AZD4547

For research use only. Not for use in humans.

目录号：S2801

CAS No. 1035270-39-3

AZD4547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。

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10mM (1mL in DMSO)	RMB 1801.43	现货
5mg	RMB 901.31	现货
10mg	RMB 1395.39	现货
50mg	RMB 4661.52	现货
100mg	RMB 7125.05	现货
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客户使用Selleck生产的AZD4547发表文献78篇：

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Br J Cancer, 2020, 22

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Br J Cancer, 2020, 10.1038/s41416-020-0952-1

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Front Oncol, 2020, 10;10:331

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Int J Mol Sci, 2020, 18;21(8):2825

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Acta Pharmacol Sin, 2020, 10.1038/s41401-020-00567-3

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Oncol Rep, 2020, 44(6):2581-2594

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EMBO Mol Med, 2020, e11793

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Biochem Genet, 2020, 10.1007/s10528-020-09982-x

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BMC Pharmacol Toxicol, 2020, 21(1):61

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Mol Cancer Res, 2020, 18(4):549-559

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Stem Cell Res Ther, 2020, 11(1):67

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Nat Commun, 2019, 10(1):2701

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EMBO Mol Med, 2019, 11(2)

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Cell Rep, 2019, 28(9):2331-2344

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J Exp Clin Cancer Res, 2019, 38(1):372

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Mol Cancer Res, 2019,

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J Cell Mol Med, 2019, 23(4):2933-2942

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J Cell Mol Med, 2019, 101111/jcmm14793

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Sci Rep, 2019, 9(1):8726

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Hepatology, 2018, 10.1002/hep.30127

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Int J Cancer, 2016,

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Oncogene, 2016, 10.1038/onc.2016.216

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J Proteome Res, 2016, 15(12):4490-4504

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Hum Mol Genet, 2016, 25(1):9-23

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Oncotarget, 2016, 7(31-:50161-50179

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Oncotarget, 2016, 7(18-:25983-6002

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PLoS One, 2015, 10(4):e0124562

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Oncotarget, 2015,

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Cell Physiol Biochem, 2014, 33(3):633-45

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Gastric Cancer, 2014, 10.1007/s10120-014-0444-1

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Celon Pharma Inc, 2013, Paulina Grygielewicz

PubMed: ( click the link to review the publication )

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	Activity Description	PMID
SNU449	M3HW[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NFm3cG44OiCq	NHjHbWVKSzVyPUCuNFgzKM7:TR?=	MmP1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|NUGzNlAoRjJ4M{WxN\|IxRC:jPh?=
SK-HEP-1	NHHpbpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NGHDfIY4OiCq	M4X3UmlEPTB;MD6wPFQh\|ryP	M1TaPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{WxN\|IxLz5{NkO1NVMzODxxYU6=
SNU475	NYHocppMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MUO3NkBp	NGTydphKSzVyPUWuOEDPxE1?	NF6wd3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO1NVMzOCd-Mk[zOVE{OjB:L3G+
Hep3B	M2TndWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MkH3O\|IhcA>?	M4\jcWlEPTB;Nj60N{DPxE1?	M1izT\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{WxN\|IxLz5{NkO1NVMzODxxYU6=
PLC/PRF5	NV[2[IJtT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MoDsO\|IhcA>?	MXvJR\|UxRTZwNUWg{txO	M4ixcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{WxN\|IxLz5{NkO1NVMzODxxYU6=
Hur7	MmrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M1jCclczKGh?	NVn6VHV[UUN3ME23MlI2KM7:TR?=	MnfpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|NUGzNlAoRjJ4M{WxN\|IxRC:jPh?=
HepG2	NYPkSIl5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NXLYSnI6PzJiaB?=	MXrJR\|UxRThwN{Og{txO	MoLDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|NUGzNlAoRjJ4M{WxN\|IxRC:jPh?=
SNU449	MlSzR4xwdm:pZX7pZ{Bie3OjeR?=	MVOxJOK2VQ>?	NH3GUHczPCCq	NUPZZWds\GWlcnXhd4V{KGOxbH;ufUBnd3KvYYTpc44he2mpbnnmbYNidnSueR?=	MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3MUOyNEc,OjZ\|NUGzNlA9N2F-
SK-HEP-1	NVTYS5BqS2yxbn;n[Y5q[yCjc4PhfS=>	Mo[2NUDDvU1?	MWSyOEBp	MnP6[IVkemWjc3XzJINwdG:weTDmc5Ju[XSrb36gd4lodmmoaXPhcpRtgQ>?	M4n6d\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{WxN\|IxLz5{NkO1NVMzODxxYU6=
SNU449	M2e1PWZ2dmO2aX;uJGF{e2G7	NWnST4lQOC1{IN88US=>	MofLOFghcA>?	MWTjZZV{\XNiYTDk[YNz\WG\|ZTDv[kBHWlN{78{MRWtVNCCjbnSgSXJMKHCqb4PwbI9zgWyjdHnvci=>	NYL0ephPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOVE{OjBpPkK2N\|UyOzJyPD;hQi=>
SK-HEP-1	MVHGeY5kfGmxbjDBd5NigQ>?	M4fVVFAuOiEQvF2=	M1HERlQ5KGh?	MVnjZZV{\XNiYTDk[YNz\WG\|ZTDv[kBHWlN{78{MRWtVNCCjbnSgSXJMKHCqb4PwbI9zgWyjdHnvci=>	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3MUOyNEc,OjZ\|NUGzNlA9N2F-
BaF3 FLT3-TEL	NXjRS45lT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NYXISmlqT0l3ME20MlYhyrFiMD61O\|ch\|ryP	NUDNTGhwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPVQ4PDFpPkK2Nlk1PzRzPD;hQi=>
BaF3 RET-TEL	NGDOb3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NEDmSmNIUTVyPUCuN\|khyrFiMD6wOFgh\|ryP	MmruQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O\|QyRC:jPh?=
BaF3 Parental	M4e1[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M1z1dmdKPTExubWxNEDPxE1?	MmPkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O\|QyRC:jPh?=
MOLM14 FLT3/ITD	NIO0SWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NU\rZpUxT0l3ME2wMlQ5PCEEsTCwMlE2PyEQvF2=	Mm[1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O\|QyRC:jPh?=
MV4-11 FLT3/ITD	MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M4DLcWdKPTB;MD60OVkhyrFiMD6wOFYh\|ryP	MmrmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O\|QyRC:jPh?=
TT RET C634W	MnzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NUm5VZNNT0l3ME2yMlkhyrFiMD65NFQh\|ryP	MlrLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O\|QyRC:jPh?=
AN3-CA FGFR2 N550K, K310R	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MmSyS2k2OD1yLkCzNUDDuSByLkCyN{DPxE1?	Mn[xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O\|QyRC:jPh?=
MFE296 FGFR2 N550K	NIXJUnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NInYU4dIUTVyPUCuO\|MxKMLzIECuNFU4KM7:TR?=	NUPXT21yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPVQ4PDFpPkK2Nlk1PzRzPD;hQi=>
MFE280 FGFR2 S252W	NVLmUVQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NWXl[FRJT0l3ME2wMlIyQCEEsTCwMlA4OyEQvF2=	NVWxT\|RHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPVQ4PDFpPkK2Nlk1PzRzPD;hQi=>
Ishikawa FGFF2 over exp.	M3;Ddmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			Mn7tS2k2OD12LkWgxtEhOS53MTFOwG0>	NYrKW\|BDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPVQ4PDFpPkK2Nlk1PzRzPD;hQi=>
HEC1A Normal FGFR2	Mn\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NF\xcW1IUTVy78olNVAh\|ryP	NH3uTYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK5OFc1OSd-Mk[yPVQ4PDF:L3G+
A549	NWDDN\|F4S2WubDD2bYFjcWyrdImgRZN{[Xl?	MU[wMlEwOSEQvF2=	NEXQeHE1QCCq	MULlcohidmOnczDFdoxwfGmwaXKgbY5lfWOnZDD2bYFjcWyrdImgcI9{ew>?	NYD0N\|V[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wOVMxOjBpPkK2NFU{ODJyPD;hQi=>
SGC-7901	M4jmRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmjYNUBvVS1zMDFOwG0>	MlO1O\|IhcA>?	NHzQ[25KSzVyIH;mJFUuOTBizszNMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7	NX;pV4dCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1O\|Y6OTVpPkK1OVc3QTF3PD;hQi=>
HGC-27	M3TCZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NV34cIdwOSCwTT2xNEDPxE1?	NEXsXJI4OiCq	NEPn[o9KSzVyIH;mJFUuOTBizszNMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7	NH7Ffmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW3OlkyPSd-MkW1O\|Y6OTV:L3G+
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NCI-H1581	NF\NfldCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		M3vOVFczKGi{cx?=	Ml;vRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCQQ1mtTFE2QDFiY3XscJMh\XiycnXzd4lv\yCIR1\SNUBi\nSncjC3NkBpenNuIFnDOVAhRSByLkC0JO69VS5?	Ml70QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5N{W5N\|coRjJ7N{e1PVM4RC:jPh?=
B16F10	M3i2e2N6fG:2b4jpZ4l1gSCjc4PhfS=>		M1zyR\|czKGi{cx?=	MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W\|ZTDCNVZHOTBiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFAvODVzIN88UU4>	MmrRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5M{[5PVMoRjJ3N{O2PVk{RC:jPh?=
