AZD4547

Catalog No.S2801

AZD4547 Chemical Structure

Molecular Weight(MW): 463.57

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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Cited by 45 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 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnxT4c4OiCq NFfwbZFKSzVyPUCuNFgzKM7:TR?= MmPrNlY{PTF|MkC=
SK-HEP-1 NGHDVGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HadFczKGh? MkjETWM2OD1yLkC4OEDPxE1? NXrBWpF2OjZ|NUGzNlA>
SNU475 MmntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVi3NkBp M{\yZ2lEPTB;NT60JO69VQ>? Mkf2NlY{PTF|MkC=
Hep3B NWrPR2ZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfUWI04OiCq M4jPXWlEPTB;Nj60N{DPxE1? MoizNlY{PTF|MkC=
PLC/PRF5 NHP0OWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXm3NkBp Mmi1TWM2OD14LkW1JO69VQ>? M1rKRVI3OzVzM{Kw
Hur7 M3O5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjTUmZiPzJiaB?= NIfxPWFKSzVyPUeuNlUh|ryP MnSyNlY{PTF|MkC=
HepG2 NXHFWnVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fUR|czKGh? NX3Nc5J7UUN3ME24Mlc{KM7:TR?= MnjLNlY{PTF|MkC=
SNU449 MUXDcI9vd2enbnnjJIF{e2G7 NGLuO2syKML3TR?= MXWyOEBp NVq2S5lx\GWlcnXhd4V{KGOxbH;ufUBnd3KvYYTpc44he2mpbnnmbYNidnSueR?= NX7UdlhSOjZ|NUGzNlA>
SK-HEP-1 NVTienlDS2yxbn;n[Y5q[yCjc4PhfS=> NFL1dnAyKML3TR?= M{j6UFI1KGh? MWnk[YNz\WG|ZYOgZ49td267IH\vdo1ifGmxbjDzbYdvcW[rY3HueIx6 M37wRlI3OzVzM{Kw
SNU449 NHXu[YJHfW6ldHnvckBCe3OjeR?= MkHrNE0zKM7:TR?= Ml3kOFghcA>? NFXBVWRk[XW|ZYOgZUBl\WO{ZXHz[UBw\iCIUmOy89yNSUuWLDDhcoQhTVKNIIDoc5NxcG:{eXzheIlwdg>? MmDwNlY{PTF|MkC=
SK-HEP-1 M{PT[mZ2dmO2aX;uJGF{e2G7 MVewMVIh|ryP MnTBOFghcA>? NWf1dYl5[2G3c3XzJIEh\GWlcnXhd4Uhd2ZiRmLTNw+9lEGNVDygZY5lKEWUSzDwbI9{eGixconsZZRqd25? NEj0ZXkzPjN3MUOyNC=>
BaF3 FLT3-TEL NV:yc2g5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jMemdKPTB;ND62JOKyKDBwNUe3JO69VQ>? MVWyOlI6PDd2MR?=
BaF3 RET-TEL NX;ZOpVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3hOndIT0l3ME2wMlM6KMLzIECuNFQ5KM7:TR?= MWSyOlI6PDd2MR?=
BaF3 Parental NGLuSYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrwOoRIUTVy78olNVAh|ryP NVvx[YV{OjZ{OUS3OFE>
MOLM14 FLT3/ITD NEnCOHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PS[mdKPTB;MD60PFQhyrFiMD6xOVch|ryP NU\JOFM4OjZ{OUS3OFE>
MV4-11 FLT3/ITD M2PvOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3OwPWdKPTB;MD60OVkhyrFiMD6wOFYh|ryP NEP6[FAzPjJ7NEe0NS=>
TT RET C634W NH3C[YxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjzZ3d5T0l3ME2yMlkhyrFiMD65NFQh|ryP M1XTZ|I3Ojl2N{Sx
AN3-CA FGFR2 N550K, K310R NVq2VGhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnLS2k2OD1yLkCzNUDDuSByLkCyN{DPxE1? NWDiNYxIOjZ{OUS3OFE>
MFE296 FGFR2 N550K Mn\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPES2k2OD1yLkezNEDDuSByLkC1O{DPxE1? NUXC[3pbOjZ{OUS3OFE>
MFE280 FGFR2 S252W MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfXZYdTT0l3ME2wMlIyQCEEsTCwMlA4OyEQvF2= MlWyNlYzQTR5NEG=
Ishikawa FGFF2 over exp. MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v0ZWdKPTB;ND61JOKyKDFwNUGg{txO NIDoU4czPjJ7NEe0NS=>
HEC1A Normal FGFR2 NI\t[ZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjq[JNKT0l3MP-5qVExKM7:TR?= MnK4NlYzQTR5NEG=
