Art. -Nr.: HY-18708

Erdafitinib

(Synonyms: JNJ-42756493)

39 Cited Publications

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Based on 39 publication(s) in Google Scholar

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC₅₀s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

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Reinheit: 99.66%
CAS. Nr.: 1346242-81-6
Formel: C₂₅H₃₀N₆O₂
Molecular Weight:446.54

Speicherung:

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

Erdafitinib Chemical Structure

CAS. Nr.: 1346242-81-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (39)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
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Biologische Aktivität

Beschreibung

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC₅₀s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

IC₅₀ & Target^[1]

FGFR1

1.2 nM (IC₅₀)

FGFR2

2.5 nM (IC₅₀)

FGFR3

3.0 nM (IC₅₀)

FGFR4

5.7 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.02 μM Compound: 1; JNJ-42756493	Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36449947]
A2780	IC₅₀	0.02 μM Compound: Erdafitnib	Antiproliferative activity against human A2780 cells Antiproliferative activity against human A2780 cells	[PMID: 38964169]
AN3-CA	GI₅₀	0.048 μM Compound: 2	Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
BaF3	GI₅₀	>5 μM Compound: 2	Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
BaF3	GI₅₀	>5 μM Compound: 2	Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
BaF3	GI₅₀	0.005 μM Compound: 2	Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
BaF3	GI₅₀	0.761 μM Compound: 2	Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
BaF3	GI₅₀	4.011 μM Compound: 2	Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
BaF3	GI₅₀	>300 nM Compound: 1	Growth inhibition against mouse BaF3 cells incubated for 72 to 96 hrs by MTT assay Growth inhibition against mouse BaF3 cells incubated for 72 to 96 hrs by MTT assay	[PMID: 38294952]
BaF3	IC₅₀	0.1 nM Compound: 5	Inhibition of VEGFR2 in mouse BAF3 cells Inhibition of VEGFR2 in mouse BAF3 cells	10.1039/C9MD90044F
DMS-114	IC₅₀	11 nM Compound: 1	Inhibition of cell viability in human DMS-114 cells harboring FGFR1-amplification incubated for 72 to 120 hrs by Cell Titer Glo assay Inhibition of cell viability in human DMS-114 cells harboring FGFR1-amplification incubated for 72 to 120 hrs by Cell Titer Glo assay	[PMID: 39258897]
HCT-116	IC₅₀	4.24 μM Compound: 1; JNJ-42756493	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36449947]
HCT-116	IC₅₀	4.24 μM Compound: Erdafitnib	Antiproliferative activity against human HCT-116 cells Antiproliferative activity against human HCT-116 cells	[PMID: 38964169]
J82	GI₅₀	3.796 μM Compound: 2	Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
Jurkat	IC₅₀	6.81 μM Compound: 1; JNJ-42756493	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36449947]
Jurkat	IC₅₀	6.81 μM Compound: Erdafitnib	Antiproliferative activity against human Jurkat cells Antiproliferative activity against human Jurkat cells	[PMID: 38964169]
K562	IC₅₀	3.02 μM Compound: 1; JNJ-42756493	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36449947]
K562	GI₅₀	>300 nM Compound: 1	Growth inhibition against human K562 cells incubated for 72 to 96 hrs by MTT assay Growth inhibition against human K562 cells incubated for 72 to 96 hrs by MTT assay	[PMID: 38294952]
K562	IC₅₀	3.02 μM Compound: Erdafitnib	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 38964169]
KATO III stomach cancer cell line	IC₅₀	0.004 μM Compound: 1; JNJ-42756493	Antiproliferative activity against human KATO III stomach cancer cell line assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human KATO III stomach cancer cell line assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36449947]
KG-1	IC₅₀	2.1 nM Compound: 1	Inhibition of cell viability in human KG-1 cells harboring FGFR1-fusion incubated for 72 to 120 hrs by Cell Titer Glo assay Inhibition of cell viability in human KG-1 cells harboring FGFR1-fusion incubated for 72 to 120 hrs by Cell Titer Glo assay	[PMID: 39258897]
KG-1a	GI₅₀	5 nM Compound: 1	Growth inhibition against human KG-1a cells incubated for 72 to 96 hrs by MTT assay Growth inhibition against human KG-1a cells incubated for 72 to 96 hrs by MTT assay	[PMID: 38294952]
KMS-11	GI₅₀	0.39 μM Compound: 2	Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay	[PMID: 35436119]
KMS-11	GI₅₀	150 nM Compound: 1	Growth inhibition against human KMS-11 cells incubated for 72 to 96 hrs by MTT assay Growth inhibition against human KMS-11 cells incubated for 72 to 96 hrs by MTT assay	[PMID: 38294952]
MDA-MB-453	GI₅₀	44 nM Compound: 1	Growth inhibition against human MDA-MB-453 cells incubated for 72 to 96 hrs by MTT assay Growth inhibition against human MDA-MB-453 cells incubated for 72 to 96 hrs by MTT assay	[PMID: 38294952]
MFE-296	GI₅₀	41 nM Compound: 1	Growth inhibition against human MFE-296 cells incubated for 72 to 96 hrs by MTT assay Growth inhibition against human MFE-296 cells incubated for 72 to 96 hrs by MTT assay	[PMID: 38294952]
NCI-H716	GI₅₀	0.9 nM Compound: 1	Growth inhibition against human NCI-H716 cells incubated for 72 to 96 hrs by MTT assay Growth inhibition against human NCI-H716 cells incubated for 72 to 96 hrs by MTT assay	[PMID: 38294952]
RT-112	IC₅₀	1.3 nM Compound: Erdafitinib	Antiproliferative activity against human RT-112 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
RT-112	IC₅₀	107 nM Compound: Erdafitinib	Antiproliferative activity against human RT-112 cells expressing FGFR3 N540K mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells expressing FGFR3 N540K mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
RT-112	IC₅₀	2.4 nM Compound: Erdafitinib	Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
RT-112	IC₅₀	39 nM Compound: Erdafitinib	Antiproliferative activity against human RT-112 cells expressing FGFR3 K650M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells expressing FGFR3 K650M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
RT-112	IC₅₀	603 nM Compound: Erdafitinib	Antiproliferative activity against human RT-112 cells expressing FGFR3 V555M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human RT-112 cells expressing FGFR3 V555M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
RT-4	GI₅₀	<10 nM Compound: 1	Growth inhibition against human RT-4 cells incubated for 72 to 96 hrs by MTT assay Growth inhibition against human RT-4 cells incubated for 72 to 96 hrs by MTT assay	[PMID: 38294952]
RT-4	IC₅₀	4.4 nM Compound: 1	Inhibition of cell viability in human RT-4 cells harboring FGFR3/TACC3 fusion incubated for 72 to 120 hrs by Cell Titer Glo assay Inhibition of cell viability in human RT-4 cells harboring FGFR3/TACC3 fusion incubated for 72 to 120 hrs by Cell Titer Glo assay	[PMID: 39258897]
Sf21	IC₅₀	3 nM Compound: JNJ-42756493	Inhibition of human recombinant N-terminal His6 tagged FGFR3 (447 to 761 residues) expressed in Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition measured after 60 mins in presence of ATP by time resolved f Inhibition of human recombinant N-terminal His6 tagged FGFR3 (447 to 761 residues) expressed in Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition measured after 60 mins in presence of ATP by time resolved f	[PMID: 32278710]
Sf21	IC₅₀	36.8 nM Compound: JNJ-42756493	Inhibition of human N-terminal His6-tagged VEGFR2 (790 to end residues) expressed in baculovirus infected Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition in presence of ATP by time resolved fluorescence a Inhibition of human N-terminal His6-tagged VEGFR2 (790 to end residues) expressed in baculovirus infected Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition in presence of ATP by time resolved fluorescence a	[PMID: 32278710]
Sf9	IC₅₀	0.003 μM Compound: 5	Inhibition of wild type His-tagged human FGFR3 (455 to 763 residues) expressed in Sf9 insect cells by ELISA Inhibition of wild type His-tagged human FGFR3 (455 to 763 residues) expressed in Sf9 insect cells by ELISA	10.1039/C9MD90044F
SNU-16	IC₅₀	0.0007 μM Compound: 1; JNJ-42756493	Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36449947]
SNU-16	IC₅₀	0.7 nM Compound: 1; JNJ-42756493	Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36449947]
SNU-16	IC₅₀	2.7 nM Compound: Erdafitinib	Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay	[PMID: 38267212]
SNU-16	IC₅₀	0.7 nM Compound: Erdafitnib	Antiproliferative activity against human SNU-16 cells Antiproliferative activity against human SNU-16 cells	[PMID: 38964169]

In Vitro

Erdafitinib (JNJ-42756493) inhibits the tyrosine kinase activities of FGFR1-4 in time-resolved fluorescence assays with IC₅₀ values of 1.2, 2.5, 3.0 and 5.7 nM, respectively. The closely related VEGFR2 kinase is less potently inhibited (30-fold less potent compared to FGFR1) by erdafitinib, with an IC₅₀ value of 36.8 nM. Erdafitinib binds FGFR1, 3, 4, and 2 with K_d values of 0.24, 1.1, 1.4 and 2.2 nM, respectively. The K_d value for VEGFR2 is higher at 6.6 nM. Erdafitinib inhibits proliferation of FGFR1, 3, and 4 expressing cells with IC₅₀ values of 22.1, 13.2, and 25nM, respectively^[1].

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

In Vivo

In xenografts from human tumor cell lines or patient-derived tumor tissue with activating FGFR alterations, Erdafitinib administration results in potent and dose-dependent antitumor activity accompanied by pharmacodynamic modulation of phospho-FGFR and phospho-ERK in tumors^[1].

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

Clinical Trial

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

Chemical Information

CAS. Nr. 1346242-81-6
Appearance Solid
Molecular Weight 446.54
Formel C₂₅H₃₀N₆O₂
Color Light yellow to yellow
SMILES

CN1N=CC(C2=NC3=CC(N(C4=CC(OC)=CC(OC)=C4)CCNC(C)C)=CC=C3N=C2)=C1
Synonyms

JNJ-42756493
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (39)

All Cell Proliferation/Viability AssayIn Vivo Efficacy StudyWBRT-PCRIHC

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Journal Impact Factor

Cancer Discov

Acquired On-Target Clinical Resistance Validates FGFR4 as a Driver of Hepatocellular Carcinoma. [Abstract]

2019 Dec;9(12):1686-1695. PMID: 31575540
Adv Funct Mater

2025 Jan 16.
Cancer Res

PI3K and MAPK Signaling Nodes Serve as Divergent Drivers of Phenotypic Plasticity in Cancer-Associated Fibroblasts in Colorectal Cancer. [Abstract]

2026 Mar 12. PMID: 41817574
Cancer Res

C-terminal Truncation and Fusion Partner Determine Oncogenicity of FGFR3. [Abstract]

2025 Dec 29. PMID: 41460723
Cancer Res

A Genome-Wide Synthetic Lethal Screen Identifies Spermidine Synthase as a Target to Enhance Erdafitinib Efficacy in FGFR-Mutant Bladder Cancer. [Abstract]

2025 Mar 24. PMID: 40126530

Erdafitinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Mar 24. [Abstract]

C, Cell Counting Kit-8 assay revealed the cell viability of WT and SRM KO MGH-U3 cells treated with erdafitinib (10 or 100 nmol/L; 24-96 h) or DMSO.

Erdafitinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Mar 24. [Abstract]

formed by subcutaneous injection of WT and SRM KO MGH-U3 cells into the right flanks of nude mice treated with DMSO or erdafitinib (5 or 15 mg/kg)

Erdafitinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Mar 24. [Abstract]

Western blotting with the indicated antibodies in WT and SRM KO MGH-U3 cells treated with 10 or 100 nmol/L erdafitinib and DMSO for 96 hours.

Erdafitinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Mar 24. [Abstract]

The expression of EGFR was detected by qRT-PCR in WT and SRM KO MGH-U3 cells treated with 100 nmol/L erdafitinib for 96 hours.

Erdafitinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Mar 24. [Abstract]

Mice were treated with DMSO, 5 mg/kg afatinib, 15 mg/kg erdafitinib, or combinational treatment. IHC staining of Ki67 on WT MGH-U3 xenografts was performed as in vivo.
Nat Commun

Accurate determination of CRISPR-mediated gene fitness in transplantable tumours. [Abstract]

2022 Aug 4;13(1):4534. PMID: 35927228
Autophagy

Inflammatory signaling attenuates spliceosome function and cognitive ability. [Abstract]

2025 Sep 29:1-19. PMID: 40963239
Cell Death Dis

FGFR inhibitors promote the autophagic degradation of IFN-γ-induced PD-L1 and alleviate the PD-L1-mediated transcriptional suppression of FGFR3-TACC3 in non-muscle-invasive bladder cancer. [Abstract]

2025 Jul 2;16(1):485. PMID: 40603902
Free Radic Biol Med

Erdafitinib promotes ferroptosis in human uveal melanoma by inducing ferritinophagy and lysosome biogenesis via modulating the FGFR1/mTORC1/TFEB signaling axis. [Abstract]

2024 Jul 4:S0891-5849(24)00548-3. PMID: 38971541
NPJ Precis Oncol

Tackling FGFR3-driven bladder cancer with a promising synergistic FGFR/HDAC targeted therapy. [Abstract]

2023 Jul 21;7(1):70. PMID: 37479885
Br J Pharmacol

FGF1ΔHBS ameliorates DSS-induced ulcerative colitis by reducing neutrophil recruitment through the MAPK pathway. [Abstract]

2025 Apr 21. PMID: 40258390
Biomed Pharmacother

FGF/FGFR inhibitors downmodulates c-Myc oncoprotein and hampers the growth of adrenocortical carcinoma. [Abstract]

2025 Oct 21:192:118677. PMID: 41124865
Cell Rep

Identification of WNK1 as a therapeutic target to suppress IgH/MYC expression in multiple myeloma. [Abstract]

2024 May 8;43(5):114211. PMID: 38722741
Cell Rep

Apatinib remodels the immunosuppressive tumor ecosystem of gastric cancer enhancing anti-PD-1 immunotherapy. [Abstract]

2023 Apr 24;42(5):112437. PMID: 37097818
Clin Transl Med

Multi-omic profiling defines three distinct molecular subtypes of urothelial carcinoma with implications for precision therapy. [Abstract]

2026 Mar;16(3):e70638. PMID: 41804750
Br J Cancer

Fibroblast growth factor signals drive the metastatic behavior in small cell lung cancer. [Abstract]

2025 Dec 13. PMID: 41390896
Breast Cancer Res

Erdafitinib inhibits the tumorigenicity of MDA-MB-231 triple-negative breast cancer cells by inducing TRIM25/ubiquitin-dependent degradation of FGFR4. [Abstract]

2025 Jul 9;27(1):128. PMID: 40635078
Mol Cancer Ther

Involvement of the FGF8/FGF receptor signaling pathway in the maintenance and progression of fusion-positive rhabdomyosarcoma. [Abstract]

2025 Nov 20. PMID: 41263060
J Chem Inf Model

Probe Substrate Dependencies in CYP3A4 Allosteric Inhibition: A Novel Molecular Mechanism Involving F-F' Loop Perturbations. [Abstract]

2024 Mar 25;64(6):2058-2067. PMID: 38457234
Life Sci

Identification of a novel fibroblast growth factor receptor-agonistic peptide and its effect on diabetic wound healing. [Abstract]

2025 Jan 28:364:123432. PMID: 39884341
Int Immunopharmacol

20(S)-PPD-HSA NPs enhance the recovery of intramedullary and extramedullary hematopoiesis in cyclophosphamide-treated mice through activation of the FGFR1/ERK pathway. [Abstract]

2025 Dec 23:170:116073. PMID: 41443104
Biochim Biophys Acta Mol Basis Dis

Inhibition of ELOVL6 activity impairs mitochondrial respiratory function and inhibits tumor progression in FGFR3-mutated bladder cancer cells. [Abstract]

2025 Aug 18;1871(8):168023. PMID: 40835210
FASEB J

P4HA2-mediated HIF-1α stabilization promotes erdafitinib-resistance in FGFR3-alteration bladder cancer. [Abstract]

2023 Apr;37(4):e22840. PMID: 36943397
Chem Res Toxicol

Mechanism-Based Inactivation of Cytochrome P450 3A4 and 3A5 by the Fibroblast Growth Factor Receptor Inhibitor Erdafitinib. [Abstract]

2021 Jul 19;34(7):1800-1813. PMID: 34189909
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
Heliyon

2024 May 13.
Heliyon

Skeletal overgrowth in a pre-pubescent child treated with pan-FGFR inhibitor. [Abstract]

2024 May 19;10(11):e30887. PMID: 38841436
J Pharm Biomed Anal

Quantification of the irreversible fibroblast growth factor receptor inhibitor futibatinib by UPLC-MS/MS: Application to the metabolic stability assay in human liver microsomes for the estimation of its in vitro hepatic intrinsic clearance. [Abstract]

2022 May 30;214:114731. PMID: 35325798
Mol Pharmacol

Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake. [Abstract]

2022 Jun;101(6):381-389. PMID: 35383108
Biochim Biophys Acta Gen Subj

The D647N mutation of FGFR1 induces ligand-independent receptor activation. [Abstract]

2023 Sep 29;1867(12):130470. PMID: 37778450
Anticancer Drugs

Derazantinib, a fibroblast growth factor receptor inhibitor, inhibits colony-stimulating factor receptor-1 in macrophages and tumor cells and in combination with a murine programmed cell death ligand-1-antibody activates the immune environment of murine syngeneic tumor models. [Abstract]

2023 Oct 1;34(9):1035-1045. PMID: 36729099
University of Auckland

2025.
bioRxiv

2024 September 10.
bioRxiv

Peristromal niches protect lung cancers from targeted therapies through a combined effect of multiple molecular mediators. [Abstract]

2024 Apr 25:2024.04.24.590626. PMID: 38712093
bioRxiv

2023 Nov 17.
University of Brescia

2023 Feb 2.
Research Square Print

September 14th, 2022.
Uppsala University

2022 Feb.
Oncotarget

MEK is a promising target in the basal subtype of bladder cancer. [Abstract]

2020 Nov 3;11(44):3921-3932. PMID: 33216841

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 62.5 mg/mL (139.97 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

2.2394 mL

11.1972 mL

22.3944 mL

5 mM

0.4479 mL

2.2394 mL

4.4789 mL

10 mM

0.2239 mL

1.1197 mL

2.2394 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.75 mg/mL (6.16 mM); Clear solution

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.75 mg/mL (6.16 mM); Clear solution

Protocol 3

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

Solubility: ≥ 2.33 mg/mL (5.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.33 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 (23.3 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

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

Solubility: ≥ 2.08 mg/mL (4.66 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 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 5

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

Solubility: ≥ 2.08 mg/mL (4.66 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.

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

Protokoll

Cell Assay^[1]

Erdafitinib is dissolved in DMSO. KATO III, RT-112, A-204, RT-4, DMS-114, A-427 and MDA-MB-453 cells are treated with erdafitinib (from 10 μM to 0.01 nM in 2% DMSO, final concentration). Following 4-day incubation, cell viability is determined using MTT reagent. The optical density is determined at 540 nm^[1].

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

Animal Administration^[1]

Mice: Mice bearing SNU-16 human gastric carcinoma (FGFR2 amplified) xenograft tumors are dosed orally with 0, 3, 10 or 30 mg/kg Erdafitinib. Tumor tissue and mouse plasma (3 mice per time point) are harvested at 0.5, 1, 3, 7, 16 and 24h post-dosing^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

Verweise

[1]. Perera TP, et al. Discovery and pharmacological characterization of JNJ-42756493 (erdafitinib), a functionally selective small molecule FGFR family inhibitor. Mol Cancer Ther. 2017 Mar 24. pii: molcanther.0589.2016. [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	2.2394 mL	11.1972 mL	22.3944 mL	55.9860 mL
	5 mM	0.4479 mL	2.2394 mL	4.4789 mL	11.1972 mL
	10 mM	0.2239 mL	1.1197 mL	2.2394 mL	5.5986 mL
	15 mM	0.1493 mL	0.7465 mL	1.4930 mL	3.7324 mL
	20 mM	0.1120 mL	0.5599 mL	1.1197 mL	2.7993 mL
	25 mM	0.0896 mL	0.4479 mL	0.8958 mL	2.2394 mL
	30 mM	0.0746 mL	0.3732 mL	0.7465 mL	1.8662 mL
	40 mM	0.0560 mL	0.2799 mL	0.5599 mL	1.3997 mL
	50 mM	0.0448 mL	0.2239 mL	0.4479 mL	1.1197 mL
	60 mM	0.0373 mL	0.1866 mL	0.3732 mL	0.9331 mL
	80 mM	0.0280 mL	0.1400 mL	0.2799 mL	0.6998 mL
	100 mM	0.0224 mL	0.1120 mL	0.2239 mL	0.5599 mL

Keywords

Erdafitinib

39 Cited Publications

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Erdafitinib

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Publications Citing Use of MedChemExpress (MCE) Erdafitinib

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Publications (39)

Lösungsmittel & Löslichkeit

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Reinheit & Dokumentation

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Help & FAQs

Complete Stock Solution Preparation Table

Erdafitinib Related Classifications

Art. -Nr.: HY-18708