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AZD4547

目录号：S2801 别名: ABSK 091

仅限科研使用

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。

CAS: 1035270-39-3

规格	价格	库存
10mM (1mL in DMSO)	RMB 1801.43	现货
5mg	RMB 901.31	现货
10mg	RMB 1395.39	现货
100mg	RMB 7125.05	现货
大包装	有超大折扣

今日订购，明日送达全国免运费分装免费分装成小规格产品（单支最小为1mg）如1支10mg产品可分装为10支1mg产品全国免费电话：400-668-6834 \| Email：info@selleck.cn

客户使用Selleck生产的AZD4547发表文献100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

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	NUf1UHB7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MoPNO\|IhcA>?	MoLzTWM2OD1yLkC4NkDPxE1?	NV7XToNLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOVE{OjBpPkK2N\|UyOzJyPD;hQi=>
SK-HEP-1	NWiye2NCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MmDzO\|IhcA>?	NIPUSGtKSzVyPUCuNFg1KM7:TR?=	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3MUOyNEc,OjZ\|NUGzNlA9N2F-
SNU475	NYf4OWtvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NV7aRooxPzJiaB?=	MVvJR\|UxRTVwNDFOwG0>	M32zPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{WxN\|IxLz5{NkO1NVMzODxxYU6=
Hep3B	M2HGVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NWDvVYZFPzJiaB?=	MoPvTWM2OD14LkSzJO69VQ>?	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3MUOyNEc,OjZ\|NUGzNlA9N2F-
PLC/PRF5	MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		Mon1O\|IhcA>?	NY\2TWRDUUN3ME22MlU2KM7:TR?=	NVHNeFlYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOVE{OjBpPkK2N\|UyOzJyPD;hQi=>
Hur7	NUDUOW9LT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M37KO\|czKGh?	Mnj3TWM2OD15LkK1JO69VQ>?	MnXhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|NUGzNlAoRjJ4M{WxN\|IxRC:jPh?=
HepG2	MoPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NF[wNpM4OiCq	NG\PXVBKSzVyPUiuO\|Mh\|ryP	MoK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|NUGzNlAoRjJ4M{WxN\|IxRC:jPh?=
SNU449	NFvPSVdEdG:wb3flcolkKGG\|c3H5	M2PUR\|EhyrWP	M1m2[VI1KGh?	M2e3doRm[3KnYYPld{Bkd2yxbomg[o9zdWG2aX;uJJNq\26rZnnjZY51dHl?	NIi3XGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO1NVMzOCd-Mk[zOVE{OjB:L3G+
SK-HEP-1	NWGyVmlQS2yxbn;n[Y5q[yCjc4PhfS=>	M3fCTVEhyrWP	MknJNlQhcA>?	NWDwWlZO\GWlcnXhd4V{KGOxbH;ufUBnd3KvYYTpc44he2mpbnnmbYNidnSueR?=	NFq5VGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO1NVMzOCd-Mk[zOVE{OjB:L3G+
SNU449	MlHRSpVv[3Srb36gRZN{[Xl?	MVKwMVIh\|ryP	M3zK[FQ5KGh?	MXLjZZV{\XNiYTDk[YNz\WG\|ZTDv[kBHWlN{78{MRWtVNCCjbnSgSXJMKHCqb4PwbI9zgWyjdHnvci=>	MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3MUOyNEc,OjZ\|NUGzNlA9N2F-
SK-HEP-1	NX;kZplUTnWwY4Tpc44hSXO\|YYm=	Ml[4NE0zKM7:TR?=	M4e3bFQ5KGh?	M1;m[oNifXOnczDhJIRm[3KnYYPlJI9nKE[UU{NvwKxCU1RuIHHu[EBGWkticHjvd5Bpd3K7bHH0bY9v	M3fXOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{WxN\|IxLz5{NkO1NVMzODxxYU6=
BaF3 FLT3-TEL	NIfJRpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NWSy[3QxT0l3ME20MlYhyrFiMD61O\|ch\|ryP	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ7NEe0NUc,OjZ{OUS3OFE9N2F-
BaF3 RET-TEL	NVLmR3ZiT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MmXoS2k2OD1yLkO5JOKyKDBwMES4JO69VQ>?	M{LxOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mkm0O\|QyLz5{NkK5OFc1OTxxYU6=
BaF3 Parental	M2TTNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NHLXU\|hIUTVy78olNVAh\|ryP	M2fTZ\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mkm0O\|QyLz5{NkK5OFc1OTxxYU6=
MOLM14 FLT3/ITD	MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M4H3[WdKPTB;MD60PFQhyrFiMD6xOVch\|ryP	M1PBeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mkm0O\|QyLz5{NkK5OFc1OTxxYU6=
MV4-11 FLT3/ITD	M1jQSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MUfHTVUxRTBwNEW5JOKyKDBwMES2JO69VQ>?	MnnZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O\|QyRC:jPh?=
TT RET C634W	MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NXvORWpNT0l3ME2yMlkhyrFiMD65NFQh\|ryP	NEfYPVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK5OFc1OSd-Mk[yPVQ4PDF:L3G+
AN3-CA FGFR2 N550K, K310R	NUTnTWQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M174V2dKPTB;MD6wN\|EhyrFiMD6wNlMh\|ryP	NWDHdY5FRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPVQ4PDFpPkK2Nlk1PzRzPD;hQi=>
MFE296 FGFR2 N550K	M2C0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MXjHTVUxRTBwN{OwJOKyKDBwMEW3JO69VQ>?	NYPSVYpXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPVQ4PDFpPkK2Nlk1PzRzPD;hQi=>
MFE280 FGFR2 S252W	NYroVphoT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MmrRS2k2OD1yLkKxPEDDuSByLkC3N{DPxE1?	MnS4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O\|QyRC:jPh?=
Ishikawa FGFF2 over exp.	NFvSVZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MnXtS2k2OD12LkWgxtEhOS53MTFOwG0>	NHzCbVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK5OFc1OSd-Mk[yPVQ4PDF:L3G+
HEC1A Normal FGFR2	M{jjOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MUHHTVUx97nnMUCg{txO	MlXPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O\|QyRC:jPh?=
A549	NWfWPZp1S2WubDD2bYFjcWyrdImgRZN{[Xl?	Ml21NE4yNzFizszN	MVi0PEBp	NH75e\|ZmdmijbnPld{BGemyxdHnubYIhcW6mdXPl[EB3cWGkaXzpeJkhdG:\|cx?=	MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB3M{CyNEc,OjZyNUOwNlA9N2F-
SGC-7901	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NI[2SlUyKG6PLUGwJO69VQ>?	NH;mWoc4OiCq	M{TnSWlEPTBib3[gOU0yOCEQvF2sJIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?	NHHxbnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW3OlkyPSd-MkW1O\|Y6OTV:L3G+
HGC-27	NF3LZ4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MoXnNUBvVS1zMDFOwG0>	MkfzO\|IhcA>?	M3riSmlEPTBib3[gOU0yOCEQvF2sJIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?	MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV5NkmxOUc,OjV3N{[5NVU9N2F-
MKN-28	M17GNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoDlNUBvVS1zMDFOwG0>	NEW2XYI4OiCq	MnWxTWM2OCCxZjC1MVExKM7:TTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?	NUnLV3FqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1O\|Y6OTVpPkK1OVc3QTF3PD;hQi=>
NCI-N87	MnrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFLDXZQyKG6PLUGwJO69VQ>?	MVu3NkBp	Mlu0TWM2OCCxZjC1MVExKM7:TTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?	NV20foNJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1O\|Y6OTVpPkK1OVc3QTF3PD;hQi=>
KATOIII	MknxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHzzS3gyKG6PLUGwJO69VQ>?	MX23NkBp	MYPJR\|UxKG:oIEGwMVExOCCwTTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?	Ml;YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3N{[5NVUoRjJ3NUe2PVE2RC:jPh?=
SNU-16	MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXmxJI5ONTFyIN88US=>	MlfHO\|IhcA>?	MU\JR\|UxKG:oIEGwMVExOCCwTTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?	NHLtbGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW3OlkyPSd-MkW1O\|Y6OTV:L3G+
4T1	MlLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MmfITWM2OD1yLk[0xtExNjFzIN88US=>	MkjIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEK4PVMoRjJ2NkSyPFk{RC:jPh?=
MDA-MB-468	MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NFPpVWZKSzVyPUSuPeKyOC56NTFOwG0>	NELnfFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0Nlg6Oyd-MkS2OFI5QTN:L3G+
HCT116	MlfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MWfJR\|UxRTF3LkpCtVEvQDJizszN	MmrQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEK4PVMoRjJ2NkSyPFk{RC:jPh?=
SW620	NFrNcGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M{LtTmlEPTExvK6yNEDPxE1?	NWH0VFBRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFI5QTNpPkK0OlQzQDl\|PD;hQi=>
MDA-MB-231	Mn3wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MomzTWM2OO,:nkKwJO69VQ>?	NEHPNnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0Nlg6Oyd-MkS2OFI5QTN:L3G+
CT26	NWLIdIFuT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MV7JR\|Ux97zgMkCg{txO	NGHsbnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0Nlg6Oyd-MkS2OFI5QTN:L3G+
SW480	NXvUTmo4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NHz0UGdKSzVy78{eNlAh\|ryP	NVT2VJpLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFI5QTNpPkK0OlQzQDl\|PD;hQi=>
4T1	M1jKU2Fxd3C2b4Ppd{BCe3OjeR?=	NHjIXG4yNjJ3LUKwJO69VQ>?	MViyOEBp	M4LpbIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm=	NEX5WoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0Nlg6Oyd-MkS2OFI5QTN:L3G+
KG1a	Mnj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MUDJR\|UxRTBwMEG4JO69VQ>?	NGW1RlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkO2PVkzQCd-MkKzOlk6Ojh:L3G+
Sum52-PE	NULYe2wyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NVq5dpg2UUN3ME2wMlA1OSEQvF2=	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN4OUmyPEc,OjJ\|Nkm5Nlg9N2F-
KMS11	NITKU2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MlrvTWM2OD1yLkK4NUDPxE1?	M1XHUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{[5PVI5Lz5{MkO2PVkzQDxxYU6=
MCF7	M1\sdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MnrHTWM2OD5\|MDFOwG0>	Mof5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ\|Nkm5NlgoRjJ{M{[5PVI5RC:jPh?=
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U-2 OS	NGnpNXZyUFSVIIPzZZk>			MnqydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFVvMjDPV{Bk\Wyucx?=	MkTYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
A673	NEHOSGhyUFSVIIPzZZk>			MWHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>?	M1uyfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2	MoTSdWhVWyC\|c3H5			MVfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy\|	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
BT-37	NEW1OIJyUFSVIIPzZZk>			MknidWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUO3JINmdGy\|	NVnJVHBLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD	M37m[pFJXFNic4PhfS=>			M1vMdJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCURDDj[Yxtew>?	M2TvU\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH	NVfyclVJeUiWUzDzd4F6			Mo\FdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO=	NXfvSXJmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12	MkHTdWhVWyC\|c3H5			NETyNGlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO=	NH\kTJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
OHS-50	MUDxTHRUKHO\|YYm=			MWfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy\|	NFzwOGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
fibroblast cells	NGXJVZdyUFSVIIPzZZk>			M3nWdZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiClb370do9tKEiqIIfpcIQhfHmyZTDmbYJzd2KuYYP0JINmdGy\|	NFrXdnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Rh41	Ml7zdWhVWyC\|c3H5			MnTpdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN?	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Rh30	NUPvdmdUeUiWUzDzd4F6			MXfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh\|MDDj[Yxtew>?	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SJ-GBM2	MYPxTHRUKHO\|YYm=			MYLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?=	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
NB-EBc1	M2rzNJFJXFNic4PhfS=>			NVP6S5BCeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM>	NFfWcWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
LAN-5	NYPaUpJSeUiWUzDzd4F6			MnradWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy\|	Mn;wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Rh18	MW\xTHRUKHO\|YYm=			M3K5UJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEG4JINmdGy\|	M2XZN\|xiKHSjcnfleF0oZ2KuYX7rK{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 pFRS2	28900173 25576915
Growth inhibition assay	Cell viability Cell viability	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]

激酶实验：^[1]	AZD4547 激酶活性: 使用浓度等于或低于相对K_m 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]	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。
动物实验：^[1]	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

参考文献	[1] Gavine PR, et al. Cancer Res, 2012, 72(8), 2045-2056.

溶解度（25°C）

体外


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 点击购买： PEG300 Tween 80	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	3年	-20°C	粉状
储存条件	2年	-80°C	溶于溶剂

Download AZD4547 SDF

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 μL 动物数量只

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

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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