A549 NUnlOYdzS2WubDD2bYFjcWyrdImgRZN{[Xl? M2TheFAvOS9zIN88US=> MnzoOFghcA>? M2n2dYVvcGGwY3XzJGVzdG:2aX7pZkBqdmS3Y3XkJJZq[WKrbHn0fUBtd3O| NFywcXIzPjB3M{CyNC=>
SGC-7901 NHL5W5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWCxJI5ONTFyIN88US=> MkfSO|IhcA>? NUjTWZYxUUN3MDDv[kA2NTFyIN88UUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NVjSPWt{OjV3N{[5NVU>
HGC-27 M4DDUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;UNUBvVS1zMDFOwG0> M3jOcVczKGh? NInZWYZKSzVyIH;mJFUuOTBizszNMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NUTuXXp{OjV3N{[5NVU>
MKN-28 Mnn0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWexJI5ONTFyIN88US=> NVTqR5BqPzJiaB?= NVT0NoREUUN3MDDv[kA2NTFyIN88UUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NVHmWoNZOjV3N{[5NVU>
NCI-N87 NFXVbHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXKNUBvVS1zMDFOwG0> MWe3NkBp M{HHZ2lEPTBib3[gOU0yOCEQvF2sJIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NX\MU5F6OjV3N{[5NVU>
KATOIII NF;1dJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWThV4QxOSCwTT2xNEDPxE1? M2PCPVczKGh? M2fCUmlEPTBib3[gNVAuOTByIH7NMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MoG0NlU2PzZ7MUW=
SNU-16 NFjxcXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUmxJI5ONTFyIN88US=> NWD6RnQ1PzJiaB?= NH3oOmpKSzVyIH;mJFExNTFyMDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NULVboJWOjV3N{[5NVU>
4T1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\oU2lEPTB;MD62OOKyOC5zMTFOwG0> MlS0NlQ3PDJ6OUO=
MDA-MB-468 M1\oc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlWyTWM2OD12LkpCtVAvQDVizszN M4Hn[lI1PjR{OEmz
HCT116 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfRU2VKSzVyPUG1MlnDuTFwOEKg{txO MXKyOFY1Ojh7Mx?=
SW620 Mn3ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3O2SWlEPTExvK6yNEDPxE1? NX7RNVM{OjR4NEK4PVM>
MDA-MB-231 NXeyZXRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPJTWM2OO,:nkKwJO69VQ>? Mn;1NlQ3PDJ6OUO=
CT26 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7hfVFKSzVy78{eNlAh|ryP Mmn3NlQ3PDJ6OUO=
SW480 Mm\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITvUVBKSzVy78{eNlAh|ryP Mn\wNlQ3PDJ6OUO=
4T1 MVLBdI9xfG:|aYOgRZN{[Xl? M4DhflEvOjVvMkCg{txO MYKyOEBp MVTpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MnThNlQ3PDJ6OUO=
KG1a M3rKPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTBwMEG4JO69VQ>? NIHPdW8zOjN4OUmyPC=>
Sum52-PE MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPLb2NSUUN3ME2wMlA1OSEQvF2= NYnpRmRIOjJ|Nkm5Nlg>
KMS11 NIe2XlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHZTWM2OD1yLkK4NUDPxE1? NWLvN2tUOjJ|Nkm5Nlg>
MCF7 NHvocHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHsb5FKSzVyPkOwJO69VQ>? MViyNlM3QTl{OB?=

... 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
  • Formulation: Formulated in a 1% (v/v) solution of polyoxyethylenesorbitan monooleate (Tween-80) in deionized water
  • 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

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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