AZD4547

Catalog No.S2801 Synonyms: ABSK 091

For research use only.

AZD4547 (ABSK 091) is a novel selective FGFR inhibitor targeting FGFR1/2/3 with IC50 of 0.2 nM/2.5 nM/1.8 nM in cell-free assays, weaker activity against FGFR4, VEGFR2(KDR), and little activity observed against IGFR, CDK2, and p38. Phase 2/3.

AZD4547 Chemical Structure

CAS No. 1035270-39-3

Selleck's AZD4547 has been cited by 102 publications

Purity & Quality Control

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Biological Activity

Description AZD4547 (ABSK 091) is a novel selective FGFR inhibitor targeting FGFR1/2/3 with IC50 of 0.2 nM/2.5 nM/1.8 nM in cell-free assays, weaker activity against FGFR4, VEGFR2(KDR), and little activity observed against IGFR, CDK2, and p38. Phase 2/3.
Features Greater selectivity for FGFR1-3 over FGFR4. AZD4547 is active against the tyrosine kinase activity of both the wild-type and mutant forms of FGFR.
Targets
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
In vitro

Compared to FGFR1-3, AZD4547 displays weaker activity against FGFR4 with IC50 of 165 nM. AZD4547 only inhibits recombinant VEGFR2 (KDR) kinase activity with IC50 of 24 nM, in the in vitro selectivity test against a diverse panel of representative human kinases. AZD4547 at 0.1 μM exhibits no activity against a range of recombinant kinases including ALK, CHK1, EGFR, MAPK1, MEK1, p70S6K, PDGFR, PKB, Src, Tie2, and PI3-kinase. Consistently, the potent selectivity of AZD4547 for FGFR1-3 over FGFR4, IGFR, and KDR is also observed in cellular phosphorylation assays. AZD4547 has potent in vitro antiproliferative activity only against tumor cell lines expressing deregulated FGFRs such as KG1a, Sum52-PE, and KMS11 with IC50 of 18-281 nM, and is inactive against MCF7 as well as more than 100 additional tumor cell lines. AZD4547 treatment potently inhibits FGFR and MAPK phosphorylation in human tumor cell lines in a dose-dependent manner. AZD4547 also potently inhibits the phosphorylation of FRS2 and PLCγ, downstream markers of FGFR signaling. Notably, AZD4547 affects the AKT phosphorylation in the breast cell lines, MCF7 and Sum52-PE but not in KG1a and KMS11 lines. AZD4547 treatment significantly induces apoptosis in Sum52-PE and KMS11 cells, dramatically increases G1 arrest but not apoptosis in KG1a cells, and has no effect on cell cycle distribution or apoptosis in MCF7 cells. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SNU449 NIXQT25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWK3NkBp M125S2lEPTB;MD6wPFIh|ryP NYHENZo6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOVE{OjBpPkK2N|UyOzJyPD;hQi=>
SK-HEP-1 M37hcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1n3S|czKGh? M12yNWlEPTB;MD6wPFQh|ryP M4fTNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{WxN|IxLz5{NkO1NVMzODxxYU6=
SNU475 NVvXZWhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TE[VczKGh? NEO5R2VKSzVyPUWuOEDPxE1? NX7WNXkzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOVE{OjBpPkK2N|UyOzJyPD;hQi=>
Hep3B NH\oU3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHMemJSPzJiaB?= M{[5SmlEPTB;Nj60N{DPxE1? NFjiRm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO1NVMzOCd-Mk[zOVE{OjB:L3G+
PLC/PRF5 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXi3NkBp NEK5RVFKSzVyPU[uOVUh|ryP NYfJcnB[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOVE{OjBpPkK2N|UyOzJyPD;hQi=>
Hur7 M4LGVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLZVYw4OiCq M2TQUGlEPTB;Nz6yOUDPxE1? M2noPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{WxN|IxLz5{NkO1NVMzODxxYU6=
HepG2 NWfxRlFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrDbo84OiCq M3\6[mlEPTB;OD63N{DPxE1? MnP5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|NUGzNlAoRjJ4M{WxN|IxRC:jPh?=
SNU449 MWnDcI9vd2enbnnjJIF{e2G7 NWm0U2N7OSEEtV2= NGWx[JIzPCCq NGfsN21l\WO{ZXHz[ZMh[2:ub375JIZwem2jdHnvckB{cWewaX\pZ4FvfGy7 NYH3S4pCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOVE{OjBpPkK2N|UyOzJyPD;hQi=>
SK-HEP-1 MVjDcI9vd2enbnnjJIF{e2G7 NXv3fpBMOSEEtV2= NEnNSIkzPCCq NUCyS|BT\GWlcnXhd4V{KGOxbH;ufUBnd3KvYYTpc44he2mpbnnmbYNidnSueR?= NXPiVnF5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOVE{OjBpPkK2N|UyOzJyPD;hQi=>
SNU449 NGD5bnhHfW6ldHnvckBCe3OjeR?= MYKwMVIh|ryP MYO0PEBp NIrOepNk[XW|ZYOgZUBl\WO{ZXHz[UBw\iCIUmOy89yNSUuWLDDhcoQhTVKNIIDoc5NxcG:{eXzheIlwdg>? Ml3hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|NUGzNlAoRjJ4M{WxN|IxRC:jPh?=
SK-HEP-1 NXjNb4VnTnWwY4Tpc44hSXO|YYm= NUnaVZBwOC1{IN88US=> M4Xr[VQ5KGh? NFnVVY9k[XW|ZYOgZUBl\WO{ZXHz[UBw\iCIUmOy89yNSUuWLDDhcoQhTVKNIIDoc5NxcG:{eXzheIlwdg>? M{CzXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{WxN|IxLz5{NkO1NVMzODxxYU6=
BaF3 FLT3-TEL Mnn3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DKeGdKPTB;ND62JOKyKDBwNUe3JO69VQ>? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ7NEe0NUc,OjZ{OUS3OFE9N2F-
BaF3 RET-TEL MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\2S2k2OD1yLkO5JOKyKDBwMES4JO69VQ>? MnizQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O|QyRC:jPh?=
BaF3 Parental MkHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHuS2k2OO,7pUGwJO69VQ>? Mlz5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O|QyRC:jPh?=
MOLM14 FLT3/ITD NIjwSGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnHTVUxRTBwNEi0JOKyKDBwMUW3JO69VQ>? NGjxO5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK5OFc1OSd-Mk[yPVQ4PDF:L3G+
MV4-11 FLT3/ITD NYLWOlJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjhcZVlT0l3ME2wMlQ2QSEEsTCwMlA1PiEQvF2= NFn3PI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK5OFc1OSd-Mk[yPVQ4PDF:L3G+
TT RET C634W NXPnVnB[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzH[25IUTVyPUKuPUDDuSByLkmwOEDPxE1? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ7NEe0NUc,OjZ{OUS3OFE9N2F-
AN3-CA FGFR2 N550K, K310R M2Lpb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LqTmdKPTB;MD6wN|EhyrFiMD6wNlMh|ryP NUPnWnZRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPVQ4PDFpPkK2Nlk1PzRzPD;hQi=>
MFE296 FGFR2 N550K MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrUS2k2OD1yLkezNEDDuSByLkC1O{DPxE1? NX6ySHRGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPVQ4PDFpPkK2Nlk1PzRzPD;hQi=>
MFE280 FGFR2 S252W Mnv0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDHTVUxRTBwMkG4JOKyKDBwMEezJO69VQ>? NV7Ue3FNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPVQ4PDFpPkK2Nlk1PzRzPD;hQi=>
Ishikawa FGFF2 over exp. NGqzUYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnYVo9IUTVyPUSuOUDDuSBzLkWxJO69VQ>? Mm\nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OUS3OFEoRjJ4Mkm0O|QyRC:jPh?=
HEC1A Normal FGFR2 M{jqVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXX0fFZqT0l3MP-5qVExKM7:TR?= NGXQS2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK5OFc1OSd-Mk[yPVQ4PDF:L3G+
A549 MmDlR4VtdCC4aXHibYxqfHliQYPzZZk> NXrQPZVYOC5zL{Gg{txO NWHMS3pEPDhiaB?= MlP0[Y5p[W6lZYOgSZJtd3SrbnniJIlv\HWlZXSgeoli[mmuaYT5JIxwe3N? M{D2O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEWzNFIxLz5{NkC1N|AzODxxYU6=
SGC-7901 M4DNbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnBcpU2OSCwTT2xNEDPxE1? NInTe2w4OiCq NVLWdodiUUN3MDDv[kA2NTFyIN88UUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV5NkmxOUc,OjV3N{[5NVU9N2F-
HGC-27 Mm[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3z4U|Ehdk1vMUCg{txO M4jvNFczKGh? NIGzfJJKSzVyIH;mJFUuOTBizszNMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M1u1OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUe2PVE2Lz5{NUW3OlkyPTxxYU6=
MKN-28 NG\xVWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYqxJI5ONTFyIN88US=> M{fhO|czKGh? NUnhWZZpUUN3MDDv[kA2NTFyIN88UUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MoPTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3N{[5NVUoRjJ3NUe2PVE2RC:jPh?=
NCI-N87 M{n6Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rGOVEhdk1vMUCg{txO NHLnOYc4OiCq MYjJR|UxKG:oIEWtNVAh|ryPLDDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NYGxS2x6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1O|Y6OTVpPkK1OVc3QTF3PD;hQi=>
KATOIII M{TXS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGxJI5ONTFyIN88US=> NX\PUIJPPzJiaB?= M3T0Z2lEPTBib3[gNVAuOTByIH7NMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M3y1VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUe2PVE2Lz5{NUW3OlkyPTxxYU6=
SNU-16 M3LHWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWixJI5ONTFyIN88US=> NU[0OIFYPzJiaB?= NXjWTZNxUUN3MDDv[kAyOC1zMECgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= NXrQToxSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1O|Y6OTVpPkK1OVc3QTF3PD;hQi=>
4T1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGG4XWVKSzVyPUCuOlTDuTBwMUGg{txO M1\rOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSyPFk{Lz5{NE[0Nlg6OzxxYU6=
MDA-MB-468 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTRwOdMxNE45PSEQvF2= M3jPXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSyPFk{Lz5{NE[0Nlg6OzxxYU6=
HCT116 M1rtSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:3ZmlEPTB;MUWuPeKyOS56MjFOwG0> M1fwTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSyPFk{Lz5{NE[0Nlg6OzxxYU6=
SW620 NYK2c3NYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LxeWlEPTExvK6yNEDPxE1? NEXUVm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0Nlg6Oyd-MkS2OFI5QTN:L3G+
MDA-MB-231 NHTucHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4GyUGlEPTExvK6yNEDPxE1? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2Mki5N{c,OjR4NEK4PVM9N2F-
CT26 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|Ux97zgMkCg{txO NY\aZnQ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFI5QTNpPkK0OlQzQDl|PD;hQi=>
SW480 NFj3U45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|Ux97zgMkCg{txO M4O1WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSyPFk{Lz5{NE[0Nlg6OzxxYU6=
4T1 MY\BdI9xfG:|aYOgRZN{[Xl? MYKxMlI2NTJyIN88US=> NWrwOWN3OjRiaB?= NWnhd21FcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M4DvdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSyPFk{Lz5{NE[0Nlg6OzxxYU6=
KG1a NYHafGt3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnwfFh5UUN3ME2wMlAyQCEQvF2= NFHMNW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkO2PVkzQCd-MkKzOlk6Ojh:L3G+
Sum52-PE MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfsRm9zUUN3ME2wMlA1OSEQvF2= NY\XS|FGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzOlk6OjhpPkKyN|Y6QTJ6PD;hQi=>
KMS11 NVXhZpZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTBwMkixJO69VQ>? Ml60QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|Nkm5NlgoRjJ{M{[5PVI5RC:jPh?=
MCF7 M1XReWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLZTWM2OD5|MDFOwG0> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN4OUmyPEc,OjJ|Nkm5Nlg9N2F-
KG1 Mk[ySpVv[3Srb36gZZN{[Xl? NH\EeFc4OiCqcoO= NHPw[YpKdmirYnn0bY9vKG:oIF\HSnIyKGmwIHj1cYFvKEuJMTDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KFOUQj;DR2suQCCjc4PhfUwhUUN3MDC9JFAvODByMjFOwG0v M4D3RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUG3OFI4Lz5{N{GxO|QzPzxxYU6=
RT112 M4P4ZmZ2dmO2aX;uJIF{e2G7 M4DJcFczKGi{cx?= NFfGUnFKdmirYnn0bY9vKG:oIF\HSnI{KGmwIHj1cYFvKFKWMUGyJINmdGy|IHHzd4V{e2WmIHHzJJN2eHC{ZYPzbY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDh[pRmeiB5MjDodpMh[nliU2LCM2NEUy16IHHzd4F6NCCLQ{WwJF0hOC5yMEC2JO69VS5? M4fxUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUG3OFI4Lz5{N{GxO|QzPzxxYU6=
KG1 NUP3TYZCSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M4DJRlczKGi{cx?= M3rwZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1exJINmdGy|IHX4dJJme3OrbnegSmdHWjFiYX\0[ZIhPzJiaILzMEBKSzVyIE2gNE4xODF7IN88UU4> MkfhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5N{W5N|coRjJ7N{e1PVM4RC:jPh?=
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NB-EBc1 MmjpdWhVWyC|c3H5 MlTydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ|Eh[2WubIO= M1XnWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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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
In vivo Oral administration of AZD4547 at 3 mg/kg twice daily in mice bearing KMS11 tumors results in significant tumor growth inhibition of 53% when compared with vehicle-treated controls, and AZD4547 at 12.5 mg/kg once daily or 6.25 mg/kg twice daily leads to complete tumor stasis, which is associated with dose proportional pharmacodynamic modulation of phospho-FGFR3 and reduced KMS11 tumor cell proliferation. Moreover, oral administration of AZD4547 at 12.5 mg/kg once daily results in 65% tumor growth inhibition in the FGFR1-fusion KG1a xenograft model. At efficacious dose levels, AZD4547 does not exhibit antiangiogenic effects. AZD4547 has no significant effect on blood pressure and therefore lacks in vivo anti-KDR activity. Consistently, dosing of 6.25 mg/kg orally twice daily AZD4547 is inactive in the cediranib-sensitive xenograft models including Calu-6, HCT-15 and LoVo. [1]

Protocol (from reference)

Kinase Assay:[1]
  • AZD4547 kinase activity:

    The ability of AZD4547 to inhibit the human recombinant kinase activities of FGFR1-3 is tested using ATP concentrations at, or just below, the respective Km.

Cell Research:[1]
  • Cell lines: KG1a, Sum52-PE, KMS11, and MCF7
  • Concentrations: Dissolved in DMSO, final concentrations ~1 μM
  • Incubation Time: 72 hours
  • Method: Cells are exposed to various concentrations of AZD4547 for 72 hours. The antiproliferative IC50 values are obtained by MTS proliferation assay. For fluorescence-activated cell sorting (FACS), cells are fixed with 70% ethanol and then incubated with propidium iodide/RNase A labeling solution. Cell cycle profiles are assessed with a FACSCalibur instrument and CellQuest analysis software. For apoptotic analysis, cells and media are gently harvested and centrifuged, followed by washing of cell pellets. Cells are then processed for Annexin V-fluorescein isothiocyanate (FITC) staining and propidium iodide uptake. The proportion of cells staining positive for Annexin V are then assessed with a FACSCalibur instrument and quadrant sorting is done by CellQuest analysis software.
Animal Research:[1]
  • Animal Models: Female swiss derived nude (nu/nu) and severe combined immunodeficient mice (SCID) injected s.c. with LoVo, HCT-15, Calu-6, KMS11 or KG1a
  • Dosages: 1.5-50 mg/kg
  • Administration: Oral gavage once daily or twice daily

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 463.57
Formula

C26H33N5O3

CAS No. 1035270-39-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CN(CC(N1)C)C2=CC=C(C=C2)C(=O)NC3=NNC(=C3)CCC4=CC(=CC(=C4)OC)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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