A549	M1jue2N6fG:2b4jpZ4l1gSCjc4PhfS=>		M2S4eFczKGi{cx?=	NWS0dm5QS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC5yNkKg{txONg>?	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd\|Nkm5N{c,OjV5M{[5PVM9N2F-
NCI-H1581	M4nJdGZ2dmO2aX;uJIF{e2G7		NF3tT5o4OiCqcoO=	MkjjTY5pcWKrdHnvckBw\iCIR1\SNUBqdiCqdX3hckBPS0lvSEG1PFEh[2WubIOgZZN{\XO\|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiN{KgbJJ{KGK7IHPlcIwh[2:3boTpcochc2m2LUigZZN{[XluIFnDOVAhRSByLkC2NlYh\|ryPLh?=	M3i5[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{G0OlkzLz5{OEexOFY6OjxxYU6=
RT112	NYHHZZJJSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NXWxWHRYPzJiaILz	NFmwdppCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGLUNVEzKGOnbHzzJIV5eHKnc4PpcochTkeIUkOgZYZ1\XJiN{KgbJJ{NCCLQ{WwJF0hOC5yOEO4JO69VS5?	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd5NUmzO{c,Ojl5N{W5N\|c9N2F-
RT112	NYDEfZFOSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MnzkO\|IhcHK\|	NVHKblc3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBHT0[UMz3hcZBtcW[rZXSgbJVu[W5iUmSxNVIh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPDT\|gwVVSWIHHzd4F6NCCLQ{WwJF0hOC5yOEi0JO69VS5?	MmrqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd\|NEi1N\|coRjJ5M{S4OVM4RC:jPh?=
NCI-H1581	NVvkOplISW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NF7kTG84OiCqcoO=	NHTIVYNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGZITlJzLXHtdIxq\mmnZDDoeY1idiCQQ1mtTFE2QDFiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JGNEUzhxTWTUJIF{e2G7LDDJR\|UxKD1iMD6wPVIyKM7:TT6=	MnO1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd\|NEi1N\|coRjJ5M{S4OVM4RC:jPh?=
HeLa 229	MWfDfZRwfG:6aXPpeJkh[XO\|YYm=		NUXaSYk4PzJiaILz	Ml:0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SB{MkmgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDBwMUSg{txONg>?	M1jqXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{O2PVk{Lz5{NUezOlk6OzxxYU6=
BAF3	NXPTV2M3SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M3z6cVczKGi{cx?=	M2m0VWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViQlHGN{Bk\WyuczDlfJBz\XO\|aX7nJHZGT0[UMjDh[pRmeiB5MjDodpMtKEmFNUCgQUAxNjJ{MjFOwG0v	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd5NUmzO{c,Ojl5N{W5N\|c9N2F-
SGC7901	M4rrWmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		M3LF[VczKGi{cx?=	M4HCXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1fDO\|kxOSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG\|c3H5MEBKSzVyIE2gNk45KM7:TT6=	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzh{OUWxPUc,Ojd6Mkm1NVk9N2F-
MGC803	MlP4RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		M{HWXVczKGi{cx?=	NXO5TYZ5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNS2M5ODNiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFYvOiEQvF2u	NVO2WGlrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4Nlk2OTlpPkK3PFI6PTF7PD;hQi=>
BGC823	MonKRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NGDRe4k4OiCqcoO=	NHzRNZRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLHR\|gzOyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG\|c3H5MEBKSzVyIE2gO{46KM7:TT6=	NYfYeJNxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4Nlk2OTlpPkK3PFI6PTF7PD;hQi=>
HL7702	MmXXR5l1d3SxeHnjbZR6KGG\|c3H5		MkDpO\|IhcHK\|	M{GzdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhNPzdyMjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOThwMkGg{txONg>?	M{mzU\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{O2PVk{Lz5{NUezOlk6OzxxYU6=
U-2 OS	M2DLd5FJXFNic4PhfS=>			NUf6XZJ5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGWtNkBQWyClZXzsdy=>	M1;4cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673	NX\wUXJEeUiWUzDzd4F6			M13IO5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy\|	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Saos-2	MYXxTHRUKHO\|YYm=			NFruVGFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz	NYPOWW9iRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37	MY\xTHRUKHO\|YYm=			MXvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN?	NILjRWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
RD	NH35PYNyUFSVIIPzZZk>			MX;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM>	NFjjbYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
SK-N-SH	MVzxTHRUKHO\|YYm=			MnWxdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO=	MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
BT-12	M2PTZZFJXFNic4PhfS=>			MXTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN?	M1nFTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50	NGfQRYtyUFSVIIPzZZk>			Ml[wdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?=	MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
fibroblast cells	MXnxTHRUKHO\|YYm=			M{PGU5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiClb370do9tKEiqIIfpcIQhfHmyZTDmbYJzd2KuYYP0JINmdGy\|	NGLuelk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Rh41	NUjaV3pyeUiWUzDzd4F6			MkH1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN?	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Rh30	M4T5eJFJXFNic4PhfS=>			NVm2endleUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGLoN\|Ah[2WubIO=	NWPyeGFTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2	MlKydWhVWyC\|c3H5			MlmxdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO=	MnTHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1	NHvwOXpyUFSVIIPzZZk>			M1:w[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
LAN-5	MoDUdWhVWyC\|c3H5			NITpPZpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO=	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Rh18	MYrxTHRUKHO\|YYm=			MVvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>?	M2fFOlxiKHSjcnfleF0oZ2KuYX7rK{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 Sci Rep 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 Oncotarget 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 Sci Rep 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 Oncotarget 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]

激酶实验：^[1]	- 合并 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]	- 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)

参考文献

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

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 Download AZD4547 SDF

分子量	463.57
化学式	C₂₆H₃₃N₅O₃
CAS号	1035270-39-3
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	N/A

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

每只动物给药体积

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

计算重置

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。

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。

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

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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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 (data from https://clinicaltrials.gov, updated on 2020-01-06)

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

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。

FGFR Signaling Pathway Map

FGFR Inhibitors with Unique Features

选择性强的FGFR抑制剂

PD173074 : FGFR1-selective, IC50=~25 nM.
FDA批准的FGFR抑制剂

Ponatinib (AP24534) : Approved by FDA for resistant or intolerant CML and Ph+ ALL.
最新的FGFR抑制剂

SSR128129E ^New : Orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs.
经典的FGFR抑制剂

Dovitinib (TKI-258, CHIR-258) : Multitargeted RTK inhibitor for class III (FLT3/c-Kit), class IV (FGFR1/3) and class V (VEGFR1-4) RTKs.

研究领域

产品类型

定制您的化合物库

AZD4547

客户使用Selleck生产的AZD4547发表文献78篇：

产品安全说明书

FGFR抑制剂选择性比较

生物活性

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)

参考文献

溶解度 (25°C)

化学数据 Download AZD4547 SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2020-01-06)

技术支持

FGFR Signaling Pathway Map

FGFR Inhibitors with Unique Features

相关FGFR产品