Erdafitinib [1346242-81-6]
Cat# HY-18708-10mg
Size : 10mg
Brand : MedChemExpress
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.
Erdafitinib Chemical Structure
CAS No. : 1346242-81-6
This product is a controlled substance and not for sale in your territory.
Based on 21 publication(s) in Google Scholar
View All FGFR Isoform Specific Products:
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. |
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IC50 & Target[1] |
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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 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. |
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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. |
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Clinical Trial |
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Molecular Weight |
446.54 |
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Formula |
C25H30N6O2 |
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CAS No. |
1346242-81-6 |
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Appearance |
Solid |
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Color |
Light yellow to yellow |
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SMILES |
CN1N=CC(C2=NC3=CC(N(C4=CC(OC)=CC(OC)=C4)CCNC(C)C)=CC=C3N=C2)=C1 |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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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
View the Complete Stock Solution Preparation Table
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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.
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 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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume 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
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.
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Purity & Documentation |
Purity: 99.66% |
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References |
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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 |
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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
- Protein Tyrosine Kinase/RTK Apoptosis
- FGFR Apoptosis