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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In DMSO USD 220 In stock
USD 110 In stock
USD 170 In stock
USD 570 In stock
USD 870 In stock
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5 Customer Reviews

  • Ependymoma cells and neural stem cell line 1 (NSC1) controls treated with or AZD4547 for 72 h and assessed using an Alamar Blue stain. Error bars show s.d. Experiment performed as six technical replicates and replicated in biological triplicates.

    Nature, 2018, 553(7686):101-105. AZD4547 purchased from Selleck.

    A-431 and ACHN cells that are partially sensitive to the EGFR inhibitor gefitinib were treated with gefitinib, the FGFR inhibitor AZD-4547, or a combination of both. Error bars depict SEM of three experiments. Cell viability and proliferation assays showed that the combination of the drugs was more effective than single compounds.

    Science, 2017, doi: 10.1126/science.aan4368. AZD4547 purchased from Selleck.

  • (b) Representative pictures of Vim expression in four groups. Bars=20 μm. (c) A box plot graph showing the quantitative evaluation of Vim staining intensity. A plot of a box plot with whiskers extending from the 5th to the 95th percentile of all the score data was used. (d) Representative pictures of Sirius red staining in tumor samples from 32 nude mice. Sirius red staining showed the increased collagen fiber in TGF +AZD group. Bars=100 μm. Percentage of positive area to total area is quantified.

    Oncogene, 2017, 36(27):3831-3841. AZD4547 purchased from Selleck.

    FCM evaluating lung CD11b+/Gr1+ myeloid cells isolated from 4T1 tumor-bearing mice after 20 days of treatment with AZD4547 or control. Statistical significance was assessed by unpaired t test.

    Cell Physiol Biochem 2014 33(3), 633-45. AZD4547 purchased from Selleck.

  • Treatment of human CECs with of IL-1β (*, P < 0.01) and FGF2 (+, P < 0.01) resulted in enhanced cell migration as measured in a scratch-induced directional migration assay. Cotreatment with AZD4547 (AZD), an antagonist against FGF receptors 1 to 3, abolished the FGF2-enhanced (++, P < 0.01) but not the IL-1β-enhanced (P > 0.05) migration in human CECs. One-way ANOVA: F(4, 80) = 512, P < 0.00001, n =17 per sample. Tukey's post hoc test, HSD[0.05] = 10.9; HSD[0.01] = 13.1.

    Mol Cell Biol 2014 34(18), 3535-45. AZD4547 purchased from Selleck.

Purity & Quality Control

Choose Selective FGFR Inhibitors

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 NYLxflBxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYK3NkBp MX;JR|UxRTBwMEiyJO69VQ>? NV;HOJpzOjZ|NUGzNlA>
SK-HEP-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFH3Spc4OiCq NHXMbGRKSzVyPUCuNFg1KM7:TR?= MV:yOlM2OTN{MB?=
SNU475 NUe1VFNrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3:4OFczKGh? MUjJR|UxRTVwNDFOwG0> MYeyOlM2OTN{MB?=
Hep3B NEXkb3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\vTlczKGh? MnPhTWM2OD14LkSzJO69VQ>? NFvPZXozPjN3MUOyNC=>
PLC/PRF5 NEnS[lVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVW4[3o1PzJiaB?= MWXJR|UxRTZwNUWg{txO MUiyOlM2OTN{MB?=
Hur7 NFjCTFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVq3PYZrPzJiaB?= MnvaTWM2OD15LkK1JO69VQ>? MViyOlM2OTN{MB?=
HepG2 MnfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3wfG9DPzJiaB?= MnXiTWM2OD16LkezJO69VQ>? MkXWNlY{PTF|MkC=
SNU449 MX\DcI9vd2enbnnjJIF{e2G7 NWDuZYxkOSEEtV2= NGDnb4UzPCCq MY\k[YNz\WG|ZYOgZ49td267IH\vdo1ifGmxbjDzbYdvcW[rY3HueIx6 NYPDeHJ5OjZ|NUGzNlA>
SK-HEP-1 MYLDcI9vd2enbnnjJIF{e2G7 NX\NVWF[OSEEtV2= NH\jVGgzPCCq Mnni[IVkemWjc3XzJINwdG:weTDmc5Ju[XSrb36gd4lodmmoaXPhcpRtgQ>? M1XnbFI3OzVzM{Kw
SNU449 NXfud5NyTnWwY4Tpc44hSXO|YYm= MXWwMVIh|ryP MlK0OFghcA>? MmDEZ4F2e2W|IHGg[IVkemWjc3Wgc4YhTlKVMv-8kGFMXCxiYX7kJGVTUyCyaH;zdIhwenmuYYTpc44> NVjoXZliOjZ|NUGzNlA>
SK-HEP-1 Mn;sSpVv[3Srb36gRZN{[Xl? MonnNE0zKM7:TR?= NVm1[49TPDhiaB?= Mn\VZ4F2e2W|IHGg[IVkemWjc3Wgc4YhTlKVMv-8kGFMXCxiYX7kJGVTUyCyaH;zdIhwenmuYYTpc44> MXiyOlM2OTN{MB?=
BaF3 FLT3-TEL MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTHTVUxRTRwNjFCtUAxNjV5NzFOwG0> NXjhfmFlOjZ{OUS3OFE>
BaF3 RET-TEL MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3r1RWdKPTB;MD6zPUDDuSByLkC0PEDPxE1? Ml3LNlYzQTR5NEG=
BaF3 Parental M2XpO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX5W5B[T0l3MP-5qVExKM7:TR?= MVOyOlI6PDd2MR?=
MOLM14 FLT3/ITD Mk\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4riTGdKPTB;MD60PFQhyrFiMD6xOVch|ryP M1\HXFI3Ojl2N{Sx
MV4-11 FLT3/ITD MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGeyPHNIUTVyPUCuOFU6KMLzIECuNFQ3KM7:TR?= MUSyOlI6PDd2MR?=
TT RET C634W M{fCSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrHTVUxRTJwOTFCtUAxNjlyNDFOwG0> NEHIc5UzPjJ7NEe0NS=>
AN3-CA FGFR2 N550K, K310R NFvZfIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1SwZmdKPTB;MD6wN|EhyrFiMD6wNlMh|ryP NEfqXm4zPjJ7NEe0NS=>
MFE296 FGFR2 N550K M33HNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrsS2k2OD1yLkezNEDDuSByLkC1O{DPxE1? M3;VbFI3Ojl2N{Sx
MFE280 FGFR2 S252W NWDpbGNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfHTVUxRTBwMkG4JOKyKDBwMEezJO69VQ>? MWeyOlI6PDd2MR?=
Ishikawa FGFF2 over exp. NUGxdHZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEn6PVlIUTVyPUSuOUDDuSBzLkWxJO69VQ>? NGD0UY4zPjJ7NEe0NS=>
HEC1A Normal FGFR2 M1HnUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrLZpF3T0l3MP-5qVExKM7:TR?= M1jabVI3Ojl2N{Sx
A549 NGnx[VRE\WyuII\pZYJqdGm2eTDBd5NigQ>? MV6wMlEwOSEQvF2= MUi0PEBp M1vBdYVvcGGwY3XzJGVzdG:2aX7pZkBqdmS3Y3XkJJZq[WKrbHn0fUBtd3O| MY[yOlA2OzB{MB?=
SGC-7901 NUPDfXp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDhNUBvVS1zMDFOwG0> NFzLcZg4OiCq NYjJUGJ7UUN3MDDv[kA2NTFyIN88UUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NHrLdpIzPTV5NkmxOS=>
HGC-27 M{SxdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFS1WHMyKG6PLUGwJO69VQ>? M2TPU|czKGh? MnHhTWM2OCCxZjC1MVExKM7:TTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NHT0SZIzPTV5NkmxOS=>
MKN-28 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3QOoUyKG6PLUGwJO69VQ>? M2nPZlczKGh? M1\6XGlEPTBib3[gOU0yOCEQvF2sJIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MV:yOVU4PjlzNR?=
NCI-N87 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfQSZQyKG6PLUGwJO69VQ>? NVfEO4ZOPzJiaB?= NWfROHJ4UUN3MDDv[kA2NTFyIN88UUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NEm5[pUzPTV5NkmxOS=>
KATOIII MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPJNUBvVS1zMDFOwG0> NV3qSnNrPzJiaB?= M{jac2lEPTBib3[gNVAuOTByIH7NMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NFjN[HMzPTV5NkmxOS=>
SNU-16 Mn[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\nZnF1OSCwTT2xNEDPxE1? M{XMclczKGh? Ml60TWM2OCCxZjCxNE0yODBibl2sJIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NY[xfWplOjV3N{[5NVU>
4T1 NInjNWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLMUIZKSzVyPUCuOlTDuTBwMUGg{txO MkjrNlQ3PDJ6OUO=
MDA-MB-468 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PMdWlEPTB;ND65xtExNjh3IN88US=> NHzIfIYzPDZ2Mki5Ny=>
HCT116 NIPCclBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\yTYpxUUN3ME2xOU46yrFzLkiyJO69VQ>? Mn3vNlQ3PDJ6OUO=
SW620 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUmzVnoyUUN3MP-8olIxKM7:TR?= MUCyOFY1Ojh7Mx?=
MDA-MB-231 MlrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fpcGlEPTExvK6yNEDPxE1? NIrPc4szPDZ2Mki5Ny=>
CT26 NXS4WYZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zSWWlEPTExvK6yNEDPxE1? MWmyOFY1Ojh7Mx?=
SW480 NFrmUJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7YboppUUN3MP-8olIxKM7:TR?= M1HaN|I1PjR{OEmz
4T1 M2XTWWFxd3C2b4Ppd{BCe3OjeR?= M4LoeFEvOjVvMkCg{txO Mn3LNlQhcA>? NISyW3BqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NH7qb2czPDZ2Mki5Ny=>
KG1a M4rhWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTyPFVYUUN3ME2wMlAyQCEQvF2= MnfTNlI{Pjl7Mki=
Sum52-PE M4iwdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXETWM2OD1yLkC0NUDPxE1? NILMVlkzOjN4OUmyPC=>
KMS11 NIq1PYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnzT5dKSzVyPUCuNlgyKM7:TR?= MkS2NlI{Pjl7Mki=
MCF7 MlK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRjNyIN88US=> MWSyNlM3QTl{OB?=

... Click to View More Cell Line Experimental Data

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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02824133 Suspended 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 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 Gastric Cancer|Oesophageal Cancer|Breast Cancer|Squamous Cell Carcinoma of the Lung Royal Marsden NHS Foundation Trust|AstraZeneca September 2012 Phase 2
NCT01791985 Active not recruiting Breast Cancer Imperial College London|Cancer Research UK|AstraZeneca July 2012 Phase 1|Phase 2
NCT01457846 Terminated Gastro-oesophageal Junction Cancer|Gastric Cancer AstraZeneca November 2011 Phase 2
NCT01202591 Completed FGFR Inhibition Pharmacokinetics Biomarkers|ER+ Breast Cancer AstraZeneca December 2010 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID