製品番号: HY-13330

Fexagratinib

(別名: AZD4547; ADSK091)

36 Cited Publications

カスタマーレビュー

Based on 36 publication(s) in Google Scholar

Fexagratinib (AZD4547; ADSK091) is a potent inhibitor of the FGFR family with IC₅₀s of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

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純度: 99.92%
CAS 番号: 1035270-39-3
分子式: C₂₆H₃₃N₅O₃
分子量:463.57

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Fexagratinib 構造式

CAS 番号: 1035270-39-3

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Amount: USD 0.00

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (36)
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生物活性

製品説明

Fexagratinib (AZD4547; ADSK091) is a potent inhibitor of the FGFR family with IC₅₀s of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

IC₅₀ & Target^[1]

FGFR1

0.2 nM (IC₅₀)

FGFR2

2.5 nM (IC₅₀)

FGFR3

1.8 nM (IC₅₀)

FGFR4

165 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.062 μM Compound: AZD4547	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 25736993]
B16-F10	IC₅₀	0.051 μM Compound: AZD4547	Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay	[PMID: 25736993]
BaF3	IC₅₀	222 nM Compound: 1; AZD-4547	Antiproliferative activity against mouse BAF3 cells expressing VEGFR2 after 72 hrs Antiproliferative activity against mouse BAF3 cells expressing VEGFR2 after 72 hrs	[PMID: 29775937]
BaF3	IC₅₀	339.2 nM Compound: 1; AZD-4547	Antiproliferative activity against mouse BAF3 cells expressing TEL-fused FGFR4 kinase after 72 hrs by CCK8 or MTT assay Antiproliferative activity against mouse BAF3 cells expressing TEL-fused FGFR4 kinase after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
BaF3	IC₅₀	543.5 nM Compound: 1; AZD-4547	Antiproliferative activity against mouse BAF3 cells expressing TEL-fused KDR kinase after 72 hrs by CCK8 or MTT assay Antiproliferative activity against mouse BAF3 cells expressing TEL-fused KDR kinase after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
BGC-823	IC₅₀	7.9 μM Compound: AZD4547	Antiproliferative activity against human BGC823 cells after 72 hrs by MTT assay Antiproliferative activity against human BGC823 cells after 72 hrs by MTT assay	[PMID: 27829519]
DMS-114	IC₅₀	14 nM Compound: AZD4547	Antiproliferative activity against human DMS-114 cells assessed as inhibition of cell growth incubated for 120 hrs by MTT assay Antiproliferative activity against human DMS-114 cells assessed as inhibition of cell growth incubated for 120 hrs by MTT assay	[PMID: 36096343]
HeLa 229	IC₅₀	0.14 μM Compound: AZD4547	Cytotoxicity against human HeLa 229 cells after 72 hrs by MTT assay Cytotoxicity against human HeLa 229 cells after 72 hrs by MTT assay	[PMID: 25736993]
HepG2	IC₅₀	3.13 μM Compound: AZD4547	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38643670]
HT-29	EC₅₀	19 nM Compound: AZD4547; F2	Anti-necroptosis activity against TNFalpha-induced human HT-29 cells assessed as reduction in cell viability Anti-necroptosis activity against TNFalpha-induced human HT-29 cells assessed as reduction in cell viability	[PMID: 38199165]
HT-29	EC₅₀	19 nM Compound: AZD4547; F2	Anti-necroptosis activity against TSZ-induced human HT-29 cells assessed as reduction in cell viability by Cell-titer glo luminescent based analysis Anti-necroptosis activity against TSZ-induced human HT-29 cells assessed as reduction in cell viability by Cell-titer glo luminescent based analysis	[PMID: 38199165]
Huh-7	IC₅₀	>10 μM Compound: AZD4547	Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
Huh-7	IC₅₀	284.3 nM Compound: 1; AZD-4547	Antiproliferative activity against FGF19/FGFR4 expressing human HuH7 cells after 72 hrs by CCK8 or MTT assay Antiproliferative activity against FGF19/FGFR4 expressing human HuH7 cells after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
HUVEC	IC₅₀	37.95 μM Compound: AZD4547	Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38643670]
KG-1	IC₅₀	<0.2 nM Compound: AZD4547	Inhibition of FGFR1 in human KG1 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay Inhibition of FGFR1 in human KG1 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay	[PMID: 27117427]
KG-1	IC₅₀	<0.2 nM Compound: AZD4547	Antiproliferative activity against human KG1 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human KG1 cells after 72 hrs by CCK-8 assay	[PMID: 27326339]
KG-1	IC₅₀	1.9 nM Compound: 1; AZD-4547	Antiproliferative activity against human KG1 cells expressing FGFR1 after 72 hrs Antiproliferative activity against human KG1 cells expressing FGFR1 after 72 hrs	[PMID: 29775937]
KG-1	IC₅₀	3.3 nM Compound: AZD4547	Antiproliferative activity against human KG1 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human KG1 cells after 72 hrs by CCK-8 assay	[PMID: 28687204]
KG-1	IC₅₀	3.7 nM Compound: 1; AZD4547	Antiproliferative activity against human KG1 cells measured after 72 hrs by CCK8 assay Antiproliferative activity against human KG1 cells measured after 72 hrs by CCK8 assay	[PMID: 31335138]
KG-1	IC₅₀	5.8 nM Compound: AZD4547	Antiproliferative activity against FGFR1 fused human KG1 cells after 72 hrs by CCK8 assay Antiproliferative activity against FGFR1 fused human KG1 cells after 72 hrs by CCK8 assay	[PMID: 30572178]
KG-1	IC₅₀	6.4 nM Compound: 5	Antiproliferative activity against FGFR1-translocated human KG1 cells after 72 hrs by CCK8/MTT assay Antiproliferative activity against FGFR1-translocated human KG1 cells after 72 hrs by CCK8/MTT assay	[PMID: 27348537]
L02	IC₅₀	18.21 μM Compound: AZD4547	Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay	[PMID: 25736993]
MDA-MB-231	IC₅₀	7.19 μM Compound: AZD4547	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38643670]
MDA-MB-435	IC₅₀	21.58 μM Compound: AZD4547	Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38643670]
MGC-803	IC₅₀	6.2 μM Compound: AZD4547	Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay	[PMID: 27829519]
NCI-H1581	IC₅₀	0.024 μM Compound: AZD4547	Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
NCI-H1581	IC₅₀	15.8 nM Compound: AZ04547	Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as reduction in cell viability measured after 72 hrs Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as reduction in cell viability measured after 72 hrs	[PMID: 36802596]
NCI-H1581	IC₅₀	37.9 nM Compound: AZD4547	Antiproliferative activity against human NCI-H1581 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1581 cells after 72 hrs by CCK-8 assay	[PMID: 27326339]
NCI-H1581	IC₅₀	4 nM Compound: AZD4547	Antiproliferative activity against human NCI-H1581 cells assessed as inhibition of cell growth incubated for 120 hrs by MTT assay Antiproliferative activity against human NCI-H1581 cells assessed as inhibition of cell growth incubated for 120 hrs by MTT assay	[PMID: 36096343]
NCI-H1581	IC₅₀	40 nM Compound: 1; AZD-4547	Antiproliferative activity against FGFR1 amplified human NCI-H1581 cells after 72 hrs by CCK8 or MTT assay Antiproliferative activity against FGFR1 amplified human NCI-H1581 cells after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
NCI-H1581	IC₅₀	40 nM Compound: 1; AZD-4547	Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 after 72 hrs Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 after 72 hrs	[PMID: 29775937]
NCI-H1581	IC₅₀	92.1 nM Compound: 5	Antiproliferative activity against FGFR1-amplified human NCI-H1581 cells after 72 hrs by CCK8/MTT assay Antiproliferative activity against FGFR1-amplified human NCI-H1581 cells after 72 hrs by CCK8/MTT assay	[PMID: 27348537]
NCI-H460	IC₅₀	>10 μM Compound: AZD4547	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
NCI-H716	IC₅₀	0.6 nM Compound: AZ04547	Antiproliferative activity against human NCI-H716 cells expressing FGFR2 assessed as reduction in cell viability measured after 72 hrs Antiproliferative activity against human NCI-H716 cells expressing FGFR2 assessed as reduction in cell viability measured after 72 hrs	[PMID: 36802596]
NCI-H716	IC₅₀	5.9 nM Compound: AZD4547	Antiproliferative activity against FGFR2 amplified human NCI-H716 cells after 72 hrs by CCK8 assay Antiproliferative activity against FGFR2 amplified human NCI-H716 cells after 72 hrs by CCK8 assay	[PMID: 30572178]
OPM-2	IC₅₀	83.6 nM Compound: 1; AZD-4547	Antiproliferative activity against FGFR3 amplified human OPM2 cells after 72 hrs by CCK8 or MTT assay Antiproliferative activity against FGFR3 amplified human OPM2 cells after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
OPM-2	IC₅₀	83.6 nM Compound: AZ04547	Antiproliferative activity against human OPM-2 cells expressing FGFR3 assessed as reduction in cell viability measured after 72 hrs Antiproliferative activity against human OPM-2 cells expressing FGFR3 assessed as reduction in cell viability measured after 72 hrs	[PMID: 36802596]
RT-112	GI₅₀	0.0292 μM Compound: AZD4547	Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay	[PMID: 27599742]
RT-112	IC₅₀	0.6 nM Compound: AZD4547	Inhibition of FGFR3 in human RT112 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay Inhibition of FGFR3 in human RT112 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay	[PMID: 27117427]
RT-112	IC₅₀	0.6 nM Compound: AZD4547	Antiproliferative activity against human RT112 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human RT112 cells after 72 hrs by CCK-8 assay	[PMID: 27326339]
RT-112	IC₅₀	36.4 nM Compound: 1; AZD-4547	Antiproliferative activity against FGFR3 amplified human RT112 cells after 72 hrs by CCK8 or MTT assay Antiproliferative activity against FGFR3 amplified human RT112 cells after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
RT-112	IC₅₀	83.8 nM Compound: 1; AZD-4547	Antiproliferative activity against human RT112 cells expressing FGFR3 after 72 hrs Antiproliferative activity against human RT112 cells expressing FGFR3 after 72 hrs	[PMID: 29775937]
RT-112	IC₅₀	88.4 nM Compound: 5	Antiproliferative activity against FGFR3-amplified human RT112 cells after 72 hrs by CCK8/MTT assay Antiproliferative activity against FGFR3-amplified human RT112 cells after 72 hrs by CCK8/MTT assay	[PMID: 27348537]
SGC-7901	IC₅₀	2.8 μM Compound: AZD4547	Antiproliferative activity against human SGC7901 cells after 72 hrs by MTT assay Antiproliferative activity against human SGC7901 cells after 72 hrs by MTT assay	[PMID: 27829519]
SK-HEP1	IC₅₀	2.78 μM Compound: AZD4547	Antiproliferative activity against human SK-HEP1 cells expressing FGFR4 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human SK-HEP1 cells expressing FGFR4 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
SNU-16	IC₅₀	0.006 μM Compound: AZD4547	Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
SNU-16	IC₅₀	1.2 nM Compound: AZD4547	Antiproliferative activity against human SNU16 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human SNU16 cells after 72 hrs by CCK-8 assay	[PMID: 27326339]
SNU-16	IC₅₀	1.5 nM Compound: 1; AZD-4547	Antiproliferative activity against FGFR2 amplified human SNU16 cells after 72 hrs by CCK8 or MTT assay Antiproliferative activity against FGFR2 amplified human SNU16 cells after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
SNU-16	IC₅₀	13.4 nM Compound: 5	Antiproliferative activity against FGFR2-amplified human SNU16 cells after 72 hrs by CCK8/MTT assay Antiproliferative activity against FGFR2-amplified human SNU16 cells after 72 hrs by CCK8/MTT assay	[PMID: 27348537]
SNU-16	IC₅₀	19.6 nM Compound: AZD4547	Antiproliferative activity against FGFR2 amplified human SNU16 cells after 72 hrs by CCK8 assay Antiproliferative activity against FGFR2 amplified human SNU16 cells after 72 hrs by CCK8 assay	[PMID: 30572178]
SNU-16	IC₅₀	3.4 nM Compound: AZD4547	Antiproliferative activity against human SNU16 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human SNU16 cells after 72 hrs by CCK-8 assay	[PMID: 28687204]
SNU-16	IC₅₀	3.6 nM Compound: AZD4547	Inhibition of recombinant FGFR2 in human SNU16 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay Inhibition of recombinant FGFR2 in human SNU16 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay	[PMID: 27117427]
SNU-16	IC₅₀	3.7 nM Compound: AZ04547	Antiproliferative activity against human SNU-16 cells assessed as reduction in cell viability measured for 72 hrs Antiproliferative activity against human SNU-16 cells assessed as reduction in cell viability measured for 72 hrs	[PMID: 36802596]
SNU-16	IC₅₀	4.9 nM Compound: 1; AZD4547	Antiproliferative activity against human SNU16 cells measured after 72 hrs by CCK8 assay Antiproliferative activity against human SNU16 cells measured after 72 hrs by CCK8 assay	[PMID: 31335138]
SNU-16	IC₅₀	6.2 nM Compound: 1; AZD-4547	Antiproliferative activity against human SNU16 cells expressing FGFR2 after 72 hrs Antiproliferative activity against human SNU16 cells expressing FGFR2 after 72 hrs	[PMID: 29775937]
SNU-16	IC₅₀	64 nM Compound: 8; AZD4547	Antiproliferative activity against human SNU-16 cells overexpressing FGFR2 assessed as inhibition of cell proliferative by measuring ATP level after 72 hrs by luminescence based assay Antiproliferative activity against human SNU-16 cells overexpressing FGFR2 assessed as inhibition of cell proliferative by measuring ATP level after 72 hrs by luminescence based assay	[PMID: 33199155]
TOV21G	EC₅₀	52 nM Compound: AZD4547; F2	Anti-necroptosis activity against TNFalpha-induced human TOV-21G cells assessed as reduction in cell viability Anti-necroptosis activity against TNFalpha-induced human TOV-21G cells assessed as reduction in cell viability	[PMID: 38199165]
U-87MG ATCC	IC₅₀	25.41 μM Compound: AZD4547	Antiproliferative activity against human U-87 MG cells incubated for 48 hrs by MTT assay Antiproliferative activity against human U-87 MG cells incubated for 48 hrs by MTT assay	[PMID: 37651879]
U-937	EC₅₀	31 nM Compound: AZD4547; F2	Anti-necroptosis activity against TNFalpha-induced human U-937 cells assessed as reduction in cell viability Anti-necroptosis activity against TNFalpha-induced human U-937 cells assessed as reduction in cell viability	[PMID: 38199165]

体外実験

Fexagratinib also inhibits recombinant VEGFR2 (KDR) kinase activity with an IC₅₀ of 24 nM. In KG1a, Sum52-PE, MCF7, and KMS11 cell lines, Fexagratinib potently inhibits autophosphorylation of FGFR1, 2, and 3 tyrosine kinases (IC₅₀ values of 12, 2, and 40 nM, respectively) and displays weaker inhibition of FGFR4 cellular kinase activity (IC₅₀=142 nM). Significantly weaker inhibitory activity is observed versus cellular KDR and IGFR ligand-induced phosphorylation (IC₅₀ values of 258 and 828 nM, respectively), representing approximately 20- and 70-fold selectivity over cellular FGFR1. Besides, Fexagratinib potently inhibits FGFR phosphorylation and downstream signaling affected through FRS2, PLCγ, and MAPK at the cellular level^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Female SCID mice bearing KMS11 tumors are randomized and treated chronically with Fexagratinib at a range of well-tolerated doses. Oral Fexagratinib treatment results in dose-dependent tumor growth inhibition. Twice daily administration of Fexagratinib at 3 mg/kg gives statistically significant tumor growth inhibition of 53% (P<0.0005 by one-tailed t test) when compare with vehicle-treated controls, whereas doses of 12.5 mg/kg once daily and 6.25 mg/kg twice daily results in complete tumor stasis (P<0.0001). A further efficacy study in the KG1a model with 12.5 mg/kg once daily Fexagratinib results in 65% tumor growth inhibition (P=0.002)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1035270-39-3
性状 Solid
分子量 463.57
分子式 C₂₆H₃₃N₅O₃
Color White to yellow
SMILES

C[C@H](C1)N[C@@H](C)CN1C2=CC=C(C(NC3=NNC(CCC4=CC(OC)=CC(OC)=C4)=C3)=O)C=C2
別名

AZD4547; ADSK091
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (36)

All In Vivo Efficacy StudyPK/PD AnalysisCell Proliferation/Viability AssayWB

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Journal Impact Factor

Bioact Mater

Turning gray selenium into a nanoaccelerator of tissue regeneration by PEG modification. [Abstract]

2022 Jan 2:15:131-144. PMID: 35386336
Cancer Res

The C-terminal Kinase Domain-Binding and Suppression Motif Prevents Constitutive Activation of FGFR2. [Abstract]

2025 Jun 24. PMID: 40554806

Fexagratinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Jun 24. [Abstract]

Quantifications of Western blots showing expression and phosphorylation of indicated proteins in serum-starved GFPhi NMuMG cells expressing GFP, Fgfr2^FL-GFP, or Fgfr2^ΔE18-GFP and treated for 15 minutes with 20 ng/mL FGF-10 and/or for 3 hours with 100 nmol/L Fexagratinib.
Nat Commun

PLK1 inhibition exhibits strong anti-tumoral activity in CCND1-driven breast cancer metastases with acquired palbociclib resistance. [Abstract]

2020 Aug 13;11(1):4053. PMID: 32792481

Fexagratinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Aug 13;11(1):4053. [Abstract]

In vivo targeting of HBCx-137 PDX by volasertib (10 mg/kg 4 times/week), palbociclib (75 mg/kg 5 days/week) and Fexagratinib (AZD4547, 12.5 mg/kg; p.o.; 5 days per week) in monotherapy and in combination with fulvestrant. n = 5 independent xenografts (control, fulvestrant, AZD4547, fulv. + AZD4547), n = 7 (volasertib), n = 8 (fulv.+vola), n = 9 (palbo, palbo + fulv.). Mean ± SD. Volasertib treated xenografts were monitored after end of treatment to detect tumour recurrence. Two xenografts relapsed at day 70 and 100 and were rechallenged with volasertib.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Nanobiotechnology

Hyaluronic acid-FGF2-derived peptide bioconjugates for suppression of FGFR2 and AR simultaneously as an acne antagonist. [Abstract]

2023 Feb 17;21(1):55. PMID: 36803994

Fexagratinib purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2023 Feb 17;21(1):55. [Abstract]

HA-P5 and Fexagratinib (AZD4547, 5-10 μM; 48 h) inhibited the colony formation in SZ95, HaCaT, and HSF cells.

Fexagratinib purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2023 Feb 17;21(1):55. [Abstract]

HA-P5 (100 μM; administered daily for up to 20 days) and Fexagratinib (AZD4547, 5 μM; administered daily for up to 20 days) remedied acne on the ears of male New Zealand rabbits with smoother epidermis and thinner stratum corneum.
J Exp Clin Cancer Res

Platform combining statistical modeling and patient-derived organoids to facilitate personalized treatment of colorectal carcinoma. [Abstract]

2023 Apr 3;42(1):79. PMID: 37013646

Fexagratinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2023 Apr 3;42(1):79. [Abstract]

The set of drugs (Regorafenib, Vemurafenib, Vatalanib, Erlotinib, Fexagratinib (AZD4547), Lapatinib, Trametinib, Palbociclib, BEZ-235, Nilotinib, Olaparib) used in the screen, their main targets, and clinical information
^aCUD Clinically used dose, calculated using the area under the curve
^b(AUC_{0-24 h}) of each drug, which corresponds to the plasma concentration of the drug over the first 24 h, and is used to calculate the average drug concentration in that time. Data was obtained from pharmacokinetic studies performed in patients exposed to the drugs at standard or maximum tolerated doses
Adv Sci (Weinh)

Osteoblast-Derived ECM1 Promotes Anti-Androgen Resistance in Bone Metastatic Prostate Cancer. [Abstract]

2025 Jan;12(2):e2407662. PMID: 39563492
J Control Release

FGFR2-responsive self-assembled hydrogel releases its inhibitor to suppress the progression of endometriosis. [Abstract]

2026 Jul 10:395:115007. PMID: 42114779
Cell Death Dis

Stattic enhances the anti-tumor activity of AZD4547 in LUSC by blocking STAT3/RRM2-mediated DNA repair and inducing ROS-driven mitochondrial dysfunction. [Abstract]

2026 May 19;17(1):632. PMID: 42156709
J Neuroinflammation

The FGF/FGFR system in the microglial neuroinflammation with Borrelia burgdorferi: likely intersectionality with other neurological conditions. [Abstract]

2023 Jan 17;20(1):10. PMID: 36650549
Mater Today Bio

Turning sublimed sulfur and bFGF into a nanocomposite to accelerate wound healing via co-activate FGFR and Hippo signaling pathway. [Abstract]

2024 May 27:26:101104. PMID: 38952539
Acta Pharmacol Sin

Repurposing of the FGFR inhibitor AZD4547 as a potent inhibitor of necroptosis by selectively targeting RIPK1. [Abstract]

2023 Apr;44(4):801-810. PMID: 36216899
NPJ Precis Oncol

Comprehensive functional evaluation of variants of fibroblast growth factor receptor genes in cancer. [Abstract]

2021 Jul 16;5(1):66. PMID: 34272467
Cell Prolif

Flavonoid chrysin activates both TrkB and FGFR1 receptors while upregulates their endogenous ligands such as brain derived neurotrophic factor to promote human neurogenesis. [Abstract]

2025 Jan;58(1):e13732. PMID: 39331585
J Med Chem

Discovery of a 1 H-Pyrazol-3-Amine Derivative as a Novel, Selective, and Orally Available RIPK1 Inhibitor for the Treatment of Inflammatory Disease. [Abstract]

2025 Oct 23;68(20):21766-21785. PMID: 41077763
Sci Signal

KRASG12C inhibition produces a driver-limited state revealing collateral dependencies. [Abstract]

2019 May 28;12(583):eaaw9450. PMID: 31138768
Eur J Pharmacol

Angiotensin II-induced fibrosis is mediated by activation of FGFR1 pathway in renal epithelial cells: Attenuation by chimeric peptide. [Abstract]

2025 Dec 15:1009:178390. PMID: 41274591
Respir Res

Fibroblast growth factor 10 attenuates chronic obstructive pulmonary disease by protecting against glycocalyx impairment and endothelial apoptosis. [Abstract]

2022 Oct 1;23(1):269. PMID: 36183124
Int J Mol Sci

FGF2 Rescued Cisplatin-Injured Granulosa Cells through the NRF2-Autophagy Pathway. [Abstract]

2023 Sep 18;24(18):14215. PMID: 37762517
Cell Oncol (Dordr)

AZD4547 targets the FGFR/Akt/SOX2 axis to overcome paclitaxel resistance in head and neck cancer. [Abstract]

2022 Feb;45(1):41-56. PMID: 34837170
Front Cell Dev Biol

An FGFR/AKT/SOX2 Signaling Axis Controls Pancreatic Cancer Stemness. [Abstract]

2020 May 7:8:287. PMID: 32457900

Fexagratinib purchased from MedChemExpress. Usage Cited in: Front Cell Dev Biol. 2020 May 7:8:287. [Abstract]

Determination in L3.6 cells of FGF2-induced FGFR phosphorylation by Western blot in the presence of AZD4547 . FGFR1 and alpha-Tubulin are used as loading controls.
PLoS Pathog

Antimicrobial peptide-producing dermal preadipocytes defend against Candida albicans skin infection via the FGFR-MEK-ERK pathway. [Abstract]

2023 Nov 30;19(11):e1011754. PMID: 38032898
Cancers (Basel)

TMEM176B Promotes EMT via FGFR/JNK Signalling in Development and Tumourigenesis of Lung Adenocarcinoma. [Abstract]

2024 Jul 3;16(13):2447. PMID: 39001509
Mol Oncol

Optimized low-dose combinatorial drug treatment boosts selectivity and efficacy of colorectal carcinoma treatment. [Abstract]

2020 Nov;14(11):2894-2919. PMID: 33021054
Am J Physiol Endocrinol Metab

Vertical sleeve gastrectomy improves glucose-insulin homeostasis by enhancing beta cell function and survival via FGF15/19. [Abstract]

2024 Feb 1;326(2):E134-E147. PMID: 38117265
Development

Regulation of otocyst patterning by Tbx2 and Tbx3 is required for inner ear morphogenesis in the mouse. [Abstract]

2021 Apr 15;148(8):dev195651. PMID: 33795231
Mol Carcinog

Epidermal growth factor receptor signaling in precancerous keratinocytes promotes neighboring head and neck cancer squamous cell carcinoma cancer stem cell-like properties and phosphoinositide 3-kinase inhibitor insensitivity. [Abstract]

2022 Jul;61(7):664-676. PMID: 35417043
Mol Cell Endocrinol

FGF2 promotes the proliferation of injured granulosa cells in premature ovarian failure via Hippo-YAP signaling pathway. [Abstract]

2024 Aug 1:589:112248. PMID: 38663484
bioRxiv

2026 May 26.
Res Sq

2025 Jul 24.
Comput Biol Med

PANoptosis-driven molecular stratification in esophageal squamous cell carcinoma: A multi-omics prognostic model and FGFR-Targeted therapeutic validation. [Abstract]

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bioRxiv

Modeling acquired TKI resistance and effective combination therapeutic strategies in murine RET+ lung adenocarcinoma. [Abstract]

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Patent

US20220305015A1.
Oncotarget

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溶剤 & 溶解度

体外:

DMSO : 125 mg/mL (269.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1572 mL

10.7859 mL

21.5717 mL

5 mM

0.4314 mL

2.1572 mL

4.3143 mL

10 mM

0.2157 mL

1.0786 mL

2.1572 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 1% CMC-Na/saline water

Solubility: 3.33 mg/mL (7.18 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

Cell Assay^[1]

Cell lines are incubated with fixed concentrations of AZD4547 for 72 hours. 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 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
Swiss derived nude (nu/nu) and severe combined immunodeficient mice (SCID) are used. Tumor xenografts are established by s.c. injection into the left flank with 0.1 mL tumor cells (1×10⁶ for LoVo, 1×10⁷ for HCT-15, and 1×10⁷ for Calu-6) or 0.2 mL (2×10⁷ for KMS11 and KG1a) mixed 1:1 with Matrigel, with the exception of LoVo and HCT-15, which do not include Matrigel. Mice are randomized into control and treatment groups (AZD4547, 1.5-50 mg/kg, once daily or twice daily by oral gavage) when tumors reach the determined size of more than 0.2 cm³. Tumor volume (measured by caliper), animal body weight, and tumor condition are recorded twice weekly for the duration of the study. Tumor volume is calculated.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (279 KB)
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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Gavine PR, et al. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res, 2012, 72(8), 2045-2056. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1572 mL	10.7859 mL	21.5717 mL	53.9293 mL
	5 mM	0.4314 mL	2.1572 mL	4.3143 mL	10.7859 mL
	10 mM	0.2157 mL	1.0786 mL	2.1572 mL	5.3929 mL
	15 mM	0.1438 mL	0.7191 mL	1.4381 mL	3.5953 mL
	20 mM	0.1079 mL	0.5393 mL	1.0786 mL	2.6965 mL
	25 mM	0.0863 mL	0.4314 mL	0.8629 mL	2.1572 mL
	30 mM	0.0719 mL	0.3595 mL	0.7191 mL	1.7976 mL
	40 mM	0.0539 mL	0.2696 mL	0.5393 mL	1.3482 mL
	50 mM	0.0431 mL	0.2157 mL	0.4314 mL	1.0786 mL
	60 mM	0.0360 mL	0.1798 mL	0.3595 mL	0.8988 mL
	80 mM	0.0270 mL	0.1348 mL	0.2696 mL	0.6741 mL
	100 mM	0.0216 mL	0.1079 mL	0.2157 mL	0.5393 mL

Keywords

Fexagratinib

36 Cited Publications

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Fexagratinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

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Anti-Pancreatic Cancer Compound Library

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High-Throughput Bioactive Compound Library

Posttranslational Modification Library

MedChemExpress（MCE）の使用を引用している文献 Fexagratinib

生物活性

化学情報

Publications (36)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Fexagratinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

MedChemExpress（MCE）の使用を引用している文献 Fexagratinib

生物活性

化学情報

Publications (36)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Fexagratinib 関連分類

HY-13330 関連分類