Fexagratinib (Synonyms: AZD4547; ADSK091)

Name: Fexagratinib
Brand: MedChemExpress
SKU: HY-13330
Rating: 5.0 (25 reviews)

Cat. No.: HY-13330 Purity: 99.85%: FAQs
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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.

For research use only. We do not sell to patients.

Fexagratinib Chemical Structure

CAS No. : 1035270-39-3

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10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 25 publication(s) in Google Scholar

Other Forms of Fexagratinib:

Fexagratinib (Standard) Get quote

24 Publications Citing Use of MCE Fexagratinib

: 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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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]
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]
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	< 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	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]
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	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	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	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]

In Vitro

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.

In Vivo

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.

Clinical Trial

Molecular Weight

463.57

Formula

C₂₆H₃₃N₅O₃

CAS No.

1035270-39-3

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.

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

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.85%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (251 KB) HNMR (289 KB) LCMS (91 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

Fexagratinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fexagratinib1035270-39-3AZD4547 ADSK091AZD 4547AZD-4547ADSK091ADSK 091ADSK-091FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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Fexagratinib (Synonyms: AZD4547; ADSK091)

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Fexagratinib Related Antibodies

24 Publications Citing Use of MCE Fexagratinib

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