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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3 Customer Reviews

  • (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. 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.

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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)
FGFR4 [1]
(Cell-free assay)
0.2 nM 1.8 nM 2.5 nM 24 nM 165 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 M4XLZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfiVWo4OiCq NID4OVJKSzVyPUCuNFgzKM7:TR?= M1fqXlI3OzVzM{Kw
SK-HEP-1 NEW3WY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoC4O|IhcA>? M{LUUWlEPTB;MD6wPFQh|ryP NUDLVFN7OjZ|NUGzNlA>
SNU475 M1K4cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXi3NkBp M2[2VmlEPTB;NT60JO69VQ>? M1XJNFI3OzVzM{Kw
Hep3B Ml[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[3NkBp M1v1TmlEPTB;Nj60N{DPxE1? NG\ofnkzPjN3MUOyNC=>
PLC/PRF5 NEDx[pJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHD[Fc4OiCq NUXq[HNoUUN3ME22MlU2KM7:TR?= MoDHNlY{PTF|MkC=
Hur7 NHTBR3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;0flczKGh? MnS1TWM2OD15LkK1JO69VQ>? MkjWNlY{PTF|MkC=
HepG2 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfSVlY4PzJiaB?= MUDJR|UxRThwN{Og{txO MVmyOlM2OTN{MB?=
SNU449 NYDFdYtyS2yxbn;n[Y5q[yCjc4PhfS=> MYWxJOK2VQ>? MWCyOEBp NIG2[JRl\WO{ZXHz[ZMh[2:ub375JIZwem2jdHnvckB{cWewaX\pZ4FvfGy7 NYLjRldXOjZ|NUGzNlA>
SK-HEP-1 NHXwXnpEdG:wb3flcolkKGG|c3H5 MlnlNUDDvU1? MVSyOEBp MWfk[YNz\WG|ZYOgZ49td267IH\vdo1ifGmxbjDzbYdvcW[rY3HueIx6 NXz3Nlh4OjZ|NUGzNlA>
SNU449 NGXMfJdHfW6ldHnvckBCe3OjeR?= MX[wMVIh|ryP NYHyXlVjPDhiaB?= M4rST4NifXOnczDhJIRm[3KnYYPlJI9nKE[UU{NvwKxCU1RuIHHu[EBGWkticHjvd5Bpd3K7bHH0bY9v NX3hcI1MOjZ|NUGzNlA>
SK-HEP-1 M4PHU2Z2dmO2aX;uJGF{e2G7 NHG4[|cxNTJizszN M4OycFQ5KGh? NILEU2pk[XW|ZYOgZUBl\WO{ZXHz[UBw\iCIUmOy89yNSUuWLDDhcoQhTVKNIIDoc5NxcG:{eXzheIlwdg>? NX\3PXppOjZ|NUGzNlA>
BaF3 FLT3-TEL NIGwNWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnHTVUxRTRwNjFCtUAxNjV5NzFOwG0> NFLSW|MzPjJ7NEe0NS=>
BaF3 RET-TEL NV7XZ2I1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnHTVUxRTBwM{mgxtEhOC5yNEig{txO MmXrNlYzQTR5NEG=
BaF3 Parental Mkn6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHtdG5IUTVy78olNVAh|ryP NUTve4ZWOjZ{OUS3OFE>
MOLM14 FLT3/ITD NV\tR49MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVexendRT0l3ME2wMlQ5PCEEsTCwMlE2PyEQvF2= M{TnU|I3Ojl2N{Sx
MV4-11 FLT3/ITD NUH1[mJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DSTGdKPTB;MD60OVkhyrFiMD6wOFYh|ryP MU[yOlI6PDd2MR?=
TT RET C634W MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfF[o5IUTVyPUKuPUDDuSByLkmwOEDPxE1? MUSyOlI6PDd2MR?=
AN3-CA FGFR2 N550K, K310R NGixO4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XiUGdKPTB;MD6wN|EhyrFiMD6wNlMh|ryP MU[yOlI6PDd2MR?=
MFE296 FGFR2 N550K NXTsUI8yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHnboNTT0l3ME2wMlc{OCEEsTCwMlA2PyEQvF2= NIjETJgzPjJ7NEe0NS=>
MFE280 FGFR2 S252W MmLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjwUW9IUTVyPUCuNlE5KMLzIECuNFc{KM7:TR?= MXmyOlI6PDd2MR?=
