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80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 NVPqSJJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHBO|IhcA>? MmTFTWM2OD1yLkC4NkDPxE1? MlXDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|NUGzNlAoRjJ4M{WxN|IxRC:jPh?=
SK-HEP-1 MnTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWq3NkBp MYjJR|UxRTBwMEi0JO69VQ>? NHjBdpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO1NVMzOCd-Mk[zOVE{OjB:L3G+
SNU475 NXPuXmpsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPsTIw4OiCq NET5PW9KSzVyPUWuOEDPxE1? Mn3YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|NUGzNlAoRjJ4M{WxN|IxRC:jPh?=
Hep3B MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnuTFQ1PzJiaB?= NHzMeoVKSzVyPU[uOFMh|ryP MoDiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|NUGzNlAoRjJ4M{WxN|IxRC:jPh?=
PLC/PRF5 MkTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfVTZY4OiCq NXfkOIFpUUN3ME22MlU2KM7:TR?= NEHxdmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO1NVMzOCd-Mk[zOVE{OjB:L3G+
Hur7 NX3VcZJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXK3NkBp NFvic29KSzVyPUeuNlUh|ryP MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3MUOyNEc,OjZ|NUGzNlA9N2F-
HepG2 M2DXZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fGUFczKGh? MlLzTWM2OD16LkezJO69VQ>? MojDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|NUGzNlAoRjJ4M{WxN|IxRC:jPh?=
SNU449 MmXUR4xwdm:pZX7pZ{Bie3OjeR?= M2HXPVEhyrWP MYOyOEBp NE\ONnZl\WO{ZXHz[ZMh[2:ub375JIZwem2jdHnvckB{cWewaX\pZ4FvfGy7 M164TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{WxN|IxLz5{NkO1NVMzODxxYU6=
SK-HEP-1 NGLudVBEdG:wb3flcolkKGG|c3H5 MXmxJOK2VQ>? NIDTTHgzPCCq NUPtd|Vi\GWlcnXhd4V{KGOxbH;ufUBnd3KvYYTpc44he2mpbnnmbYNidnSueR?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3MUOyNEc,OjZ|NUGzNlA9N2F-
SNU449 M4TqNGZ2dmO2aX;uJGF{e2G7 NXrqXWJbOC1{IN88US=> MY[0PEBp NHL0d2xk[XW|ZYOgZUBl\WO{ZXHz[UBw\iCIUmOy89yNSUuWLDDhcoQhTVKNIIDoc5NxcG:{eXzheIlwdg>? NYnJPI9CRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOVE{OjBpPkK2N|UyOzJyPD;hQi=>
SK-HEP-1 NVu5flB1TnWwY4Tpc44hSXO|YYm= NWiyTGg3OC1{IN88US=> Mkn5OFghcA>? MUfjZZV{\XNiYTDk[YNz\WG|ZTDv[kBHWlN{78{MRWtVNCCjbnSgSXJMKHCqb4PwbI9zgWyjdHnvci=> NULEfm44RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOVE{OjBpPkK2N|UyOzJyPD;hQi=>
BaF3 FLT3-TEL NIniRlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrGVGRuT0l3ME20MlYhyrFiMD61O|ch|ryP Ml[3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O|QyRC:jPh?=
BaF3 RET-TEL NGPBUJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\HTVUxRTBwM{mgxtEhOC5yNEig{txO MnrMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O|QyRC:jPh?=
BaF3 Parental M2LMNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkL4S2k2OO,7pUGwJO69VQ>? NFXWeIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK5OFc1OSd-Mk[yPVQ4PDF:L3G+
MOLM14 FLT3/ITD MnnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXn2bXNtT0l3ME2wMlQ5PCEEsTCwMlE2PyEQvF2= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ7NEe0NUc,OjZ{OUS3OFE9N2F-
MV4-11 FLT3/ITD M2jpeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfOfVZDT0l3ME2wMlQ2QSEEsTCwMlA1PiEQvF2= M2q1cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mkm0O|QyLz5{NkK5OFc1OTxxYU6=
TT RET C634W MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;HTVUxRTJwOTFCtUAxNjlyNDFOwG0> NFftNlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK5OFc1OSd-Mk[yPVQ4PDF:L3G+
AN3-CA FGFR2 N550K, K310R MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXHTVUxRTBwMEOxJOKyKDBwMEKzJO69VQ>? NXj2ZWpGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPVQ4PDFpPkK2Nlk1PzRzPD;hQi=>
MFE296 FGFR2 N550K MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLaS2k2OD1yLkezNEDDuSByLkC1O{DPxE1? NWnNc2VPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPVQ4PDFpPkK2Nlk1PzRzPD;hQi=>
MFE280 FGFR2 S252W MkXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXHTVUxRTBwMkG4JOKyKDBwMEezJO69VQ>? NXvXO3FDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPVQ4PDFpPkK2Nlk1PzRzPD;hQi=>
Ishikawa FGFF2 over exp. NH;JU5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXIR4VmT0l3ME20MlUhyrFiMT61NUDPxE1? Mn;rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O|QyRC:jPh?=
HEC1A Normal FGFR2 NGPhbmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfWSZJXT0l3MP-5qVExKM7:TR?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ7NEe0NUc,OjZ{OUS3OFE9N2F-
A549 NFPrZopE\WyuII\pZYJqdGm2eTDBd5NigQ>? M3TwVlAvOS9zIN88US=> NFuxS4E1QCCq NHLR[WhmdmijbnPld{BGemyxdHnubYIhcW6mdXPl[EB3cWGkaXzpeJkhdG:|cx?= MmPsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNUOwNlAoRjJ4MEWzNFIxRC:jPh?=
SGC-7901 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLyWYhiOSCwTT2xNEDPxE1? MX:3NkBp NV3JT2tLUUN3MDDv[kA2NTFyIN88UUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M4DyT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUe2PVE2Lz5{NUW3OlkyPTxxYU6=
HGC-27 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYqxJI5ONTFyIN88US=> Ml3hO|IhcA>? MmO0TWM2OCCxZjC1MVExKM7:TTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NVj0XpRRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1O|Y6OTVpPkK1OVc3QTF3PD;hQi=>
MKN-28 Mn;uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX[2cYxLOSCwTT2xNEDPxE1? MVi3NkBp NUPrVHYzUUN3MDDv[kA2NTFyIN88UUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV5NkmxOUc,OjV3N{[5NVU9N2F-
NCI-N87 M1jVSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vuUlEhdk1vMUCg{txO MV23NkBp MX\JR|UxKG:oIEWtNVAh|ryPLDDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 Ml33QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3N{[5NVUoRjJ3NUe2PVE2RC:jPh?=
KATOIII MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{f5elEhdk1vMUCg{txO M2HneVczKGh? M{LZeGlEPTBib3[gNVAuOTByIH7NMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV5NkmxOUc,OjV3N{[5NVU9N2F-
SNU-16 NGTTU5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fnOFEhdk1vMUCg{txO NWHaOm9QPzJiaB?= M1vJXGlEPTBib3[gNVAuOTByIH7NMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NGP2Om09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW3OlkyPSd-MkW1O|Y6OTV:L3G+
4T1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvGTWM2OD1yLk[0xtExNjFzIN88US=> M1XLbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSyPFk{Lz5{NE[0Nlg6OzxxYU6=
MDA-MB-468 NIX5d4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjGTFVtUUN3ME20MlnDuTBwOEWg{txO NEm1NWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0Nlg6Oyd-MkS2OFI5QTN:L3G+
HCT116 NIjONZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTF3LkpCtVEvQDJizszN NWjCNY1nRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFI5QTNpPkK0OlQzQDl|PD;hQi=>
SW620 NVL2VJZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPKRZVbUUN3MP-8olIxKM7:TR?= NELtSXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0Nlg6Oyd-MkS2OFI5QTN:L3G+
MDA-MB-231 Mk\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LYTWlEPTExvK6yNEDPxE1? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2Mki5N{c,OjR4NEK4PVM9N2F-
CT26 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|Ux97zgMkCg{txO Mn7QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEK4PVMoRjJ2NkSyPFk{RC:jPh?=
SW480 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVX5NVdUUUN3MP-8olIxKM7:TR?= MlX6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEK4PVMoRjJ2NkSyPFk{RC:jPh?=
4T1 M2f6XmFxd3C2b4Ppd{BCe3OjeR?= NUj0cmV1OS5{NT2yNEDPxE1? NIT1c4gzPCCq M2DBcolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MkO0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEK4PVMoRjJ2NkSyPFk{RC:jPh?=
KG1a MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTBwMEG4JO69VQ>? NGTv[ZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkO2PVkzQCd-MkKzOlk6Ojh:L3G+
Sum52-PE NWTifmhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLoU|ZuUUN3ME2wMlA1OSEQvF2= NGTCVXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkO2PVkzQCd-MkKzOlk6Ojh:L3G+
KMS11 NXW5[VJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfG[IFKSzVyPUCuNlgyKM7:TR?= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN4OUmyPEc,OjJ|Nkm5Nlg9N2F-
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KG1 NGDNWoZHfW6ldHnvckBie3OjeR?= M1\wblczKGi{cx?= M{fNVmlvcGmkaYTpc44hd2ZiRlfGVlEhcW5iaIXtZY4hU0dzIHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA4OiCqcoOgZpkhW1KEL1PDT{05KGG|c3H5MEBKSzVyIE2gNE4xODB{IN88UU4> NG\zRWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GxO|QzPyd-MkexNVc1Ojd:L3G+
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A673 NVzCbJlyeUiWUzDzd4F6 MW\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 NUXjUJJjeUiWUzDzd4F6 NEDMcZFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 NFrPPVhyUFSVIIPzZZk> MoT6dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUO3JINmdGy| M3TDcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
RD MWLxTHRUKHO|YYm= M3vYcJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCURDDj[Yxtew>? NHnZfHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH NVnxZpN3eUiWUzDzd4F6 MUnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= NXT3NXZKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12 M1jRbJFJXFNic4PhfS=> MXzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 MofCdWhVWyC|c3H5 Mn7OdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= Ml3GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
fibroblast cells M3L3WpFJXFNic4PhfS=> MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5Ih[2:wdILvcEBJcCC5aXzkJJR6eGViZnnido9jdGG|dDDj[Yxtew>? NF\yPWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 NEDxSotyUFSVIIPzZZk> MYPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? NXzqWnllRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh30 MXrxTHRUKHO|YYm= M1X1ZpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEOwJINmdGy| M3HxOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 M2rQdJFJXFNic4PhfS=> NETJRW9yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> NWnINpA2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1 MkD4dWhVWyC|c3H5 MUPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= MlzIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 M3;WVJFJXFNic4PhfS=> NX7UbnJneUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz Ml\oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh18 M{nHb5FJXFNic4PhfS=> M3jjcpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEG4JINmdGy| M{TSfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... 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、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

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