NFTDV|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfWR5lUUUN3ME2yPE4xPDl3IN88US=> MX7TRW5ITVJ?
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HDLM-2 NVr4SFRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTJ6LkK0OVkh|ryP NI\vS4pUSU6JRWK=
NCI-H1651 NUPrbY1uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;hWmlEPTB;MkiuNlU6OiEQvF2= MUXTRW5ITVJ?
SK-N-AS NI\GblFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PET2lEPTB;MkiuN|E4OSEQvF2= M{C1VHNCVkeHUh?=
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NCI-H28 NVGxUVdUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\FTWM2OD1{OT6wNVIh|ryP NXXHUm94W0GQR1XS
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CAL-54 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LqcWlEPTB;MkmuOlA1PiEQvF2= M2\uXXNCVkeHUh?=
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HEC-1 NFjwOFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXv1dWZwUUN3ME2zNE4xODV|IN88US=> M1PYUnNCVkeHUh?=
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OVCAR-8 NEnpdGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTNyLk[3PVQh|ryP M2PEb3NCVkeHUh?=
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NCI-H596 MmHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvKTWM2OD1|MT6wOlIyKM7:TR?= NEizPVhUSU6JRWK=
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KYSE-70 M2XwOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1L1emlEPTB;M{GuN|AxQCEQvF2= NUjkTo5lW0GQR1XS
LAN-6 NWXpO|A5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULze49NUUN3ME2zNU41QTl{IN88US=> NUfhWWxFW0GQR1XS
NCI-H2228 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWf4dGM1UUN3ME2zNU42PjJ3IN88US=> NXrNWHVZW0GQR1XS
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EHEB Mm\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTN|LkC0PVQh|ryP NXW4SndPW0GQR1XS
NCI-H441 MnH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTN|LkKyN|Uh|ryP MYfTRW5ITVJ?
LOXIMVI MlzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIn1TXRKSzVyPUOzMlM3PzlizszN MmexV2FPT0WU
MC-IXC NI\n[3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTN|LkW2OVUh|ryP MVPTRW5ITVJ?
NCI-H522 NUHCelZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfQfWxKSzVyPUOzMlY2PCEQvF2= M2HKcnNCVkeHUh?=
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NCI-H1417 MkjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWP5fG4{UUN3ME2zN{46PTh3IN88US=> NXnhbJFSW0GQR1XS
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HC-1 MkKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTITWM2OD1|NT60NFI1KM7:TR?= MUTTRW5ITVJ?
HH NGPrPHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTN3LkSxOFEh|ryP MYLTRW5ITVJ?
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NCI-H1355 M3ThOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTN3Lke3NVgh|ryP M1rBTnNCVkeHUh?=
BV-173 NHziV4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoS4TWM2OD1|NT64NlY1KM7:TR?= MlmxV2FPT0WU
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SW1463 NILBeJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvybmh{UUN3ME2zOk43PTZ4IN88US=> NYPtO4FCW0GQR1XS
KYSE-140 MkPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\Ob4tsUUN3ME2zOk44Ojl6IN88US=> M1T2[nNCVkeHUh?=
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LNCaP-Clone-FGC NY[0bXd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrVSXZVUUN3ME2zO{4yQTB|IN88US=> MVTTRW5ITVJ?
KARPAS-422 M3HodGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17C[GlEPTB;M{euOFQ{OSEQvF2= M1XHUHNCVkeHUh?=
RCM-1 NEX0empIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3uzc2lEPTB;M{euOVM2QCEQvF2= NYDndFA6W0GQR1XS
A375 NVTFOmdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWKySmQxUUN3ME2zO{44PjR5IN88US=> M4[xWHNCVkeHUh?=
TGBC24TKB NVixfmw1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nTNWlEPTB;M{iuNFI{QSEQvF2= M1zVWHNCVkeHUh?=
MDA-MB-453 NEW4[ohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3zc|ZKSzVyPUO5MlAzOThizszN Mn[zV2FPT0WU
Capan-2 MnTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTN7LkC1NFkh|ryP M3rSWHNCVkeHUh?=
SW756 MoDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkX0TWM2OD1|OT61NFkyKM7:TR?= NV7YToJEW0GQR1XS
KU-19-19 Ml\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTN7Lk[yPFIh|ryP MYHTRW5ITVJ?
NCI-H2170 NIGyWpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3u3Z2lEPTB;M{muPVk4PyEQvF2= NX7L[5o4W0GQR1XS
COLO-678 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjENmlKSzVyPUSwMlU6PSEQvF2= Mnz4V2FPT0WU
PF-382 M1TT[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTRyLke0PFch|ryP MnizV2FPT0WU
OAW-42 M1TTNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILSbYFKSzVyPUSyMlI6PDJizszN NFuyO5NUSU6JRWK=
LB996-RCC NWrle5hDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3WeGM6UUN3ME20Nk45ODB6IN88US=> NYTheHVUW0GQR1XS
SAS NILLWGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXz[nVKSzVyPUSzMlQzQDhizszN MULTRW5ITVJ?
MRK-nu-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGj4endKSzVyPUS0Mlc1OTRizszN MVHTRW5ITVJ?
EoL-1-cell M1q4WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTR2LkmxN|Yh|ryP MYnTRW5ITVJ?
NCI-H2342 NGT2S|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTR3LkGxNVch|ryP NYfSWYdTW0GQR1XS
NCI-H1703 NEfMPHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXlN29rUUN3ME20Ok4xPTl{IN88US=> MXTTRW5ITVJ?
NCI-H187 MmTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIj6boNKSzVyPUS2MlE5PjlizszN MmXjV2FPT0WU
CP66-MEL NFH3ZW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDaNpJKSzVyPUS2MlI4QDlizszN NX3BcmRXW0GQR1XS
HCC1569 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\TTWM2OD12Nj61PVE4KM7:TR?= MWTTRW5ITVJ?
BL-70 M1KyXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLPdJRDUUN3ME20Ok44PzN5IN88US=> NVTFcoI6W0GQR1XS
Saos-2 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnXTWM2OD12Nz6zNVI{KM7:TR?= MXPTRW5ITVJ?
LC-1F NXHyWIRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTR5Lk[xNFUh|ryP MknDV2FPT0WU
KY821 M3PPTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfnZYVvUUN3ME20O{43PDN2IN88US=> NH\kWXNUSU6JRWK=
PSN1 NX34TmE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3[1XGlEPTB;NEiuNVQxOSEQvF2= M330dnNCVkeHUh?=
RT4 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3BPINUUUN3ME20PE45Ozd5IN88US=> NIjFWlhUSU6JRWK=
LS-1034 NUjRUFF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\aSoluUUN3ME20PE45QTV2IN88US=> M3ewRnNCVkeHUh?=
NCI-H1395 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTR7LkC0PVIh|ryP NH7mXWpUSU6JRWK=
EKVX MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXWdFZKSzVyPUS5MlY4OzFizszN NF73fmNUSU6JRWK=
IST-MES1 NFHVcGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHSwRlBKSzVyPUS5Mlg6PDRizszN MlXrV2FPT0WU

... 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