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。

AZD4547 Chemical Structure

CAS: 1035270-39-3

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 7125.05 现货
大包装 有超大折扣

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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

相关FGFR产品

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 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=
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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]

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]
  • 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]
  • 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

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

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
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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,: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: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: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

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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