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Purity: ≥98%
Erdafitinib (formerly known as JNJ-42756493; JNJ42756493; Balversa), a quinoxaline derivative compound and approved anticancer drug, is a novel, potent and selective, orally bioavailable, pan inhibitor of fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. Erdafitinib binds to FGFR1/2/3/4, with a mean pIC50 of approximately 9/8.5/8.5/8.25, correspondingly. JNJ-42756493 treatment reduces the proliferation of treated cells in vitro, which is linked to a rise in apoptosis and a decrease in cell survival. Drug therapy alone can delay the growth of NCI-H716 tumors in vivo by five days; however, when drug delivery is halted, the relative tumor volume increases in comparison to the control group. FGFR is a receptor tyrosine kinase that is crucial for the growth, differentiation, and survival of tumor cells. It is upregulated in a variety of tumor cell types.
| Targets |
FGFR1 (IC50 = 1.2 nM); FGFR2 (IC50 = 2.5 nM); FGFR3 (IC50 = 3.0 nM); FGFR4 (IC50 = 5.7 nM)
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| ln Vitro |
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| Enzyme Assay |
Erdafitinib (JNJ-42756493) is a potent FGFR family inhibitor that can be taken orally; its IC50 values for FGFR1/2/3/4 are 1.2, 2.5, 3.0, and 5.7 nM, respectively.
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| Cell Assay |
In DMSO, Erdafitinib is dissolved. Erdafitinib is used to treat KATO III, RT-112, A-204, RT-4, DMS-114, A-427, and MDA-MB-453 cells (final concentration: 2% DMSO; ranging from 10 μM to 0.01 nM). MTT reagent is used to assess the viability of the cells after a 4-day incubation period. A measurement of the optical density is made at 540 nm[1].
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| Animal Protocol |
Mice: Erdafitinib at doses of 0, 3, 10, or 30 mg/kg is administered orally to mice with xenograft tumors of SNU-16 human gastric carcinoma (FGFR2 amplified). At 0.5, 1, 3, 7, 16, and 24 hours after dosing, tumor tissue and mouse plasma are extracted from three mice per time point[1].
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| References |
| Molecular Formula |
C25H30N6O2
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| Molecular Weight |
446.54
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| Exact Mass |
446.24
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| Elemental Analysis |
C, 67.24; H, 6.77; N, 18.82; O, 7.17
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| CAS # |
1346242-81-6
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| Related CAS # |
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| Appearance |
Yellow solid powder
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| SMILES |
CC(C)NCCN(C1=CC2=NC(=CN=C2C=C1)C3=CN(N=C3)C)C4=CC(=CC(=C4)OC)OC
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| InChi Key |
OLAHOMJCDNXHFI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H30N6O2/c1-17(2)26-8-9-31(20-10-21(32-4)13-22(11-20)33-5)19-6-7-23-24(12-19)29-25(15-27-23)18-14-28-30(3)16-18/h6-7,10-17,26H,8-9H2,1-5H3
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| Chemical Name |
N'-(3,5-dimethoxyphenyl)-N'-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-N-propan-2-ylethane-1,2-diamine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (6.16 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (6.16 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.33 mg/mL (5.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (4.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.08 mg/mL (4.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: 5%DMSO+40%PEG300+5%Tween80+50%ddH2O: 22.25mg/ml |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02365597 | Active Recruiting |
Drug: Erdafitinib Drug: Midazolam |
Urothelial Cancer | Janssen Research & Development, LLC |
April 22, 2015 | Phase 2 |
| NCT03238196 | Active Recruiting |
Drug: Erdafitinib Drug: Palbociclib |
Metastatic Breast Cancer | Vanderbilt-Ingram Cancer Center | August 18, 2017 | Phase 1 |
| NCT04172675 | Active Recruiting |
Drug: Erdafitinib Drug: Investigator Choice (Mitomycin C) |
Urinary Bladder Neoplasms | Janssen Research & Development, LLC |
February 28, 2020 | Phase 2 |
| NCT02699606 | Active Recruiting |
Drug: Erdafitinib | Neoplasm | Janssen Research & Development, LLC |
July 8, 2016 | Phase 2 |
| NCT04083976 | Active Recruiting |
Drug: Erdafitinib | Advanced Solid Tumor | Janssen Research & Development, LLC |
November 20, 2019 | Phase 2 |
 JNJ-42756493 inhibits FGFR auto-phosphorylation in cancer cells lines with activated FGFR1-4 and FGFR-dependent signaling in NCI-H1581 cells.
Relationship betweenin vivoJNJ-42756493 plasma concentration, inhibition of pFGFR2, and efficacy in SNU-16 human gastric xenograft mouse model.Mol Cancer Ther.2017 Jun;16(6):1010-1020. |
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 JNJ-42756493 antiproliferative activity against human cancer cell lines.
Relationship betweenin vivoJNJ-42756493 plasma concentration, inhibition of pERK and efficacy in LUX001 PDX with FGFR3–TACC3 fusion mouse model.Mol Cancer Ther.2017 Jun;16(6):1010-1020. |
 Lysosomal accumulation of JNJ-42756493 and sustained inhibition of FGFR following compound washout.GAMG cells showing (A) intrinsic fluorescence of JNJ-427556493 (green), fluorescence of a lysosome staining probe (LysoTracker, red), and merging of the 2 images (merged, yellow).B,Reduced lysosomal fluorescence intensity of JNJ-42756493 and LysoTracker in the presence of bafilomycin (C) absence of changes in JNJ-42883919 fluorescence intensity compared with LysoTracker in the presence of bafilomycin.Mol Cancer Ther.2017 Jun;16(6):1010-1020. |
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