AZD4547

For research use only. Not for use in humans.

目录号:S2801 别名: ABSK 091

AZD4547 Chemical Structure

CAS No. 1035270-39-3

AZD4547 (ABSK 091)是一种新型选择性的FGFR抑制剂,靶向作用于FGFR1/2/3,在无细胞试验中IC50为0.2 nM/2.5 nM/1.8 nM,对FGFR4, VEGFR2(KDR)具有微弱的作用活性,对IGFR, CDK2和p38几乎没有作用活性。Phase 2/3。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1801.43 现货
RMB 901.31 现货
RMB 1395.39 现货
RMB 4661.52 现货
RMB 7125.05 现货
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客户使用Selleck生产的AZD4547发表文献91篇:

产品安全说明书

FGFR抑制剂选择性比较

生物活性

产品描述 AZD4547 (ABSK 091)是一种新型选择性的FGFR抑制剂,靶向作用于FGFR1/2/3,在无细胞试验中IC50为0.2 nM/2.5 nM/1.8 nM,对FGFR4, VEGFR2(KDR)具有微弱的作用活性,对IGFR, CDK2和p38几乎没有作用活性。Phase 2/3。
特性 AZD4547高选择性作用于 FGFR1-3,比作用于FGFR4选择性高。AZD4547有效作用于野生型和突变型FGFR酪氨酸激酶活性。
靶点
FGFR1 [1]
(Cell-free assay)
FGFR3 [1]
(Cell-free assay)
FGFR2 [1]
(Cell-free assay)
KDR [1]
(Cell-free assay)
0.2 nM 1.8 nM 2.5 nM 24 nM
体外研究

与 FGFR1-3相比, AZD4547作用于FGFR4,活性微弱,IC50为165 nM。AZD4547 只抑制重组 VEGFR2 (KDR) 激酶活性, IC50为 24 nM,在体外选择性作用于一组多种代表性的人类激酶。0.1 μM AZD4547 作用于一系列重组激酶,包括 ALK, CHK1, EGFR, MAPK1, MEK1, p70S6K, PDGFR, PKB, Src, Tie2,和 PI3K,没有作用活性。相应地,在细胞磷酸化实验中,可观察到AZD4547 作用于FGFR1-3的选择性比作用于 FGFR4, IGFR, 和 KDR高。AZD4547在体外,只有作用于表达去调控FGFRs 如KG1a, Sum52-PE,和KMS11的肿瘤细胞,具有有效抗增殖活性,IC50 为18-281 nM,而对MCF7 及100 种以上其他肿瘤细胞无活性。AZD4547 处理人类肿瘤细胞,有效抑制FGFR 和 MAPK 磷酸化,这种作用存在剂量依赖性。AZD4547 也有效抑制FRS2 和 PLCγ磷酸化,及下游FGFR信号。另外, AZD4547作用于乳腺细胞系,MCF7和Sum52-PE 而不是KG1a和 KMS11细胞,影响AKT磷酸化。AZD4547处理Sum52-PE 和 KMS11细胞,显著诱导凋亡,作用于KG1a细胞,显著提高细胞周期在G1期停滞而不是凋亡, 而作用于MCF7细胞,对细胞周期分布和凋亡都没有作用效果。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SNU449 NIHp[5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\xO|IhcA>? NXrCe5pIUUN3ME2wMlA5OiEQvF2= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3MUOyNEc,OjZ|NUGzNlA9N2F-
SK-HEP-1 NHHacFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEX2SHI4OiCq MVzJR|UxRTBwMEi0JO69VQ>? MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3MUOyNEc,OjZ|NUGzNlA9N2F-
SNU475 NETZXoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\BVYs4OiCq NG\zUGtKSzVyPUWuOEDPxE1? NITVfFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO1NVMzOCd-Mk[zOVE{OjB:L3G+
Hep3B NUjUSIVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nNPFczKGh? NGf0ToFKSzVyPU[uOFMh|ryP MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3MUOyNEc,OjZ|NUGzNlA9N2F-
PLC/PRF5 NVvpbVd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWj0U3Q1PzJiaB?= MlPiTWM2OD14LkW1JO69VQ>? MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3MUOyNEc,OjZ|NUGzNlA9N2F-
Hur7 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDQO|IhcA>? MVfJR|UxRTdwMkWg{txO MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3MUOyNEc,OjZ|NUGzNlA9N2F-
HepG2 MlP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVK3NkBp MoTqTWM2OD16LkezJO69VQ>? NVHpRWx[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOVE{OjBpPkK2N|UyOzJyPD;hQi=>
SNU449 MXrDcI9vd2enbnnjJIF{e2G7 NVjEXYMzOSEEtV2= NVjXenN{OjRiaB?= M3vBfIRm[3KnYYPld{Bkd2yxbomg[o9zdWG2aX;uJJNq\26rZnnjZY51dHl? M4PQcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{WxN|IxLz5{NkO1NVMzODxxYU6=
SK-HEP-1 M4jwVWNtd26xZ3XubYMh[XO|YYm= NIjYdZIyKML3TR?= MoXPNlQhcA>? MXTk[YNz\WG|ZYOgZ49td267IH\vdo1ifGmxbjDzbYdvcW[rY3HueIx6 NYLqb2dlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOVE{OjBpPkK2N|UyOzJyPD;hQi=>
SNU449 NVLSd|NVTnWwY4Tpc44hSXO|YYm= NUixZ|kzOC1{IN88US=> NEHuOlY1QCCq MnK3Z4F2e2W|IHGg[IVkemWjc3Wgc4YhTlKVMv-8kGFMXCxiYX7kJGVTUyCyaH;zdIhwenmuYYTpc44> M3j0elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{WxN|IxLz5{NkO1NVMzODxxYU6=
SK-HEP-1 MWPGeY5kfGmxbjDBd5NigQ>? M1jR[VAuOiEQvF2= NFLJZlM1QCCq M2XFW4NifXOnczDhJIRm[3KnYYPlJI9nKE[UU{NvwKxCU1RuIHHu[EBGWkticHjvd5Bpd3K7bHH0bY9v M4SzVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{WxN|IxLz5{NkO1NVMzODxxYU6=
BaF3 FLT3-TEL M3XkUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[4NmtoT0l3ME20MlYhyrFiMD61O|ch|ryP MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ7NEe0NUc,OjZ{OUS3OFE9N2F-
BaF3 RET-TEL NV7xWWZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXUOpJST0l3ME2wMlM6KMLzIECuNFQ5KM7:TR?= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ7NEe0NUc,OjZ{OUS3OFE9N2F-
BaF3 Parental NFexSldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XyNWdKPTExubWxNEDPxE1? MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ7NEe0NUc,OjZ{OUS3OFE9N2F-
MOLM14 FLT3/ITD NHOwWHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XyfWdKPTB;MD60PFQhyrFiMD6xOVch|ryP MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ7NEe0NUc,OjZ{OUS3OFE9N2F-
MV4-11 FLT3/ITD MnryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Ln[GdKPTB;MD60OVkhyrFiMD6wOFYh|ryP M2LQflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mkm0O|QyLz5{NkK5OFc1OTxxYU6=
TT RET C634W NX\SenFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jE[WdKPTB;Mj65JOKyKDBwOUC0JO69VQ>? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ7NEe0NUc,OjZ{OUS3OFE9N2F-
AN3-CA FGFR2 N550K, K310R NUDOSI9iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonaS2k2OD1yLkCzNUDDuSByLkCyN{DPxE1? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ7NEe0NUc,OjZ{OUS3OFE9N2F-
MFE296 FGFR2 N550K MmHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfLR|dIUTVyPUCuO|MxKMLzIECuNFU4KM7:TR?= Ml3sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O|QyRC:jPh?=
MFE280 FGFR2 S252W NXvJR3c3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jMc2dKPTB;MD6yNVghyrFiMD6wO|Mh|ryP M1;lRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mkm0O|QyLz5{NkK5OFc1OTxxYU6=
Ishikawa FGFF2 over exp. NYXYUohvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mki2S2k2OD12LkWgxtEhOS53MTFOwG0> MnLlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O|QyRC:jPh?=
HEC1A Normal FGFR2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL3S2k2OO,7pUGwJO69VQ>? NHvLTGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK5OFc1OSd-Mk[yPVQ4PDF:L3G+
A549 MUHD[YxtKH[rYXLpcIl1gSCDc4PhfS=> MX:wMlEwOSEQvF2= NG[yN4w1QCCq M2W5WYVvcGGwY3XzJGVzdG:2aX7pZkBqdmS3Y3XkJJZq[WKrbHn0fUBtd3O| NXnXTGhJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wOVMxOjBpPkK2NFU{ODJyPD;hQi=>
SGC-7901 NEPGVJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\KXYgyKG6PLUGwJO69VQ>? NUn5OHlWPzJiaB?= MVfJR|UxKG:oIEWtNVAh|ryPLDDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NHnpTJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW3OlkyPSd-MkW1O|Y6OTV:L3G+
HGC-27 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYq0fXB1OSCwTT2xNEDPxE1? NUGxVVE6PzJiaB?= NIr3WndKSzVyIH;mJFUuOTBizszNMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M2HGZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUe2PVE2Lz5{NUW3OlkyPTxxYU6=
MKN-28 MoXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHSZVEyKG6PLUGwJO69VQ>? M2W0OFczKGh? MkHXTWM2OCCxZjC1MVExKM7:TTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NXjy[YFkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1O|Y6OTVpPkK1OVc3QTF3PD;hQi=>
NCI-N87 M{GxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXLbHEyKG6PLUGwJO69VQ>? NIL0O204OiCq MYfJR|UxKG:oIEWtNVAh|ryPLDDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M4frN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUe2PVE2Lz5{NUW3OlkyPTxxYU6=
KATOIII Mof4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:xJI5ONTFyIN88US=> M{m1SFczKGh? MUDJR|UxKG:oIEGwMVExOCCwTTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV5NkmxOUc,OjV3N{[5NVU9N2F-
SNU-16 Mof5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTKbpQyKG6PLUGwJO69VQ>? M1HWfFczKGh? MYHJR|UxKG:oIEGwMVExOCCwTTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M4\xRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUe2PVE2Lz5{NUW3OlkyPTxxYU6=
4T1 NUntUHVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTBwNkVCtVAvOTFizszN MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2Mki5N{c,OjR4NEK4PVM9N2F-
MDA-MB-468 NVS4bnB6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTRwOdMxNE45PSEQvF2= MkDVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEK4PVMoRjJ2NkSyPFk{RC:jPh?=
HCT116 NXPndVFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLBTWM2OD1zNT65xtEyNjh{IN88US=> NVLJWoFERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFI5QTNpPkK0OlQzQDl|PD;hQi=>
SW620 MnPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlOzTWM2OO,:nkKwJO69VQ>? NYrTWG1XRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFI5QTNpPkK0OlQzQDl|PD;hQi=>
MDA-MB-231 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoL0TWM2OO,:nkKwJO69VQ>? M3KyNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSyPFk{Lz5{NE[0Nlg6OzxxYU6=
CT26 M3LsXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHEeXVjUUN3MP-8olIxKM7:TR?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2Mki5N{c,OjR4NEK4PVM9N2F-
SW480 NH[zeGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|Ux97zgMkCg{txO NELoWZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0Nlg6Oyd-MkS2OFI5QTN:L3G+
4T1 M2S2XmFxd3C2b4Ppd{BCe3OjeR?= MlPzNU4zPS1{MDFOwG0> MWGyOEBp NUj0NXZmcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2Mki5N{c,OjR4NEK4PVM9N2F-
KG1a M3q5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTBwMEG4JO69VQ>? NXnWcVBkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzOlk6OjhpPkKyN|Y6QTJ6PD;hQi=>
Sum52-PE NV3YfVQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTBwMESxJO69VQ>? Mn;rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|Nkm5NlgoRjJ{M{[5PVI5RC:jPh?=
KMS11 M17vcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXJOIVUUUN3ME2wMlI5OSEQvF2= NUfVWGdMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzOlk6OjhpPkKyN|Y6QTJ6PD;hQi=>
MCF7 NEX2TIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXy3R4dxUUN3ME6zNEDPxE1? M133ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{[5PVI5Lz5{MkO2PVkzQDxxYU6=
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A673 MkjJdWhVWyC|c3H5 MUTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MoXRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 NFXwOnlyUFSVIIPzZZk> NGHHfGpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz NV\kUJAyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 MVnxTHRUKHO|YYm= NWLybJZqeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD NIPGSmRyUFSVIIPzZZk> MYPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM> NYHIWWJiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH NHXxV41yUFSVIIPzZZk> M1mwZpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz MojDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 Mn[zdWhVWyC|c3H5 NWLubIVEeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 NGPFVoRyUFSVIIPzZZk> Mn\LdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
fibroblast cells NVLz[YtNeUiWUzDzd4F6 MYTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5Ih[2:wdILvcEBJcCC5aXzkJJR6eGViZnnido9jdGG|dDDj[Yxtew>? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh41 M3vCSZFJXFNic4PhfS=> NWnjUIFneUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 NV;RNItGeUiWUzDzd4F6 M1G2[JFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEOwJINmdGy| NGrndnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 NG\zeJlyUFSVIIPzZZk> MorsdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= MoLEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 MlvFdWhVWyC|c3H5 NH7sfGFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> M3LkVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 NVqxZZFneUiWUzDzd4F6 MUPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? NUTmZZF[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18 NH\mPHhyUFSVIIPzZZk> Mmm4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-FGFR / FGFR1 / p-AKT / AKT / p-ERK / ERK; 

PubMed: 28900173     


Western blots (cropped) are shown for the indicated proteins in MDA-MB-361, BT474, and SKBR3 cells treated with AZD4547 (0, 1, 3, or 5 µM) for 72 hours. 

pFRS2; 

PubMed: 25576915     


AZD4547 inhibits FGFR2 pathway activation in SNU16 and KATOIII cells. Cells were incubated with AZD4547 at the indicated doses. Cell lysates were immunoblotted for phospho-FGFR, phospho-FRS2, phospho- and total AKT, and phospho- and total ERK.

28900173 25576915
Growth inhibition assay
Cell viability; 

PubMed: 28900173     


MDA-MB-361, BT474, and SKBR3 ErbB2-overexpressing breast cancer cells were treated with AZD4547 (0, 0.1, 0.3, 1, 3, or 5 µM) for 5 days. Then the viable fraction of each cell line was determined with an MTS assay. 

Cell viability; 

PubMed: 25576915     


FGFR2-amplified GC cells are selectively sensitive to AZD4547. In vitro CCK-8 assay across a panel of 6 GC cells demonstrated that SNU16 and KATOIII cells were extremely sensitive to AZD4547 with IC50 values of 5-10 nM. Data (n = 6) are presented as mean ± SD.

28900173 25576915
体内研究 AZD4547按3 mg/kg剂量口服处理携带KMS11肿瘤的小鼠,每天两次,与空白对照组相比,显著抑制53%肿瘤生长,AZD4547 按 12.5 mg/kg剂量每天处理一次,或按 6.25 mg/kg剂量每天处理两次,则完全抑制肿瘤,这与p-FGFR3的药效学调节剂量正相关,且降低 KMS11肿瘤细胞增殖。而且, AZD4547按 12.5 mg/kg剂量口服处理给药FGFR1融合KG1a 移植瘤模型,每天一次,抑制65% 肿瘤生长。在有效剂量水平,AZD4547不表现出抗血管生成的效果。AZD4547 对血压没有显著作用效果,因此在体内缺乏 抗-KDR 活性。相应地, AZD4547按6.25 mg/kg剂量口服处理对Cediranib敏感的移植瘤模型,包括 Calu-6, HCT-15 和 LoVo,每天两次,没有作用活性。[1]

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)

激酶实验:[1]
- 合并

AZD4547 激酶活性:

使用浓度等于或低于相对Km 的ATP,测定AZD4547抑制 FGFR1-3的人类重组激酶活性的效果。
细胞实验:[1]
- 合并
  • Cell lines: KG1a, Sum52-PE, KMS11, 和MCF7
  • Concentrations: 溶于DMSO,终浓度为 ~1 μM
  • Incubation Time: 72 小时
  • Method: 使用多种浓度AZD4547处理细胞72小时。通过 MTS 增殖实验获得抗增殖的IC50值。荧光激活细胞分选(FACS)中,细胞与70%乙醇混合,然后与碘化丙啶/RNase A标记溶液温育。使用 FACSCalibur 仪器和CellQuest分析软件测定细胞周期谱。为了分析凋亡,轻轻收集细胞和培养基,离心,然后冲洗细胞颗粒。细胞进行Annexin膜联蛋白 V-异硫氰酸荧光素(FITC)染色和碘化丙啶吸收。使用FACSCalibur仪器测定 膜联蛋白 V染色阳性细胞比例,使用CellQuest分析软件进行象限分类。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 皮下注射LoVo, HCT-15, Calu-6, KMS11 或 KG1a的雌性Swiss衍生裸鼠和SCID小鼠
  • Dosages: 1.5-50 mg/kg
  • Administration: 口服饲喂,每天一次或两次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 92 mg/mL (198.45 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):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/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 463.57
化学式

C26H33N5O3

CAS号 1035270-39-3
储存条件 粉状
溶于溶剂
别名 ABSK 091

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

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 (mg) = 浓度 (mM) x 体积 (mL) 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、SDS / 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、SDS / 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

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02824133 Completed Drug: AZD4547 Recurrent IDHwt Gliomas With FGFR3-TACC3 Fusion|Recurrent IDHwt Gliomas With FGFR1-TACC1 Fusion Assistance Publique - Hôpitaux de Paris September 2015 Phase 1|Phase 2
NCT01824901 Completed Drug: docetaxel|Drug: AZD4547 Recurrent Non-small Cell Lung Cancer|Squamous Cell Lung Cancer ECOG-ACRIN Cancer Research Group|National Cancer Institute (NCI)|Eastern Cooperative Oncology Group September 2013 Phase 1|Phase 2
NCT01795768 Unknown status Drug: AZD 4547 Gastric Cancer|Oesophageal Cancer|Breast Cancer|Squamous Cell Carcinoma of the Lung Royal Marsden NHS Foundation Trust|AstraZeneca September 2012 Phase 2
NCT01791985 Completed Drug: AZD4547 / anastrozole or letrozole Breast Cancer Imperial College London|Cancer Research UK|AstraZeneca July 2012 Phase 1|Phase 2
NCT01213160 Completed Drug: AZD4547 Cancer|Advanced Solid Malignancies AstraZeneca November 2010 Phase 1

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操作手册

如果有其他问题,请给我们留言。

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FGFR Signaling Pathway Map

FGFR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID