Erdafitinib
Erdafitinib is an effective, selective and oral bioactive pan-fibroblast growth factor receptor FGFR inhibitor with potential anti-tumor activity and inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.In vitro, Erdafitinib-treated cells reduced proliferation, increased apoptotic death, and reduced cell survival. In vivo experiments, Erdafitinib treatment delayed the growth of NCI-H716 tumors, and when drug treatment was withdrawn, tumor volume increased.
| Storage | Store at -20°C |
| M.Wt | 446.54 |
| Cas No. | 1346242-81-6 |
| Formula | C25H30N6O2 |
| Synonyms | JNJ-42756493 |
| Solubility | insoluble in H2O; ≥15 mg/mL in EtOH; ≥54.5 mg/mL in DMSO |
| Chemical Name | N1-(3,5-dimethoxyphenyl)-N2-isopropyl-N1-(3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl)ethane-1,2-diamine |
| SDF | Download SDF |
| Canonical SMILES | CN(N=C1)C=C1C2=NC3=CC(N(CCNC(C)C)C4=CC(OC)=CC(OC)=C4)=CC=C3N=C2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Various colorectal cancer (CRC) cell lines with FGFR wild type (Caco2 and HCA7) and FGFR2 amplification (HCT116, NCI-H716) |
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Reaction Conditions |
72 h incubation |
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Applications |
Erdafitinib significantly decreased cell growth and survival of NCI-H716 cells at concentrations of ≧ 0.5nM, whereas ≧ 5000 nM was required for all other cell lines, including Caco2. |
| Animal experiment:[1] | |
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Animal models |
NMRI nu/nu female mice xenografted with NCI-H716 cells |
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Dosage form |
40 mg/kg Administered in the morning three times a week for three weeks by gavage |
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Applications |
In vivo, growth of NCI-H716 tumors was delayed by 5 days by drug treatment alone, although when drug delivery was stopped the relative tumor volume increased compared to control. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Verstraete M, Debucquoy A, Gonnissen A, et al. In vitro and in vivo evaluation of the radiosensitizing effect of a selective FGFR inhibitor (JNJ-42756493) for rectal cancer. BMC Cancer, 2015, 15: 946. |
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Quality Control & MSDS
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Chemical structure