Ishikawa FGFF2 over exp. M2nQbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjHTVUxRTRwNTFCtUAyNjVzIN88US=> MmDENlYzQTR5NEG=
HEC1A Normal FGFR2 NIqzdJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnIdJNIUTVy78olNVAh|ryP M{S5S|I3Ojl2N{Sx
A549 MkX5R4VtdCC4aXHibYxqfHliQYPzZZk> NIXqSHUxNjFxMTFOwG0> M{fsO|Q5KGh? M1KzcIVvcGGwY3XzJGVzdG:2aX7pZkBqdmS3Y3XkJJZq[WKrbHn0fUBtd3O| MmHJNlYxPTNyMkC=
SGC-7901 M2WyT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvjNUBvVS1zMDFOwG0> M17uS|czKGh? MUPJR|UxKG:oIEWtNVAh|ryPLDDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MXiyOVU4PjlzNR?=
HGC-27 MofUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzYUmpLOSCwTT2xNEDPxE1? NVLxUmFZPzJiaB?= M1LHW2lEPTBib3[gOU0yOCEQvF2sJIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MmHrNlU2PzZ7MUW=
MKN-28 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrw[ZQyKG6PLUGwJO69VQ>? MnvRO|IhcA>? NWLhXFN[UUN3MDDv[kA2NTFyIN88UUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= Mk\nNlU2PzZ7MUW=
NCI-N87 NXfGPVhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3qNUBvVS1zMDFOwG0> MlPjO|IhcA>? NI\FVI1KSzVyIH;mJFUuOTBizszNMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MlSzNlU2PzZ7MUW=
KATOIII MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXnW|cyKG6PLUGwJO69VQ>? MnLDO|IhcA>? NHnRNXlKSzVyIH;mJFExNTFyMDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NFXLcI0zPTV5NkmxOS=>
SNU-16 M4ruVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjlbXduOSCwTT2xNEDPxE1? M2Dy[FczKGh? NVTnPGtyUUN3MDDv[kAyOC1zMECgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= NWG3SoFrOjV3N{[5NVU>
4T1 NWrle|VwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;FTWM2OD1yLk[0xtExNjFzIN88US=> NUfkUVBKOjR4NEK4PVM>
MDA-MB-468 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPJNm5KSzVyPUSuPeKyOC56NTFOwG0> M3PkWVI1PjR{OEmz
HCT116 M335UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrBdnhKSzVyPUG1MlnDuTFwOEKg{txO M{Pid|I1PjR{OEmz
SW620 Mk[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vBcGlEPTExvK6yNEDPxE1? M{LMT|I1PjR{OEmz
MDA-MB-231 MoDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDRTWM2OO,:nkKwJO69VQ>? NG\Fb|EzPDZ2Mki5Ny=>
CT26 NHjDRWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPod3BbUUN3MP-8olIxKM7:TR?= MWiyOFY1Ojh7Mx?=
SW480 NWTMTW5iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnewTWM2OO,:nkKwJO69VQ>? MUOyOFY1Ojh7Mx?=
4T1 M1mwSGFxd3C2b4Ppd{BCe3OjeR?= M2\lWVEvOjVvMkCg{txO NFvGO|kzPCCq NGnCZZhqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NFXDWYwzPDZ2Mki5Ny=>
KG1a MlL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonETWM2OD1yLkCxPEDPxE1? M3X2O|IzOzZ7OUK4
Sum52-PE NYTLPZk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF2yWWtKSzVyPUCuNFQyKM7:TR?= M4nPcFIzOzZ7OUK4
KMS11 M4DSW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe2ZVNKSzVyPUCuNlgyKM7:TR?= NXvPRYJuOjJ|Nkm5Nlg>
MCF7 NED3cY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRjNyIN88US=> M3e0d|IzOzZ7OUK4

... 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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID