Erdafitinib
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- 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
Publications Citing Use of MedChemExpress (MCE) Erdafitinib
More- Cancer Discov. 2019 Dec;9(12):1686-1695. [Abstract]
- Adv Funct Mater. 2025 Jan 16.
- Cancer Res. 2026 Mar 12. [Abstract]
- Cancer Res. 2025 Dec 29. [Abstract]
- Cancer Res. 2025 Mar 24. [Abstract]
- Nat Commun. 2022 Aug 4;13(1):4534. [Abstract]
- Autophagy. 2025 Sep 29:1-19. [Abstract]
- Cell Death Dis. 2025 Jul 2;16(1):485. [Abstract]
- Free Radic Biol Med. 2024 Jul 4:S0891-5849(24)00548-3. [Abstract]
- NPJ Precis Oncol. 2023 Jul 21;7(1):70. [Abstract]
- Br J Pharmacol. 2025 Apr 21. [Abstract]
- Biomed Pharmacother. 2025 Oct 21:192:118677. [Abstract]
- Cell Rep. 2024 May 8;43(5):114211. [Abstract]
- Cell Rep. 2023 Apr 24;42(5):112437. [Abstract]
- Clin Transl Med. 2026 Mar;16(3):e70638. [Abstract]
- Br J Cancer. 2025 Dec 13. [Abstract]
- Breast Cancer Res. 2025 Jul 9;27(1):128. [Abstract]
- Mol Cancer Ther. 2025 Nov 20. [Abstract]
- J Chem Inf Model. 2024 Mar 25;64(6):2058-2067. [Abstract]
- Life Sci. 2025 Jan 28:364:123432. [Abstract]
- Int Immunopharmacol. 2025 Dec 23:170:116073. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2025 Aug 18;1871(8):168023. [Abstract]
- FASEB J. 2023 Apr;37(4):e22840. [Abstract]
- Chem Res Toxicol. 2021 Jul 19;34(7):1800-1813. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Heliyon. 2024 May 13.
- Heliyon. 2024 May 19;10(11):e30887. [Abstract]
- J Pharm Biomed Anal. 2022 May 30;214:114731. [Abstract]
- Mol Pharmacol. 2022 Jun;101(6):381-389. [Abstract]
- Biochim Biophys Acta Gen Subj. 2023 Sep 29;1867(12):130470. [Abstract]
- Anticancer Drugs. 2023 Oct 1;34(9):1035-1045. [Abstract]
- University of Auckland. 2025.
- bioRxiv. 2024 September 10.
- bioRxiv. 2024 Apr 25:2024.04.24.590626. [Abstract]
- bioRxiv. 2023 Nov 17.
- University of Brescia. 2023 Feb 2.
- Research Square Print. September 14th, 2022.
- Uppsala University. 2022 Feb.
- Oncotarget. 2020 Nov 3;11(44):3921-3932. [Abstract]
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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WB
-
RT-PCR
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IHC
Biologische Aktivität
|
FGFR1 1.2 nM (IC50) |
FGFR2 2.5 nM (IC50) |
FGFR3 3.0 nM (IC50) |
FGFR4 5.7 nM (IC50) |
|
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] |
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 Kd values of 0.24, 1.1, 1.4 and 2.2 nM, respectively. The Kd 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| 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
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Synonyms
JNJ-42756493
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (39)
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Journal Impact Factor
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Most Recent
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Cancer Discov
Acquired On-Target Clinical Resistance Validates FGFR4 as a Driver of Hepatocellular Carcinoma. [Abstract]2019 Dec;9(12):1686-1695. PMID: 31575540 -
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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
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.
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Nat Commun
2022 Aug 4;13(1):4534. PMID: 35927228 -
Autophagy
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 -
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Heliyon
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
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 -
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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 -
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Oncotarget
2020 Nov 3;11(44):3921-3932. PMID: 33216841
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protokoll
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.
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
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
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Handling Instructions (2659 KB)
Verweise
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.
| 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 |