AZD4547

For research use only.

Catalog No.S2801

64 publications

AZD4547 Chemical Structure

CAS No. 1035270-39-3

AZD4547 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.

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Selleck's AZD4547 has been cited by 64 publications

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Biological Activity

Description AZD4547 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 NGLNSllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvzO|IhcA>? M16wVmlEPTB;MD6wPFIh|ryP NGfqVoYzPjN3MUOyNC=>
SK-HEP-1 MmjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIK2N3c4OiCq MVvJR|UxRTBwMEi0JO69VQ>? M4ruSFI3OzVzM{Kw
SNU475 NWToPXg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HVSlczKGh? NXjFW2Y2UUN3ME21MlQh|ryP MUSyOlM2OTN{MB?=
Hep3B MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofwO|IhcA>? NX;CNZFwUUN3ME22MlQ{KM7:TR?= MkixNlY{PTF|MkC=
PLC/PRF5 Mon4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4naXVczKGh? MonKTWM2OD14LkW1JO69VQ>? NHO2VW4zPjN3MUOyNC=>
Hur7 NEnsPHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnMVlhpPzJiaB?= NEPJZY9KSzVyPUeuNlUh|ryP MV:yOlM2OTN{MB?=
HepG2 MnKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXK3NkBp MorGTWM2OD16LkezJO69VQ>? M{HDdlI3OzVzM{Kw
SNU449 NFTWOmJEdG:wb3flcolkKGG|c3H5 MkCwNUDDvU1? MoO5NlQhcA>? NXe3PIx4\GWlcnXhd4V{KGOxbH;ufUBnd3KvYYTpc44he2mpbnnmbYNidnSueR?= MV[yOlM2OTN{MB?=
SK-HEP-1 MljyR4xwdm:pZX7pZ{Bie3OjeR?= M{\ac|EhyrWP Mn;sNlQhcA>? NHHUUG5l\WO{ZXHz[ZMh[2:ub375JIZwem2jdHnvckB{cWewaX\pZ4FvfGy7 MlTONlY{PTF|MkC=
SNU449 NXS1RXpkTnWwY4Tpc44hSXO|YYm= M33GVlAuOiEQvF2= Mlj0OFghcA>? NH;1fVZk[XW|ZYOgZUBl\WO{ZXHz[UBw\iCIUmOy89yNSUuWLDDhcoQhTVKNIIDoc5NxcG:{eXzheIlwdg>? MkDRNlY{PTF|MkC=
SK-HEP-1 NEDlVmhHfW6ldHnvckBCe3OjeR?= MlzUNE0zKM7:TR?= M{TiN|Q5KGh? NXPtWVNV[2G3c3XzJIEh\GWlcnXhd4Uhd2ZiRmLTNw+9lEGNVDygZY5lKEWUSzDwbI9{eGixconsZZRqd25? NHXZ[XEzPjN3MUOyNC=>
BaF3 FLT3-TEL M1;ZRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrSbGo{T0l3ME20MlYhyrFiMD61O|ch|ryP MYKyOlI6PDd2MR?=
BaF3 RET-TEL M1TKZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfHTVUxRTBwM{mgxtEhOC5yNEig{txO MoHPNlYzQTR5NEG=
BaF3 Parental M3rL[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvocHlnT0l3MP-5qVExKM7:TR?= M331c|I3Ojl2N{Sx
MOLM14 FLT3/ITD MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmK5S2k2OD1yLkS4OEDDuSByLkG1O{DPxE1? NXfyfYN6OjZ{OUS3OFE>
MV4-11 FLT3/ITD NVH2UWtCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPHTVUxRTBwNEW5JOKyKDBwMES2JO69VQ>? NGrUVnMzPjJ7NEe0NS=>
TT RET C634W M{HJXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7rS2k2OD1{LkmgxtEhOC57MESg{txO NGLwOZAzPjJ7NEe0NS=>
AN3-CA FGFR2 N550K, K310R M4fQdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnkPFBYT0l3ME2wMlA{OSEEsTCwMlAzOyEQvF2= NWjhRXpXOjZ{OUS3OFE>
MFE296 FGFR2 N550K MkHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jVWWdKPTB;MD63N|AhyrFiMD6wOVch|ryP NX\xOHF5OjZ{OUS3OFE>
MFE280 FGFR2 S252W MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\YToR[T0l3ME2wMlIyQCEEsTCwMlA4OyEQvF2= NYPyb|IxOjZ{OUS3OFE>
Ishikawa FGFF2 over exp. NXvoeXNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnL2S2k2OD12LkWgxtEhOS53MTFOwG0> MWGyOlI6PDd2MR?=
HEC1A Normal FGFR2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXUVYRIUTVy78olNVAh|ryP MY[yOlI6PDd2MR?=
