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.

    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.

  • 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.

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 Mmr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzFOYdUPzJiaB?= MmHpTWM2OD1yLkC4NkDPxE1? NVXB[nRYOjZ|NUGzNlA>
SK-HEP-1 NFX1cGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHxO|IhcA>? NFvRNFNKSzVyPUCuNFg1KM7:TR?= NW\Cfmp2OjZ|NUGzNlA>
SNU475 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjvXmFtPzJiaB?= MnLZTWM2OD13LkSg{txO NV60[JhwOjZ|NUGzNlA>
Hep3B M1ixd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13ZUVczKGh? MoDRTWM2OD14LkSzJO69VQ>? M33Eb|I3OzVzM{Kw
PLC/PRF5 MmnLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTrV2k3PzJiaB?= MnjXTWM2OD14LkW1JO69VQ>? MlrVNlY{PTF|MkC=
Hur7 NVzWXXdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXKfG44OiCq NVLWSXpbUUN3ME23MlI2KM7:TR?= Mn[4NlY{PTF|MkC=
HepG2 NF73eopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHUR4RFPzJiaB?= M4X5PWlEPTB;OD63N{DPxE1? MXSyOlM2OTN{MB?=
SNU449 NFvQb4ZEdG:wb3flcolkKGG|c3H5 M2nJRVEhyrWP MUSyOEBp MVPk[YNz\WG|ZYOgZ49td267IH\vdo1ifGmxbjDzbYdvcW[rY3HueIx6 Mmj6NlY{PTF|MkC=
SK-HEP-1 MljLR4xwdm:pZX7pZ{Bie3OjeR?= M1fYeVEhyrWP M4X1XFI1KGh? NXm4bVA4\GWlcnXhd4V{KGOxbH;ufUBnd3KvYYTpc44he2mpbnnmbYNidnSueR?= MnL3NlY{PTF|MkC=
SNU449 NHHyOGxHfW6ldHnvckBCe3OjeR?= Ml3ONE0zKM7:TR?= NGnUd5A1QCCq M3LDV4NifXOnczDhJIRm[3KnYYPlJI9nKE[UU{NvwKxCU1RuIHHu[EBGWkticHjvd5Bpd3K7bHH0bY9v NULaR5lQOjZ|NUGzNlA>
SK-HEP-1 NH;Y[21HfW6ldHnvckBCe3OjeR?= MYGwMVIh|ryP M1X0UVQ5KGh? NHfIWFJk[XW|ZYOgZUBl\WO{ZXHz[UBw\iCIUmOy89yNSUuWLDDhcoQhTVKNIIDoc5NxcG:{eXzheIlwdg>? MUWyOlM2OTN{MB?=
BaF3 FLT3-TEL Mn\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXHTVUxRTRwNjFCtUAxNjV5NzFOwG0> NFPa[4kzPjJ7NEe0NS=>
BaF3 RET-TEL NIn3RndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fwT2dKPTB;MD6zPUDDuSByLkC0PEDPxE1? MUGyOlI6PDd2MR?=
BaF3 Parental MoDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4i1OGdKPTExubWxNEDPxE1? M{fT[VI3Ojl2N{Sx
MOLM14 FLT3/ITD NVz5dpFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoD5S2k2OD1yLkS4OEDDuSByLkG1O{DPxE1? MY[yOlI6PDd2MR?=
MV4-11 FLT3/ITD MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfHTVUxRTBwNEW5JOKyKDBwMES2JO69VQ>? MmDwNlYzQTR5NEG=
TT RET C634W M{TNZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HKc2dKPTB;Mj65JOKyKDBwOUC0JO69VQ>? NYXOe41lOjZ{OUS3OFE>
AN3-CA FGFR2 N550K, K310R NH:wR3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDiO|VIUTVyPUCuNFMyKMLzIECuNFI{KM7:TR?= MUKyOlI6PDd2MR?=
MFE296 FGFR2 N550K Mk\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TnUGdKPTB;MD63N|AhyrFiMD6wOVch|ryP M4XSbVI3Ojl2N{Sx
MFE280 FGFR2 S252W NFmwdodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLPS2k2OD1yLkKxPEDDuSByLkC3N{DPxE1? NHHvTW0zPjJ7NEe0NS=>
Ishikawa FGFF2 over exp. MkjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7HTVUxRTRwNTFCtUAyNjVzIN88US=> MojvNlYzQTR5NEG=
HEC1A Normal FGFR2 NUnNOnpJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nnTmdKPTExubWxNEDPxE1? NXriNVJXOjZ{OUS3OFE>
A549 MUjD[YxtKH[rYXLpcIl1gSCDc4PhfS=> MWSwMlEwOSEQvF2= MYq0PEBp MXzlcohidmOnczDFdoxwfGmwaXKgbY5lfWOnZDD2bYFjcWyrdImgcI9{ew>? M1X6[FI3ODV|MEKw
SGC-7901 MmKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDwOY0yKG6PLUGwJO69VQ>? Mn\IO|IhcA>? NVPUVIlPUUN3MDDv[kA2NTFyIN88UUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NITOdJIzPTV5NkmxOS=>
HGC-27 MnnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\RemxEOSCwTT2xNEDPxE1? NEXvZpk4OiCq MnfVTWM2OCCxZjC1MVExKM7:TTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NUHOfI9SOjV3N{[5NVU>
MKN-28 M3:1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2H0[|Ehdk1vMUCg{txO NG\PWYo4OiCq MlrXTWM2OCCxZjC1MVExKM7:TTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NFj3VYkzPTV5NkmxOS=>
NCI-N87 M37KbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzHVFYyKG6PLUGwJO69VQ>? Mo[5O|IhcA>? MUfJR|UxKG:oIEWtNVAh|ryPLDDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MViyOVU4PjlzNR?=
KATOIII NHvHRVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XZdFEhdk1vMUCg{txO NFvodmg4OiCq Mlz4TWM2OCCxZjCxNE0yODBibl2sJIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M{W2RVI2PTd4OUG1
SNU-16 Mne4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWCxJI5ONTFyIN88US=> NF;tfG04OiCq NGq5UFlKSzVyIH;mJFExNTFyMDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NWrDOnltOjV3N{[5NVU>
4T1 MlzxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPK[4NZUUN3ME2wMlY1yrFyLkGxJO69VQ>? MWGyOFY1Ojh7Mx?=
MDA-MB-468 NFfJXmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTRwOdMxNE45PSEQvF2= NUO2W5loOjR4NEK4PVM>
HCT116 NHPlUmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTabIxKSzVyPUG1MlnDuTFwOEKg{txO NFfEV2wzPDZ2Mki5Ny=>
SW620 MoX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfvRm9KSzVy78{eNlAh|ryP MnnNNlQ3PDJ6OUO=
MDA-MB-231 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|Ux97zgMkCg{txO M2TWWVI1PjR{OEmz
CT26 M{LtUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\yNXZKSzVy78{eNlAh|ryP NV3D[5FNOjR4NEK4PVM>
SW480 NHH6eWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoO5TWM2OO,:nkKwJO69VQ>? M16w[lI1PjR{OEmz
4T1 M3;kXGFxd3C2b4Ppd{BCe3OjeR?= NEj3cnIyNjJ3LUKwJO69VQ>? NHjMXnkzPCCq NIHt[nRqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MYSyOFY1Ojh7Mx?=
KG1a NXTaSoN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjQTWM2OD1yLkCxPEDPxE1? NHz0cpEzOjN4OUmyPC=>
Sum52-PE M3LDemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljzTWM2OD1yLkC0NUDPxE1? M4DMb|IzOzZ7OUK4
KMS11 NUPhW4s6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF:2UlhKSzVyPUCuNlgyKM7:TR?= MUWyNlM3QTl{OB?=
MCF7 NX3pSmkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;iTWM2OD5|MDFOwG0> NVO3OXA2OjJ|Nkm5Nlg>

... 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
NCT02546661 Recruiting Muscle Invasive Bladder Cancer AstraZeneca October 2016 Phase 1
NCT02824133 Recruiting 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
NCT02465060 Recruiting Advanced Malignant Neoplasm|Lymphoma|Recurrent Plasma Cell Myeloma|Recurrent Solid Neoplasm|Refractory Malignant Neoplasm|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) August 2015 Phase 2
NCT02664935 Recruiting Non-Small Cell Lung Cancer|Carcinoma, Squamous Cell|Adenocarcinoma University of Birmingham|Cancer Research UK|AstraZeneca|Pfizer|Experimental Cancer Medicine Centre Network March 2015 Phase 2
NCT02965378 Active, not recruiting Recurrent Squamous Cell Lung Carcinoma|Stage IV Squamous Cell Lung Carcinoma Southwest Oncology Group|National Cancer Institute (NCI) June 2014 Phase 2|Phase 3
NCT02154490 Recruiting Recurrent Squamous Cell Lung Carcinoma|Stage IV Squamous Cell Lung Carcinoma Southwest Oncology Group|National Cancer Institute (NCI) June 2014 Phase 2|Phase 3

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Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID