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.

Size Price Stock Quantity  
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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2 Customer Reviews

  • 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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NICw[WFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnf3O|IhcA>? NVfldIY2UUN3ME2wMlA5OiEQvF2= NFmxPYczPjN3MUOyNC=>
SK-HEP-1 NGL4NnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfzO|IhcA>? M{LDPGlEPTB;MD6wPFQh|ryP MXWyOlM2OTN{MB?=
SNU475 Mmm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfpSpM5PzJiaB?= M{PzXGlEPTB;NT60JO69VQ>? MUOyOlM2OTN{MB?=
Hep3B MmruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnFO3M4OiCq M3Xp[GlEPTB;Nj60N{DPxE1? MWSyOlM2OTN{MB?=
PLC/PRF5 NHuzWpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUS3NkBp MXXJR|UxRTZwNUWg{txO M335OFI3OzVzM{Kw
Hur7 MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXG3NkBp M{jQbmlEPTB;Nz6yOUDPxE1? M{nSSlI3OzVzM{Kw
HepG2 M2XE[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrJXIg4OiCq M2DGU2lEPTB;OD63N{DPxE1? NULibGVROjZ|NUGzNlA>
SNU449 NU\CVoVLS2yxbn;n[Y5q[yCjc4PhfS=> MXSxJOK2VQ>? NFzaXZkzPCCq NX6zZZBJ\GWlcnXhd4V{KGOxbH;ufUBnd3KvYYTpc44he2mpbnnmbYNidnSueR?= M3zIbFI3OzVzM{Kw
SK-HEP-1 NXjWVZFkS2yxbn;n[Y5q[yCjc4PhfS=> NE\HNXAyKML3TR?= M4fhdlI1KGh? Mmru[IVkemWjc3XzJINwdG:weTDmc5Ju[XSrb36gd4lodmmoaXPhcpRtgQ>? Ml7WNlY{PTF|MkC=
SNU449 NWDtU2lQTnWwY4Tpc44hSXO|YYm= MoDiNE0zKM7:TR?= NIfLPI41QCCq NVvVbYxC[2G3c3XzJIEh\GWlcnXhd4Uhd2ZiRmLTNw+9lEGNVDygZY5lKEWUSzDwbI9{eGixconsZZRqd25? NFLmVlMzPjN3MUOyNC=>
SK-HEP-1 NY\PSmtqTnWwY4Tpc44hSXO|YYm= M{nlSVAuOiEQvF2= M3PIVlQ5KGh? MUnjZZV{\XNiYTDk[YNz\WG|ZTDv[kBHWlN{78{MRWtVNCCjbnSgSXJMKHCqb4PwbI9zgWyjdHnvci=> NXSzSVVKOjZ|NUGzNlA>
BaF3 FLT3-TEL NVjRSG4yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXHTVUxRTRwNjFCtUAxNjV5NzFOwG0> MojDNlYzQTR5NEG=
BaF3 RET-TEL M4XKSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTrS2k2OD1yLkO5JOKyKDBwMES4JO69VQ>? NYLMRlMxOjZ{OUS3OFE>
BaF3 Parental MoHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnxS3VTT0l3MP-5qVExKM7:TR?= NEnZ[ngzPjJ7NEe0NS=>
MOLM14 FLT3/ITD M{joSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPDS2k2OD1yLkS4OEDDuSByLkG1O{DPxE1? MYiyOlI6PDd2MR?=
MV4-11 FLT3/ITD M2K5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;2N2N1T0l3ME2wMlQ2QSEEsTCwMlA1PiEQvF2= NUfGZVFTOjZ{OUS3OFE>
TT RET C634W MmnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHubFlIUTVyPUKuPUDDuSByLkmwOEDPxE1? MlPGNlYzQTR5NEG=
AN3-CA FGFR2 N550K, K310R M4myXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrHTVUxRTBwMEOxJOKyKDBwMEKzJO69VQ>? Ml\INlYzQTR5NEG=
MFE296 FGFR2 N550K MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\BXmdKPTB;MD63N|AhyrFiMD6wOVch|ryP NY\0dWNGOjZ{OUS3OFE>
MFE280 FGFR2 S252W MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\LWW1IUTVyPUCuNlE5KMLzIECuNFc{KM7:TR?= NWHne5NOOjZ{OUS3OFE>
Ishikawa FGFF2 over exp. M{TsR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLHTVUxRTRwNTFCtUAyNjVzIN88US=> MlnXNlYzQTR5NEG=
HEC1A Normal FGFR2 NXXMO|hXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfHXZZIUTVy78olNVAh|ryP NI\yeYEzPjJ7NEe0NS=>
A549 Mly3R4VtdCC4aXHibYxqfHliQYPzZZk> NXK0S25NOC5zL{Gg{txO MWC0PEBp NFrkVXJmdmijbnPld{BGemyxdHnubYIhcW6mdXPl[EB3cWGkaXzpeJkhdG:|cx?= MnfKNlYxPTNyMkC=
SGC-7901 NX:0VnBJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnMfmFYOSCwTT2xNEDPxE1? MX:3NkBp MnW3TWM2OCCxZjC1MVExKM7:TTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MXGyOVU4PjlzNR?=
HGC-27 NFTiSXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX22SVB5OSCwTT2xNEDPxE1? Ml24O|IhcA>? NYLRN|E2UUN3MDDv[kA2NTFyIN88UUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NXvYXFl2OjV3N{[5NVU>
MKN-28 MnO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHr[XkyKG6PLUGwJO69VQ>? MXO3NkBp Ml;pTWM2OCCxZjC1MVExKM7:TTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NUDtcmk3OjV3N{[5NVU>
NCI-N87 NEPHUoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjXbXhpOSCwTT2xNEDPxE1? NHjYZZY4OiCq MUPJR|UxKG:oIEWtNVAh|ryPLDDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NXXBe4RwOjV3N{[5NVU>
KATOIII NI\XVFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEmxUYIyKG6PLUGwJO69VQ>? MlfsO|IhcA>? MX3JR|UxKG:oIEGwMVExOCCwTTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NXXBWo9pOjV3N{[5NVU>
SNU-16 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXH2TIo4OSCwTT2xNEDPxE1? MkLQO|IhcA>? MkPvTWM2OCCxZjCxNE0yODBibl2sJIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MVKyOVU4PjlzNR?=
4T1 NEexbYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mon6TWM2OD1yLk[0xtExNjFzIN88US=> NXnEVWt5OjR4NEK4PVM>
MDA-MB-468 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7DZYFKSzVyPUSuPeKyOC56NTFOwG0> MkL2NlQ3PDJ6OUO=
HCT116 NVj3Z|U4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\2[4VKSzVyPUG1MlnDuTFwOEKg{txO NVjYR2ZFOjR4NEK4PVM>
SW620 M4r0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3v2TGlEPTExvK6yNEDPxE1? NWLL[VNJOjR4NEK4PVM>
MDA-MB-231 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|Ux97zgMkCg{txO MlHaNlQ3PDJ6OUO=
CT26 NFLSfFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXH1NHZ{UUN3MP-8olIxKM7:TR?= NHfRcmczPDZ2Mki5Ny=>
SW480 NWHPNlhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlj5TWM2OO,:nkKwJO69VQ>? NV\MOIFUOjR4NEK4PVM>
4T1 MWHBdI9xfG:|aYOgRZN{[Xl? NXL1T2lXOS5{NT2yNEDPxE1? M1raOVI1KGh? NHXz[W9qdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NYXLPGJiOjR4NEK4PVM>
KG1a NFvYeXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTBwMEG4JO69VQ>? M1rSOlIzOzZ7OUK4
Sum52-PE M4e0Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX20SYE3UUN3ME2wMlA1OSEQvF2= NIDyTFIzOjN4OUmyPC=>
KMS11 NHHMXZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTBwMkixJO69VQ>? NFPvNVYzOjN4OUmyPC=>
MCF7 M3L2emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[2SFl5UUN3ME6zNEDPxE1? NYnEclBxOjJ|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
+ 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
+ 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
+ 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% 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 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 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|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
NCT02117167 Recruiting Non-small Cell Lung Cancer Metastatic UNICANCER|IFCT|Fondation ARC|AstraZeneca April 2014 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID