AZD4547

Catalog No.S2801

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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AZD4547 Chemical Structure

AZD4547 Chemical Structure
Molecular Weight: 463.57

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  • Research Area
  • Inhibition Profile

Product Description

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.
Targets FGFR1 [1]
(Cell-free assay)
FGFR3 [1]
(Cell-free assay)
FGFR2 [1]
(Cell-free assay)
KDR [1]
(Cell-free assay)

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IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
SNU449NIrxNlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M{nnd|czKGh?NWD0SHFJUUN3ME2wMlA5OiEQvF2=NI\LPVMzPjN3MUOyNC=>
SK-HEP-1NEfGd4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Ml71O|IhcA>?Mn:wTWM2OD1yLkC4OEDPxE1?M2HGelI3OzVzM{Kw
SNU475MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MmO1O|IhcA>?MkjtTWM2OD13LkSg{txONYPHNYFKOjZ|NUGzNlA>
Hep3BNXnNUYl5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NWnnUoRrPzJiaB?=MXLJR|UxRTZwNEOg{txONVK2UVJ7OjZ|NUGzNlA>
PLC/PRF5MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXi3NkBpMlvyTWM2OD14LkW1JO69VQ>?MWGyOlM2OTN{MB?=
Hur7MlPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MWK3NkBpMV\JR|UxRTdwMkWg{txONIn3Uo0zPjN3MUOyNC=>
HepG2NUPRXGZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVW3NkBpM1fFRWlEPTB;OD63N{DPxE1?NUjY[mZGOjZ|NUGzNlA>
SNU449MkH2R4xwdm:pZX7pZ{Bie3OjeR?=M17jNFEhyrWPMUCyOEBpMmfG[IVkemWjc3XzJINwdG:weTDmc5Ju[XSrb36gd4lodmmoaXPhcpRtgQ>?M3\rWVI3OzVzM{Kw
SK-HEP-1M4LUU2Ntd26xZ3XubYMh[XO|YYm=M2TkW|EhyrWPMknGNlQhcA>?M2HRSoRm[3KnYYPld{Bkd2yxbomg[o9zdWG2aX;uJJNq\26rZnnjZY51dHl?NVrYbW5NOjZ|NUGzNlA>
SNU449MlzKSpVv[3Srb36gRZN{[Xl?NV3IepJmOC1{IN88US=>M4DNTlQ5KGh?NFPDb|Vk[XW|ZYOgZUBl\WO{ZXHz[UBw\iCIUmOy89yNSUuWLDDhcoQhTVKNIIDoc5NxcG:{eXzheIlwdg>?NYDP[FByOjZ|NUGzNlA>
SK-HEP-1Mke4SpVv[3Srb36gRZN{[Xl?MVWwMVIh|ryPNGWxOoQ1QCCqMl\mZ4F2e2W|IHGg[IVkemWjc3Wgc4YhTlKVMv-8kGFMXCxiYX7kJGVTUyCyaH;zdIhwenmuYYTpc44>NEjuU5YzPjN3MUOyNC=>
BaF3 FLT3-TELMnHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NYHIeZo{T0l3ME20MlYhyrFiMD61O|ch|ryPNGjuSFEzPjJ7NEe0NS=>
BaF3 RET-TELMX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXHHTVUxRTBwM{mgxtEhOC5yNEig{txONFrRcYQzPjJ7NEe0NS=>
BaF3 ParentalMUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MV\HTVUx97nnMUCg{txOMkTyNlYzQTR5NEG=
MOLM14 FLT3/ITDNI\WRVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MX7HTVUxRTBwNEi0JOKyKDBwMUW3JO69VQ>?Mlf2NlYzQTR5NEG=
MV4-11 FLT3/ITDMnjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MmjVS2k2OD1yLkS1PUDDuSByLkC0OkDPxE1?MUSyOlI6PDd2MR?=
TT RET C634WM{TVZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXz1U5luT0l3ME2yMlkhyrFiMD65NFQh|ryPM4jrNFI3Ojl2N{Sx
AN3-CA FGFR2 N550K, K310RMXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MoH4S2k2OD1yLkCzNUDDuSByLkCyN{DPxE1?MUeyOlI6PDd2MR?=
MFE296 FGFR2 N550KNFvvc3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NGrM[IhIUTVyPUCuO|MxKMLzIECuNFU4KM7:TR?=MkHoNlYzQTR5NEG=
MFE280 FGFR2 S252WNGPEcHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MXnHTVUxRTBwMkG4JOKyKDBwMEezJO69VQ>?M2fGPVI3Ojl2N{Sx
Ishikawa FGFF2 over exp.Mn7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NWn6SnMyT0l3ME20MlUhyrFiMT61NUDPxE1?MYWyOlI6PDd2MR?=
HEC1A Normal FGFR2M4TZRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M{LWfmdKPTExubWxNEDPxE1?MYKyOlI6PDd2MR?=
A549M4P4OGNmdGxidnnhZoltcXS7IFHzd4F6MnjxNE4yNzFizszNMYG0PEBpMlnm[Y5p[W6lZYOgSZJtd3SrbnniJIlv\HWlZXSgeoli[mmuaYT5JIxwe3N?Ml7uNlYxPTNyMkC=
SGC-7901NFS1SXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MVSxJI5ONTFyIN88US=>NVTpRpdRPzJiaB?=MYHJR|UxKG:oIEWtNVAh|ryPLDDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6M4Hjb|I2PTd4OUG1
HGC-27NWXaTJZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NV;1SVZbOSCwTT2xNEDPxE1?NVvxenFiPzJiaB?=NIPjXo9KSzVyIH;mJFUuOTBizszNMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7NWPEUFhuOjV3N{[5NVU>
MKN-28NEe5NmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NW\DbI9OOSCwTT2xNEDPxE1?MUm3NkBpMYTJR|UxKG:oIEWtNVAh|ryPLDDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6MkX3NlU2PzZ7MUW=
NCI-N87MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NG\s[mQyKG6PLUGwJO69VQ>?Ml72O|IhcA>?Mnu4TWM2OCCxZjC1MVExKM7:TTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?M1O2UFI2PTd4OUG1
KATOIIIM2PmXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MorRNUBvVS1zMDFOwG0>MoGxO|IhcA>?NXvYS3dxUUN3MDDv[kAyOC1zMECgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm=NYjqXlByOjV3N{[5NVU>
SNU-16NWOxd3dDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NH;l[JMyKG6PLUGwJO69VQ>?NUXjbnFCPzJiaB?=NXXGV2NWUUN3MDDv[kAyOC1zMECgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm=NWjI[pBTOjV3N{[5NVU>
4T1NFyxU2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Ml2zTWM2OD1yLk[0xtExNjFzIN88US=>M2nxV|I1PjR{OEmz
MDA-MB-468NGHCVZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NF7JdGlKSzVyPUSuPeKyOC56NTFOwG0>NYrSTFI6OjR4NEK4PVM>
HCT116NFPrOmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXTESWJUUUN3ME2xOU46yrFzLkiyJO69VQ>?M2PSdFI1PjR{OEmz
SW620M324T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NInaU|ZKSzVy78{eNlAh|ryPNIHiPY4zPDZ2Mki5Ny=>
MDA-MB-231MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXjUdW1WUUN3MP-8olIxKM7:TR?=MlvLNlQ3PDJ6OUO=
CT26MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NFzEfWlKSzVy78{eNlAh|ryPNGPLRpgzPDZ2Mki5Ny=>
SW480Mn;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NUX3UJF6UUN3MP-8olIxKM7:TR?=NWrLcHp3OjR4NEK4PVM>
4T1MlyxRZBweHSxc3nzJGF{e2G7MlfYNU4zPS1{MDFOwG0>NXfNS41iOjRiaB?=NF62eXdqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5M{TrelI1PjR{OEmz
KG1aM3rUOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVTJR|UxRTBwMEG4JO69VQ>?MWCyNlM3QTl{OB?=
Sum52-PEMmfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NUHqUI1sUUN3ME2wMlA1OSEQvF2=MoDvNlI{Pjl7Mki=
KMS11MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NVLScGlVUUN3ME2wMlI5OSEQvF2=NEm0NmczOjN4OUmyPC=>
MCF7M1LQNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NEXveWFKSzVyPkOwJO69VQ>?NYXyRXQzOjJ|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]
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.

Protocol(Only for Reference)

Kinase Assay: [1]

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 Assay: [1]

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.

Animal Study: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Gavine PR, et al. Cancer Res, 2012, 72(8), 2045-2056.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02546661 Not yet recruiting Muscle Invasive Bladder Cancer AstraZeneca August 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|Refractory Malignant Neoplasm|Solid Neoplasm 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|P  ...more University of Birmingham|Cancer Research UK|AstraZeneca|Pfizer|Experimental Cancer Medicine Centre Network March 2015 Phase 2
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

view more

Chemical Information

Download AZD4547 SDF
Molecular Weight (MW) 463.57
Formula

C26H33N5O3

CAS No. 1035270-39-3
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 92 mg/mL (198.45 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+PEG 300+5% Tween 80+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name N-(5-(3,5-dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3S,5R)-3,5-dimethylpiperazin-1-yl)benzamide

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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