Erdafitinib (Synonyms: JNJ-42756493)

Name: Erdafitinib
Brand: MedChemExpress
SKU: HY-18708
Rating: 5.0 (39 reviews)

Cat. No.: HY-18708 Purity: 99.66%: Data Sheet
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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.

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

CAS No. : 1346242-81-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 39 publication(s) in Google Scholar

Other Forms of Erdafitinib:

Erdafitinib (Standard) Get quote

39 Publications Citing Use of MCE Erdafitinib

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

RT-PCR

IHC

: 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.

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Description

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 3 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 3 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 3 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]
BaF3	IC₅₀	0.1 1 Compound: 5	Inhibition of VEGFR2 in mouse BAF3 cells Inhibition of VEGFR2 in mouse BAF3 cells	10.1039/C9MD90044F
AN3-CA	GI₅₀	0.048 3 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]
A2780	IC₅₀	0.02 3 Compound: Erdafitnib	Antiproliferative activity against human A2780 cells Antiproliferative activity against human A2780 cells	[PMID: 38964169]
AN3-CA	GI₅₀	0.048 3 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]
AN3-CA	GI₅₀	0.048 3 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 3 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	0.005 3 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	> 5 3 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	>5 3 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	0.005 3 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	0.005 3 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 3 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 3 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	0.761 3 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	0.761 3 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	> 300 1 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	GI₅₀	4.011 3 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	4.011 3 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	> 5 3 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]
HCT-116	IC₅₀	4.24 3 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]
SNU-16	IC₅₀	0.7 1 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]
BaF3	GI₅₀	> 5 3 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]
J82	GI₅₀	3.796 3 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]
Sf21	IC₅₀	3 1 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]
HCT-116	IC₅₀	4.24 3 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]
Jurkat	IC₅₀	6.81 3 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]
BaF3	IC₅₀	0.1 1 Compound: 5	Inhibition of VEGFR2 in mouse BAF3 cells Inhibition of VEGFR2 in mouse BAF3 cells	10.1039/C9MD90044F
K562	IC₅₀	3.02 3 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]
J82	GI₅₀	3.796 3 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]
DMS-114	IC₅₀	11 1 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]
Jurkat	IC₅₀	6.81 3 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]
KATO III stomach cancer cell line	IC₅₀	0.004 3 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]
KMS-11	GI₅₀	0.39 3 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]
K562	IC₅₀	3.02 3 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]
HCT-116	IC₅₀	4.24 3 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 3 Compound: Erdafitnib	Antiproliferative activity against human HCT-116 cells Antiproliferative activity against human HCT-116 cells	[PMID: 38964169]
Sf21	IC₅₀	3 1 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]
KATO III stomach cancer cell line	IC₅₀	0.004 3 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]
Sf21	IC₅₀	36.8 1 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]
Sf21	IC₅₀	36.8 1 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 3 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
KMS-11	GI₅₀	0.39 3 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]
J82	GI₅₀	3.796 3 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 3 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]
SNU-16	IC₅₀	0.0007 3 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]
Sf9	IC₅₀	0.003 3 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
Jurkat	IC₅₀	6.81 3 Compound: Erdafitnib	Antiproliferative activity against human Jurkat cells Antiproliferative activity against human Jurkat cells	[PMID: 38964169]
K562	GI₅₀	> 300 1 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 3 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	IC₅₀	3.02 3 Compound: Erdafitnib	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 38964169]
KG-1	IC₅₀	2.1 1 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 1 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 3 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 1 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 1 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 1 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 1 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 1 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 1 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 1 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 1 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 1 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 1 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 1 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]
SNU-16	IC₅₀	0.0007 3 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 1 Compound: Erdafitnib	Antiproliferative activity against human SNU-16 cells Antiproliferative activity against human SNU-16 cells	[PMID: 38964169]
SNU-16	IC₅₀	2.7 1 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]
Sf21	IC₅₀	3 1 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 1 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 3 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

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

Molecular Weight

446.54

Formula

C₂₅H₃₀N₆O₂

CAS No.

1346242-81-6

Appearance

Solid

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

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 : 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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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: 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(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: 99.66%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (253 KB) HNMR (227 KB) LCMS (120 KB)

Handling Instructions (2659 KB)

References

[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]

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

Complete Stock Solution Preparation Table

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

Erdafitinib 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:

Erdafitinib1346242-81-6JNJ-42756493JNJ42756493JNJ 42756493FGFRApoptosisFibroblast growth factor receptorInhibitorinhibitorinhibit

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Erdafitinib (Synonyms: JNJ-42756493)

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