Erdafitinib (Synonyms: Erdafitinib) |
Catalog No.GC19142
One-Click Copy Product Info
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Erdafitinib is an orally available, selective tyrosine kinase inhibitor of the entire FGFR family (FGFR1: IC50 = 1.2nM; FGFR2: IC50 = 2.5nM; FGFR3: IC50 = 3.0nM; FGFR4: IC50 = 5.7nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1346242-81-6
Sample solution is provided at 25 µL, 10mM.
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Erdafitinib is an orally available, selective tyrosine kinase inhibitor of the entire FGFR family (FGFR1: IC50 = 1.2nM; FGFR2: IC50 = 2.5nM; FGFR3: IC50 = 3.0nM; FGFR4: IC50 = 5.7nM) [1]. Erdafitinib inhibits the proliferation and survival of cells with abnormal FGFR genes (such as FGFR3 or FGFR2 variants) by blocking phosphorylation and downstream signaling pathways, thereby inducing apoptosis [2-3]. Erdafitinib is primarily used to treat advanced or metastatic urothelial carcinoma harboring FGFR2/3 genetic abnormalities [4].
In HEK293 ABCB1 overexpressing cells, Erdafitinib (0.06-0.6μM; 2 h) enhances the sensitivity of cells to chemotherapeutic drugs [5]. In BV2 microglial cells, Erdafitinib (0.1-20μM; 24h) pretreatment decreases LPS-mediated proinflammatory cytokine expression through NLRP3 [6]. In MDA-MB-231 cells, Erdafitinib (0-100μM; 24h) inhibited the growth of cells in a dose-dependent manner [7].
In A549 cells xenograft tumor mouse model, Erdafitinib (10mg/kg; ip; 21d) suppresses tumor growth, accompanied by decreased CDK2 expression [8]. In SRM KO MGH-U3 cells xenograft tumor mouse model, combination of SRM deletion and Erdafitinib (5mg/kg, 15mg/kg; po; 4 weeks) targeted therapy elicited a complete inhibition of tumor growth [9].
References:
[1]. Perera T P S, Jovcheva E, Mevellec L, et al. Discovery and pharmacological characterization of JNJ-42756493 (Erdafitinib), a functionally selective small-molecule FGFR family inhibitor[J]. Molecular cancer therapeutics, 2017, 16(6): 1010-1020.
[2]. Haura E B, Hicks J K, Boyle T A. Erdafitinib overcomes FGFR3-TACC3–mediated resistance to osimertinib[J]. Journal of Thoracic Oncology, 2020, 15(9): e154-e156.
[3]. Kaur J, Singh A, Shah M, et al. Erdafitinib for tumors with FGFR3 mutation: A promising targeted therapy[J]. Cancer Research, Statistics, and Treatment, 2023, 6(2): 288-295.
[4]. Guercio B J, Sarfaty M, Teo M Y, et al. Clinical and genomic landscape of FGFR3-altered urothelial carcinoma and treatment outcomes with erdafitinib: a real-world experience[J]. Clinical Cancer Research, 2023, 29(22): 4586-4595.
[5]. Feng W, Zhang M, Wu Z X, et al. Erdafitinib antagonizes ABCB1-mediated multidrug resistance in cancer cells[J]. Frontiers in oncology, 2020, 10: 955.
[6]. Lee H, Kim S H, Jung T M, et al. Erdafitinib diminishes LPS-mediated neuroinflammatory responses through NLRP3 in wild-type mice[J]. Frontiers in Pharmacology, 2025, 16: 1572604.
[7]. Luo Q, Zhang L, Hao Y, et al. Erdafitinib inhibits the tumorigenicity of MDA-MB-231 triple-negative breast cancer cells by inducing TRIM25/ubiquitin-dependent degradation of FGFR4[J]. Breast Cancer Research, 2025, 27(1): 128.
[8]. Meng X, Zhu X, Ji J, et al. Erdafitinib inhibits tumorigenesis of human lung adenocarcinoma A549 by inducing S-phase cell-cycle arrest as a CDK2 inhibitor[J]. Molecules, 2022, 27(19): 6733.
[9]. Yu Y, Gao X, Zhao H, et al. A Genome-Wide Synthetic Lethal Screen Identifies Spermidine Synthase as a Target to Enhance Erdafitinib Efficacy in FGFR-Mutant Bladder Cancer[J]. Cancer Research, 2025, 85(12): 2288-2301.
| Cell experiment [1]: | |
Cell lines | HEK293 ABCB1 overexpressing cells |
Preparation Method | For reversal study, different concentrations of paclitaxel, vincristine, or cisplatin were added into the wells after cells pre-incubated with different concentrations (0.06, 0.2, or 0.6μM) of Erdafitinib for 2h. The cells were incubated for 72h. |
Reaction Conditions | 0.06-0.6μM; 2h |
Applications | Erdafitinib increased the sensitivity of chemotherapeutic drugs in HEK293 ABCB1 overexpressing cells. |
| Animal experiment [2]: | |
Animal models | A549 cells xenograft tumor mouse model |
Preparation Method | A549-Luc cells (5 × 107) were mixed with Matrigel (2:1) and injected subcutaneously into BALB/c nude mice. The mice were randomly divided into two groups (n = 3 per group): vehicle and Erdafitinib (10mg/kg), when the tumor volumes reached approximately 100mm3. Body weight and tumor volumes were measured every other day. |
Dosage form | 10mg/kg; ip; 21d |
Applications | In A549 cells xenograft tumor mouse model, Erdafitinib suppresses tumor growth suppresses tumor growth, accompanied by decreased CDK2 expression. |
References: | |
| Cas No. | 1346242-81-6 | SDF | |
| Synonyms | Erdafitinib | ||
| Canonical SMILES | CN1N=CC(C2=NC3=CC(N(C4=CC(OC)=CC(OC)=C4)CCNC(C)C)=CC=C3N=C2)=C1 | ||
| Formula | C25H30N6O2 | M.Wt | 446.54 |
| Solubility | DMSO : ≥ 33 mg/mL (73.90 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2394 mL | 11.1972 mL | 22.3944 mL |
| 5 mM | 447.9 μL | 2.2394 mL | 4.4789 mL |
| 10 mM | 223.9 μL | 1.1197 mL | 2.2394 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)