A549 MVLD[YxtKH[rYXLpcIl1gSCDc4PhfS=> MWWwMlEwOSEQvF2= MX20PEBp NHjj[4RmdmijbnPld{BGemyxdHnubYIhcW6mdXPl[EB3cWGkaXzpeJkhdG:|cx?= NYPzeJpjOjZyNUOwNlA>
SGC-7901 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorDNUBvVS1zMDFOwG0> MUS3NkBp NX3WN2pGUUN3MDDv[kA2NTFyIN88UUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NWHsO2FpOjV3N{[5NVU>
HGC-27 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVOxJI5ONTFyIN88US=> MoDWO|IhcA>? M37MT2lEPTBib3[gOU0yOCEQvF2sJIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NInUWIwzPTV5NkmxOS=>
MKN-28 NHnpdWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXyxJI5ONTFyIN88US=> MoToO|IhcA>? MX7JR|UxKG:oIEWtNVAh|ryPLDDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NH7ubYMzPTV5NkmxOS=>
NCI-N87 NIm1WFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;jZmdXOSCwTT2xNEDPxE1? M{nQSVczKGh? NHjjS3NKSzVyIH;mJFUuOTBizszNMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MmDNNlU2PzZ7MUW=
KATOIII NI\iUmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPsXFMyKG6PLUGwJO69VQ>? MV23NkBp MWPJR|UxKG:oIEGwMVExOCCwTTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MoLBNlU2PzZ7MUW=
SNU-16 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljFNUBvVS1zMDFOwG0> M2nWbFczKGh? NICzN2hKSzVyIH;mJFExNTFyMDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NIfDZYczPTV5NkmxOS=>
4T1 NIfoS3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4f3PGlEPTB;MD62OOKyOC5zMTFOwG0> MYSyOFY1Ojh7Mx?=
MDA-MB-468 NHX1SHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDMVGFYUUN3ME20MlnDuTBwOEWg{txO NXe3WlJjOjR4NEK4PVM>
HCT116 M{mzd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTF3LkpCtVEvQDJizszN NE\jPWozPDZ2Mki5Ny=>
SW620 NHHWdHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3iNnpKSzVy78{eNlAh|ryP MXuyOFY1Ojh7Mx?=
MDA-MB-231 M4O2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkG2TWM2OO,:nkKwJO69VQ>? MXmyOFY1Ojh7Mx?=
CT26 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjiSZhKSzVy78{eNlAh|ryP NHLiOY4zPDZ2Mki5Ny=>
SW480 NXnGWYZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MniwTWM2OO,:nkKwJO69VQ>? MYOyOFY1Ojh7Mx?=
4T1 M4nSZmFxd3C2b4Ppd{BCe3OjeR?= NUK3RnlzOS5{NT2yNEDPxE1? M2rBWFI1KGh? M1HIVolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NH3jWpMzPDZ2Mki5Ny=>
KG1a NUfuRmNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXr3e|FLUUN3ME2wMlAyQCEQvF2= M3Xxb|IzOzZ7OUK4
Sum52-PE NEW1[XRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHqflM2UUN3ME2wMlA1OSEQvF2= MUKyNlM3QTl{OB?=
KMS11 NFjZZndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlP4TWM2OD1yLkK4NUDPxE1? MYqyNlM3QTl{OB?=
MCF7 NGTRRZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPoWoJxUUN3ME6zNEDPxE1? NH;UVmUzOjN4OUmyPC=>

... 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
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

Kinase Assay:[1]
- Collapse

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]
- Collapse
  • 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.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (198.45 mM)
Water Insoluble
Ethanol Insoluble
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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 463.57
Formula

C26H33N5O3

CAS No. 1035270-39-3
Storage powder
in solvent
Synonyms N/A
Smiles CC1CN(CC(N1)C)C2=CC=C(C=C2)C(=O)NC3=NNC(=C3)CCC4=CC(=CC(=C4)OC)OC

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID